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AZD6244 (Selumetinib) inibitore di MEK1/2

Name: AZD6244 (Selumetinib)
Brand: Selleck Chemicals
SKU: S1008
Rating: 5 (711 reviews)

N. Cat.S1008

Selumetinib (AZD6244, ARRY-142886) è un potente e altamente selettivo inibitore di MEK con IC50 di 14 nM per MEK1 e valore di Kd di 530 nM per MEK2. Inoltre, inibisce la fosforilazione di ERK1/2 con IC50 di 10 nM, senza inibizione di p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, ecc. Selumetinib sopprime la proliferazione cellulare, la migrazione e innesca l'apoptosi. Fase 3.

AZD6244 (Selumetinib) MEK Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 457.68

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.80%

99.80

Prodotti spesso usati con AZD6244 (Selumetinib)

AZD0364 (ATG-017)

Combination use of this compound and AZD0364 results in significant tumor regressions in multiple KRAS-mutant xenograft models.

AZD8055

It and AZD8055 lead to enhanced antitumor efficacy in KRAS-mutant human NSCLC xenograft models.

Target correlati	ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Altro MEK Inibitori	PD0325901 (Mirdametinib) U0126-EtOH PD 98059 CI-1040 (PD184352) (E/Z)-BIX02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 GDC-0623

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dell'attività	PMID
CHP-212	Growth inhibition assay		Inhibition of human CHP-212 cell growth in a cell viability assay, IC50 = 0.003153 μM.	SANGER
H9	Growth inhibition assay		Inhibition of human H9 cell growth in a cell viability assay, IC50 = 0.02288 μM.	SANGER
HL-60	Growth inhibition assay		Inhibition of human HL-60 cell growth in a cell viability assay, IC50 = 0.02459 μM.	SANGER
NOMO-1	Growth inhibition assay		Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50 = 0.03197 μM.	SANGER
DU-4475	Growth inhibition assay		Inhibition of human DU-4475 cell growth in a cell viability assay, IC50 = 0.03367 μM.	SANGER
M14	Growth inhibition assay		Inhibition of human M14 cell growth in a cell viability assay, IC50 = 0.03689 μM.	SANGER
HT-144	Growth inhibition assay		Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 0.08905 μM.	SANGER
SK-N-AS	Growth inhibition assay		Inhibition of human SK-N-AS cell growth in a cell viability assay, IC50 = 0.09283 μM.	SANGER
LB2518-MEL	Growth inhibition assay		Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50 = 0.09382 μM.	SANGER
C32	Growth inhibition assay		Inhibition of human C32 cell growth in a cell viability assay, IC50 = 0.09823 μM.	SANGER
BHT-101	Growth inhibition assay		Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 0.10693 μM.	SANGER
KY821	Growth inhibition assay		Inhibition of human KY821 cell growth in a cell viability assay, IC50 = 0.10718 μM.	SANGER
CP50-MEL-B	Growth inhibition assay		Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 0.12794 μM.	SANGER
MEL-HO	Growth inhibition assay		Inhibition of human MEL-HO cell growth in a cell viability assay, IC50 = 0.13884 μM.	SANGER
EoL-1-cell	Growth inhibition assay		Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50 = 0.14476 μM.	SANGER
DOK	Growth inhibition assay		Inhibition of human DOK cell growth in a cell viability assay, IC50 = 0.14708 μM.	SANGER
SH-4	Growth inhibition assay		Inhibition of human SH-4 cell growth in a cell viability assay, IC50 = 0.16648 μM.	SANGER
BPH-1	Growth inhibition assay		Inhibition of human BPH-1 cell growth in a cell viability assay, IC50 = 0.18231 μM.	SANGER
HuP-T4	Growth inhibition assay		Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50 = 0.19532 μM.	SANGER
KU812	Growth inhibition assay		Inhibition of human KU812 cell growth in a cell viability assay, IC50 = 0.21168 μM.	SANGER
A549	Growth inhibition assay		Inhibition of human A549 cell growth in a cell viability assay, IC50 = 0.21413 μM.	SANGER
HTC-C3	Growth inhibition assay		Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 0.21461 μM.	SANGER
A101D	Growth inhibition assay		Inhibition of human A101D cell growth in a cell viability assay, IC50 = 0.24033 μM.	SANGER
ONS-76	Growth inhibition assay		Inhibition of human ONS-76 cell growth in a cell viability assay, IC50 = 0.24453 μM.	SANGER
RKO	Growth inhibition assay		Inhibition of human RKO cell growth in a cell viability assay, IC50 = 0.24838 μM.	SANGER
WM-115	Growth inhibition assay		Inhibition of human WM-115 cell growth in a cell viability assay, IC50 = 0.26754 μM.	SANGER
HCC2998	Growth inhibition assay		Inhibition of human HCC2998 cell growth in a cell viability assay, IC50 = 0.26907 μM.	SANGER
C2BBe1	Growth inhibition assay		Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50 = 0.27259 μM.	SANGER
RVH-421	Growth inhibition assay		Inhibition of human RVH-421 cell growth in a cell viability assay, IC50 = 0.27939 μM.	SANGER
H-EMC-SS	Growth inhibition assay		Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50 = 0.29099 μM.	SANGER
ML-2	Growth inhibition assay		Inhibition of human ML-2 cell growth in a cell viability assay, IC50 = 0.29363 μM.	SANGER
SW620	Growth inhibition assay		Inhibition of human SW620 cell growth in a cell viability assay, IC50 = 0.3022 μM.	SANGER
UACC-257	Growth inhibition assay		Inhibition of human UACC-257 cell growth in a cell viability assay, IC50 = 0.32184 μM.	SANGER
AsPC-1	Growth inhibition assay		Inhibition of human AsPC-1 cell growth in a cell viability assay, IC50 = 0.32439 μM.	SANGER
CAL-39	Growth inhibition assay		Inhibition of human CAL-39 cell growth in a cell viability assay, IC50 = 0.33226 μM.	SANGER
COLO-679	Growth inhibition assay		Inhibition of human COLO-679 cell growth in a cell viability assay, IC50 = 0.34119 μM.	SANGER
NCI-H747	Growth inhibition assay		Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 0.35098 μM.	SANGER
NCI-H1437	Growth inhibition assay		Inhibition of human NCI-H1437 cell growth in a cell viability assay, IC50 = 0.35285 μM.	SANGER
PSN1	Growth inhibition assay		Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 0.36609 μM.	SANGER
NKM-1	Growth inhibition assay		Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 0.3858 μM.	SANGER
MZ2-MEL	Growth inhibition assay		Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50 = 0.39437 μM.	SANGER
SK-MEL-2	Growth inhibition assay		Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 0.40506 μM.	SANGER
LAMA-84	Growth inhibition assay		Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 0.45622 μM.	SANGER
U-266	Growth inhibition assay		Inhibition of human U-266 cell growth in a cell viability assay, IC50 = 0.48774 μM.	SANGER
RCM-1	Growth inhibition assay		Inhibition of human RCM-1 cell growth in a cell viability assay, IC50 = 0.49385 μM.	SANGER
EM-2	Growth inhibition assay		Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 0.51175 μM.	SANGER
Mewo	Growth inhibition assay		Inhibition of human Mewo cell growth in a cell viability assay, IC50 = 0.52101 μM.	SANGER
COLO-741	Growth inhibition assay		Inhibition of human COLO-741 cell growth in a cell viability assay, IC50 = 0.53119 μM.	SANGER
ACN	Growth inhibition assay		Inhibition of human ACN cell growth in a cell viability assay, IC50 = 0.5669 μM.	SANGER
MV-4-11	Growth inhibition assay		Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50 = 0.57543 μM.	SANGER
SW780	Growth inhibition assay		Inhibition of human SW780 cell growth in a cell viability assay, IC50 = 0.66634 μM.	SANGER
JVM-3	Growth inhibition assay		Inhibition of human JVM-3 cell growth in a cell viability assay, IC50 = 0.7006 μM.	SANGER
RPMI-8226	Growth inhibition assay		Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 0.74 μM.	SANGER
HO-1-N-1	Growth inhibition assay		Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50 = 0.74052 μM.	SANGER
BV-173	Growth inhibition assay		Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 0.74802 μM.	SANGER
NCI-H2291	Growth inhibition assay		Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50 = 0.76173 μM.	SANGER
SK-MEL-30	Growth inhibition assay		Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50 = 0.78171 μM.	SANGER
LB2241-RCC	Growth inhibition assay		Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 0.78991 μM.	SANGER
LOXIMVI	Growth inhibition assay		Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 0.85854 μM.	SANGER
HT-29	Growth inhibition assay		Inhibition of human HT-29 cell growth in a cell viability assay, IC50 = 0.87319 μM.	SANGER
KG-1	Growth inhibition assay		Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 0.89547 μM.	SANGER
SW954	Growth inhibition assay		Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 0.89645 μM.	SANGER
MIA-PaCa-2	Growth inhibition assay		Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 0.89768 μM.	SANGER
HCE-T	Growth inhibition assay		Inhibition of human HCE-T cell growth in a cell viability assay, IC50 = 0.97131 μM.	SANGER
HN	Growth inhibition assay		Inhibition of human HN cell growth in a cell viability assay, IC50 = 1.00257 μM.	SANGER
LCLC-97TM1	Growth inhibition assay		Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50 = 1.03191 μM.	SANGER
NB69	Growth inhibition assay		Inhibition of human NB69 cell growth in a cell viability assay, IC50 = 1.0539 μM.	SANGER
LoVo	Growth inhibition assay		Inhibition of human LoVo cell growth in a cell viability assay, IC50 = 1.06231 μM.	SANGER
HCT-116	Growth inhibition assay		Inhibition of human HCT-116 cell growth in a cell viability assay, IC50 = 1.06431 μM.	SANGER
AGS	Growth inhibition assay		Inhibition of human AGS cell growth in a cell viability assay, IC50 = 1.11831 μM.	SANGER
NCI-H292	Growth inhibition assay		Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50 = 1.1199 μM.	SANGER
P12-ICHIKAWA	Growth inhibition assay		Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50 = 1.15899 μM.	SANGER
D-263MG	Growth inhibition assay		Inhibition of human D-263MG cell growth in a cell viability assay, IC50 = 1.18094 μM.	SANGER
COLO-792	Growth inhibition assay		Inhibition of human COLO-792 cell growth in a cell viability assay, IC50 = 1.1863 μM.	SANGER
HSC-3	Growth inhibition assay		Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 1.18823 μM.	SANGER
NUGC-3	Growth inhibition assay		Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50 = 1.20379 μM.	SANGER
SW872	Growth inhibition assay		Inhibition of human SW872 cell growth in a cell viability assay, IC50 = 1.26855 μM.	SANGER
HuCCT1	Growth inhibition assay		Inhibition of human HuCCT1 cell growth in a cell viability assay, IC50 = 1.2996 μM.	SANGER
QIMR-WIL	Growth inhibition assay		Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 1.34384 μM.	SANGER
NCI-H2087	Growth inhibition assay		Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 1.3751 μM.	SANGER
LS-513	Growth inhibition assay		Inhibition of human LS-513 cell growth in a cell viability assay, IC50 = 1.42191 μM.	SANGER
CAL-54	Growth inhibition assay		Inhibition of human CAL-54 cell growth in a cell viability assay, IC50 = 1.49314 μM.	SANGER
A204	Growth inhibition assay		Inhibition of human A204 cell growth in a cell viability assay, IC50 = 1.51667 μM.	SANGER
CAL-62	Growth inhibition assay		Inhibition of human CAL-62 cell growth in a cell viability assay, IC50 = 1.52292 μM.	SANGER
CAL-33	Growth inhibition assay		Inhibition of human CAL-33 cell growth in a cell viability assay, IC50 = 1.54694 μM.	SANGER
COLO-678	Growth inhibition assay		Inhibition of human COLO-678 cell growth in a cell viability assay, IC50 = 1.62382 μM.	SANGER
MEG-01	Growth inhibition assay		Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 1.62959 μM.	SANGER
HAL-01	Growth inhibition assay		Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 1.6957 μM.	SANGER
OAW-28	Growth inhibition assay		Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 1.74397 μM.	SANGER
NCI-SNU-1	Growth inhibition assay		Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 1.77243 μM.	SANGER
BHY	Growth inhibition assay		Inhibition of human BHY cell growth in a cell viability assay, IC50 = 1.81034 μM.	SANGER
EGI-1	Growth inhibition assay		Inhibition of human EGI-1 cell growth in a cell viability assay, IC50 = 1.8282 μM.	SANGER
BB65-RCC	Growth inhibition assay		Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50 = 1.83855 μM.	SANGER
GAK	Growth inhibition assay		Inhibition of human GAK cell growth in a cell viability assay, IC50 = 1.90475 μM.	SANGER
SK-MEL-3	Growth inhibition assay		Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50 = 1.95077 μM.	SANGER
KARPAS-45	Growth inhibition assay		Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 2.08248 μM.	SANGER
BCPAP	Growth inhibition assay		Inhibition of human BCPAP cell growth in a cell viability assay, IC50 = 2.1274 μM.	SANGER
RT-112	Growth inhibition assay		Inhibition of human RT-112 cell growth in a cell viability assay, IC50 = 2.26046 μM.	SANGER
SK-HEP-1	Growth inhibition assay		Inhibition of human SK-HEP-1 cell growth in a cell viability assay, IC50 = 2.29048 μM.	SANGER
Ca9-22	Growth inhibition assay		Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 2.37667 μM.	SANGER
OS-RC-2	Growth inhibition assay		Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50 = 2.40337 μM.	SANGER
BFTC-905	Growth inhibition assay		Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 2.42312 μM.	SANGER
HT-1080	Growth inhibition assay		Inhibition of human HT-1080 cell growth in a cell viability assay, IC50 = 2.4301 μM.	SANGER
HCC2218	Growth inhibition assay		Inhibition of human HCC2218 cell growth in a cell viability assay, IC50 = 2.48487 μM.	SANGER
KM12	Growth inhibition assay		Inhibition of human KM12 cell growth in a cell viability assay, IC50 = 2.53961 μM.	SANGER
NB5	Growth inhibition assay		Inhibition of human NB5 cell growth in a cell viability assay, IC50 = 2.56641 μM.	SANGER
BB30-HNC	Growth inhibition assay		Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50 = 2.71293 μM.	SANGER
NCI-H460	Growth inhibition assay		Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50 = 2.80274 μM.	SANGER
LAN-6	Growth inhibition assay		Inhibition of human LAN-6 cell growth in a cell viability assay, IC50 = 2.82867 μM.	SANGER
EW-3	Growth inhibition assay		Inhibition of human EW-3 cell growth in a cell viability assay, IC50 = 2.92505 μM.	SANGER
CAL-27	Growth inhibition assay		Inhibition of human CAL-27 cell growth in a cell viability assay, IC50 = 3.06118 μM.	SANGER
COR-L105	Growth inhibition assay		Inhibition of human COR-L105 cell growth in a cell viability assay, IC50 = 3.13462 μM.	SANGER
EFO-21	Growth inhibition assay		Inhibition of human EFO-21 cell growth in a cell viability assay, IC50 = 3.19226 μM.	SANGER
MZ1-PC	Growth inhibition assay		Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50 = 3.31605 μM.	SANGER
EFO-27	Growth inhibition assay		Inhibition of human EFO-27 cell growth in a cell viability assay, IC50 = 3.32612 μM.	SANGER
HPAF-II	Growth inhibition assay		Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 3.33729 μM.	SANGER
KU-19-19	Growth inhibition assay		Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50 = 3.41951 μM.	SANGER
NCI-SNU-5	Growth inhibition assay		Inhibition of human NCI-SNU-5 cell growth in a cell viability assay, IC50 = 3.61449 μM.	SANGER
LS-123	Growth inhibition assay		Inhibition of human LS-123 cell growth in a cell viability assay, IC50 = 3.61831 μM.	SANGER
769-P	Growth inhibition assay		Inhibition of human 769-P cell growth in a cell viability assay, IC50 = 3.7426 μM.	SANGER
SJSA-1	Growth inhibition assay		Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50 = 3.78146 μM.	SANGER
SK-LU-1	Growth inhibition assay		Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50 = 3.86231 μM.	SANGER
A3-KAW	Growth inhibition assay		Inhibition of human A3-KAW cell growth in a cell viability assay, IC50 = 3.91055 μM.	SANGER
LB996-RCC	Growth inhibition assay		Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50 = 3.95043 μM.	SANGER
SN12C	Growth inhibition assay		Inhibition of human SN12C cell growth in a cell viability assay, IC50 = 3.95573 μM.	SANGER
COR-L23	Growth inhibition assay		Inhibition of human COR-L23 cell growth in a cell viability assay, IC50 = 3.95669 μM.	SANGER
VM-CUB-1	Growth inhibition assay		Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50 = 3.96931 μM.	SANGER
RXF393	Growth inhibition assay		Inhibition of human RXF393 cell growth in a cell viability assay, IC50 = 4.01591 μM.	SANGER
MOLT-13	Growth inhibition assay		Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50 = 4.03419 μM.	SANGER
GCT	Growth inhibition assay		Inhibition of human GCT cell growth in a cell viability assay, IC50 = 4.10442 μM.	SANGER
SW1990	Growth inhibition assay		Inhibition of human SW1990 cell growth in a cell viability assay, IC50 = 4.16622 μM.	SANGER
RD	Growth inhibition assay		Inhibition of human RD cell growth in a cell viability assay, IC50 = 4.19138 μM.	SANGER
HOP-92	Growth inhibition assay		Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 4.20093 μM.	SANGER
ME-180	Growth inhibition assay		Inhibition of human ME-180 cell growth in a cell viability assay, IC50 = 4.25859 μM.	SANGER
MZ7-mel	Growth inhibition assay		Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50 = 4.45265 μM.	SANGER
CAKI-1	Growth inhibition assay		Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50 = 4.46057 μM.	SANGER
YKG-1	Growth inhibition assay		Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 4.53421 μM.	SANGER
PANC-03-27	Growth inhibition assay		Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50 = 4.53929 μM.	SANGER
A4-Fuk	Growth inhibition assay		Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 4.54202 μM.	SANGER
NCI-H441	Growth inhibition assay		Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 4.56342 μM.	SANGER
BxPC-3	Growth inhibition assay		Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50 = 4.65976 μM.	SANGER
ES3	Growth inhibition assay		Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 4.69173 μM.	SANGER
GP5d	Growth inhibition assay		Inhibition of human GP5d cell growth in a cell viability assay, IC50 = 4.78553 μM.	SANGER
CAL-85-1	Growth inhibition assay		Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50 = 4.7942 μM.	SANGER
EPLC-272H	Growth inhibition assay		Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 4.81698 μM.	SANGER
HuP-T3	Growth inhibition assay		Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 4.82408 μM.	SANGER
SW1710	Growth inhibition assay		Inhibition of human SW1710 cell growth in a cell viability assay, IC50 = 5.03549 μM.	SANGER
TE-8	Growth inhibition assay		Inhibition of human TE-8 cell growth in a cell viability assay, IC50 = 5.06911 μM.	SANGER
TE-12	Growth inhibition assay		Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 5.13703 μM.	SANGER
NCI-H1573	Growth inhibition assay		Inhibition of human NCI-H1573 cell growth in a cell viability assay, IC50 = 5.27238 μM.	SANGER
SW1417	Growth inhibition assay		Inhibition of human SW1417 cell growth in a cell viability assay, IC50 = 5.27398 μM.	SANGER
CHL-1	Growth inhibition assay		Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 5.3199 μM.	SANGER
Calu-6	Growth inhibition assay		Inhibition of human Calu-6 cell growth in a cell viability assay, IC50 = 5.42927 μM.	SANGER
MDA-MB-231	Growth inhibition assay		Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50 = 5.56523 μM.	SANGER
SCC-25	Growth inhibition assay		Inhibition of human SCC-25 cell growth in a cell viability assay, IC50 = 5.97121 μM.	SANGER
639-V	Growth inhibition assay		Inhibition of human 639-V cell growth in a cell viability assay, IC50 = 6.12933 μM.	SANGER
D-502MG	Growth inhibition assay		Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 6.17659 μM.	SANGER
PANC-10-05	Growth inhibition assay		Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50 = 6.20181 μM.	SANGER
Ramos-2G6-4C10	Growth inhibition assay		Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 6.27094 μM.	SANGER
NB10	Growth inhibition assay		Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 6.32533 μM.	SANGER
MSTO-211H	Growth inhibition assay		Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50 = 6.4008 μM.	SANGER
NCI-H1651	Growth inhibition assay		Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50 = 6.65328 μM.	SANGER
697	Growth inhibition assay		Inhibition of human 697 cell growth in a cell viability assay, IC50 = 6.67397 μM.	SANGER
HCC70	Growth inhibition assay		Inhibition of human HCC70 cell growth in a cell viability assay, IC50 = 6.68865 μM.	SANGER
SW1116	Growth inhibition assay		Inhibition of human SW1116 cell growth in a cell viability assay, IC50 = 6.81297 μM.	SANGER
SK-MES-1	Growth inhibition assay		Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 6.8488 μM.	SANGER
GCIY	Growth inhibition assay		Inhibition of human GCIY cell growth in a cell viability assay, IC50 = 6.91962 μM.	SANGER
GMS-10	Growth inhibition assay		Inhibition of human GMS-10 cell growth in a cell viability assay, IC50 = 7.07755 μM.	SANGER
NCI-H1092	Growth inhibition assay		Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50 = 7.15334 μM.	SANGER
CFPAC-1	Growth inhibition assay		Inhibition of human CFPAC-1 cell growth in a cell viability assay, IC50 = 7.22101 μM.	SANGER
TK10	Growth inhibition assay		Inhibition of human TK10 cell growth in a cell viability assay, IC50 = 7.35587 μM.	SANGER
FADU	Growth inhibition assay		Inhibition of human FADU cell growth in a cell viability assay, IC50 = 7.5093 μM.	SANGER
8305C	Growth inhibition assay		Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 7.85355 μM.	SANGER
DK-MG	Growth inhibition assay		Inhibition of human DK-MG cell growth in a cell viability assay, IC50 = 7.94937 μM.	SANGER
BFTC-909	Growth inhibition assay		Inhibition of human BFTC-909 cell growth in a cell viability assay, IC50 = 7.97836 μM.	SANGER
IGR-1	Growth inhibition assay		Inhibition of human IGR-1 cell growth in a cell viability assay, IC50 = 8.18051 μM.	SANGER
MDA-MB-361	Growth inhibition assay		Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50 = 8.1824 μM.	SANGER
KYSE-150	Growth inhibition assay		Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50 = 8.21937 μM.	SANGER
DB	Growth inhibition assay		Inhibition of human DB cell growth in a cell viability assay, IC50 = 8.36905 μM.	SANGER
NH-12	Growth inhibition assay		Inhibition of human NH-12 cell growth in a cell viability assay, IC50 = 8.42736 μM.	SANGER
CTV-1	Growth inhibition assay		Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 8.43337 μM.	SANGER
A498	Growth inhibition assay		Inhibition of human A498 cell growth in a cell viability assay, IC50 = 8.78475 μM.	SANGER
LS-1034	Growth inhibition assay		Inhibition of human LS-1034 cell growth in a cell viability assay, IC50 = 8.96464 μM.	SANGER
FTC-133	Growth inhibition assay		Inhibition of human FTC-133 cell growth in a cell viability assay, IC50 = 8.98459 μM.	SANGER
TGBC11TKB	Growth inhibition assay		Inhibition of human TGBC11TKB cell growth in a cell viability assay, IC50 = 9.10836 μM.	SANGER
SK-MEL-1	Growth inhibition assay		Inhibition of human SK-MEL-1 cell growth in a cell viability assay, IC50 = 9.19136 μM.	SANGER
RPMI-7951	Growth inhibition assay		Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50 = 9.25201 μM.	SANGER
GT3TKB	Growth inhibition assay		Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 9.37403 μM.	SANGER
SW962	Growth inhibition assay		Inhibition of human SW962 cell growth in a cell viability assay, IC50 = 9.52325 μM.	SANGER
T-24	Growth inhibition assay		Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 9.65807 μM.	SANGER
DBTRG-05MG	Growth inhibition assay		Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50 = 9.75666 μM.	SANGER
G-401	Growth inhibition assay		Inhibition of human G-401 cell growth in a cell viability assay, IC50 = 10.0739 μM.	SANGER
RS4-11	Growth inhibition assay		Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 10.2791 μM.	SANGER
KGN	Growth inhibition assay		Inhibition of human KGN cell growth in a cell viability assay, IC50 = 10.4046 μM.	SANGER
786-0	Growth inhibition assay		Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 10.4166 μM.	SANGER
EW-18	Growth inhibition assay		Inhibition of human EW-18 cell growth in a cell viability assay, IC50 = 10.4366 μM.	SANGER
DEL	Growth inhibition assay		Inhibition of human DEL cell growth in a cell viability assay, IC50 = 10.545 μM.	SANGER
HuH-7	Growth inhibition assay		Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 10.5705 μM.	SANGER
MG-63	Growth inhibition assay		Inhibition of human MG-63 cell growth in a cell viability assay, IC50 = 10.7333 μM.	SANGER
A253	Growth inhibition assay		Inhibition of human A253 cell growth in a cell viability assay, IC50 = 10.7902 μM.	SANGER
TGW	Growth inhibition assay		Inhibition of human TGW cell growth in a cell viability assay, IC50 = 10.7937 μM.	SANGER
HH	Growth inhibition assay		Inhibition of human HH cell growth in a cell viability assay, IC50 = 10.8062 μM.	SANGER
LS-411N	Growth inhibition assay		Inhibition of human LS-411N cell growth in a cell viability assay, IC50 = 10.8244 μM.	SANGER
NCI-H2347	Growth inhibition assay		Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50 = 10.8437 μM.	SANGER
LU-65	Growth inhibition assay		Inhibition of human LU-65 cell growth in a cell viability assay, IC50 = 10.9226 μM.	SANGER
TE-11	Growth inhibition assay		Inhibition of human TE-11 cell growth in a cell viability assay, IC50 = 11.025 μM.	SANGER
SBC-1	Growth inhibition assay		Inhibition of human SBC-1 cell growth in a cell viability assay, IC50 = 11.1032 μM.	SANGER
TGBC24TKB	Growth inhibition assay		Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50 = 11.118 μM.	SANGER
ECC10	Growth inhibition assay		Inhibition of human ECC10 cell growth in a cell viability assay, IC50 = 11.2283 μM.	SANGER
GR-ST	Growth inhibition assay		Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 11.268 μM.	SANGER
NCI-H720	Growth inhibition assay		Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50 = 11.3977 μM.	SANGER
VA-ES-BJ	Growth inhibition assay		Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50 = 11.5513 μM.	SANGER
MOLT-16	Growth inhibition assay		Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 12.1161 μM.	SANGER
KYSE-140	Growth inhibition assay		Inhibition of human KYSE-140 cell growth in a cell viability assay, IC50 = 12.1596 μM.	SANGER
SCC-4	Growth inhibition assay		Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 12.24 μM.	SANGER
NCI-H1155	Growth inhibition assay		Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50 = 12.3017 μM.	SANGER
OCUB-M	Growth inhibition assay		Inhibition of human OCUB-M cell growth in a cell viability assay, IC50 = 12.3189 μM.	SANGER
MN-60	Growth inhibition assay		Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 12.3732 μM.	SANGER
RO82-W-1	Growth inhibition assay		Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50 = 12.3879 μM.	SANGER
KOSC-2	Growth inhibition assay		Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50 = 12.5508 μM.	SANGER
L-363	Growth inhibition assay		Inhibition of human L-363 cell growth in a cell viability assay, IC50 = 12.5925 μM.	SANGER
NCI-H661	Growth inhibition assay		Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50 = 12.8587 μM.	SANGER
KYSE-450	Growth inhibition assay		Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 13.0396 μM.	SANGER
TI-73	Growth inhibition assay		Inhibition of human TI-73 cell growth in a cell viability assay, IC50 = 13.044 μM.	SANGER
KNS-81-FD	Growth inhibition assay		Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50 = 13.0748 μM.	SANGER
HCC1954	Growth inhibition assay		Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 13.2783 μM.	SANGER
A427	Growth inhibition assay		Inhibition of human A427 cell growth in a cell viability assay, IC50 = 13.6689 μM.	SANGER
MOLT-4	Growth inhibition assay		Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 13.8531 μM.	SANGER
U-118-MG	Growth inhibition assay		Inhibition of human U-118-MG cell growth in a cell viability assay, IC50 = 13.8702 μM.	SANGER
SF126	Growth inhibition assay		Inhibition of human SF126 cell growth in a cell viability assay, IC50 = 13.9165 μM.	SANGER
SF539	Growth inhibition assay		Inhibition of human SF539 cell growth in a cell viability assay, IC50 = 13.9474 μM.	SANGER
Daoy	Growth inhibition assay		Inhibition of human Daoy cell growth in a cell viability assay, IC50 = 14.4979 μM.	SANGER
DoTc2-4510	Growth inhibition assay		Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50 = 14.5175 μM.	SANGER
TYK-nu	Growth inhibition assay		Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 14.56 μM.	SANGER
CGTH-W-1	Growth inhibition assay		Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 14.8483 μM.	SANGER
HuO9	Growth inhibition assay		Inhibition of human HuO9 cell growth in a cell viability assay, IC50 = 15.063 μM.	SANGER
EW-16	Growth inhibition assay		Inhibition of human EW-16 cell growth in a cell viability assay, IC50 = 15.0949 μM.	SANGER
NCI-H630	Growth inhibition assay		Inhibition of human NCI-H630 cell growth in a cell viability assay, IC50 = 15.1613 μM.	SANGER
CAL-12T	Growth inhibition assay		Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 15.331 μM.	SANGER
TE-5	Growth inhibition assay		Inhibition of human TE-5 cell growth in a cell viability assay, IC50 = 15.6133 μM.	SANGER
U251	Growth inhibition assay		Inhibition of human U251 cell growth in a cell viability assay, IC50 = 15.7383 μM.	SANGER
BB49-HNC	Growth inhibition assay		Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50 = 16.506 μM.	SANGER
OCI-AML2	Growth inhibition assay		Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50 = 16.665 μM.	SANGER
KINGS-1	Growth inhibition assay		Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50 = 16.6918 μM.	SANGER
D-566MG	Growth inhibition assay		Inhibition of human D-566MG cell growth in a cell viability assay, IC50 = 16.7262 μM.	SANGER
P30-OHK	Growth inhibition assay		Inhibition of human P30-OHK cell growth in a cell viability assay, IC50 = 16.9068 μM.	SANGER
GAMG	Growth inhibition assay		Inhibition of human GAMG cell growth in a cell viability assay, IC50 = 16.9243 μM.	SANGER
HCC1419	Growth inhibition assay		Inhibition of human HCC1419 cell growth in a cell viability assay, IC50 = 17.6139 μM.	SANGER
SNU-C2B	Growth inhibition assay		Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50 = 17.7377 μM.	SANGER
MHH-NB-11	Growth inhibition assay		Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50 = 18.1383 μM.	SANGER
COLO-684	Growth inhibition assay		Inhibition of human COLO-684 cell growth in a cell viability assay, IC50 = 18.2383 μM.	SANGER
OC-314	Growth inhibition assay		Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 18.358 μM.	SANGER
Becker	Growth inhibition assay		Inhibition of human Becker cell growth in a cell viability assay, IC50 = 18.4623 μM.	SANGER
NCI-H1623	Growth inhibition assay		Inhibition of human NCI-H1623 cell growth in a cell viability assay, IC50 = 18.6368 μM.	SANGER
IGROV-1	Growth inhibition assay		Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50 = 18.6559 μM.	SANGER
HSC-2	Growth inhibition assay		Inhibition of human HSC-2 cell growth in a cell viability assay, IC50 = 18.9577 μM.	SANGER
RMG-I	Growth inhibition assay		Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 19.1338 μM.	SANGER
CAL-120	Growth inhibition assay		Inhibition of human CAL-120 cell growth in a cell viability assay, IC50 = 19.2354 μM.	SANGER
GB-1	Growth inhibition assay		Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 19.7444 μM.	SANGER
LU-139	Growth inhibition assay		Inhibition of human LU-139 cell growth in a cell viability assay, IC50 = 20.1816 μM.	SANGER
HT-1376	Growth inhibition assay		Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 20.5772 μM.	SANGER
SW982	Growth inhibition assay		Inhibition of human SW982 cell growth in a cell viability assay, IC50 = 20.6837 μM.	SANGER
SK-N-FI	Growth inhibition assay		Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 21.0886 μM.	SANGER
SCC-9	Growth inhibition assay		Inhibition of human SCC-9 cell growth in a cell viability assay, IC50 = 21.1409 μM.	SANGER
SW756	Growth inhibition assay		Inhibition of human SW756 cell growth in a cell viability assay, IC50 = 21.2156 μM.	SANGER
SW948	Growth inhibition assay		Inhibition of human SW948 cell growth in a cell viability assay, IC50 = 21.5236 μM.	SANGER
SW1573	Growth inhibition assay		Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 21.8345 μM.	SANGER
NCI-H1792	Growth inhibition assay		Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50 = 21.8565 μM.	SANGER
BE-13	Growth inhibition assay		Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 22.5873 μM.	SANGER
SK-OV-3	Growth inhibition assay		Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50 = 22.7388 μM.	SANGER
PA-1	Growth inhibition assay		Inhibition of human PA-1 cell growth in a cell viability assay, IC50 = 22.8712 μM.	SANGER
NCI-H1693	Growth inhibition assay		Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50 = 22.9313 μM.	SANGER
no-10	Growth inhibition assay		Inhibition of human no-10 cell growth in a cell viability assay, IC50 = 23.3588 μM.	SANGER
JVM-2	Growth inhibition assay		Inhibition of human JVM-2 cell growth in a cell viability assay, IC50 = 23.4147 μM.	SANGER
SK-NEP-1	Growth inhibition assay		Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 23.5205 μM.	SANGER
PC-3	Growth inhibition assay		Inhibition of human PC-3 cell growth in a cell viability assay, IC50 = 23.5722 μM.	SANGER
U-2-OS	Growth inhibition assay		Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 23.8469 μM.	SANGER
NBsusSR	Growth inhibition assay		Inhibition of human NBsusSR cell growth in a cell viability assay, IC50 = 24.1062 μM.	SANGER
EW-13	Growth inhibition assay		Inhibition of human EW-13 cell growth in a cell viability assay, IC50 = 24.1398 μM.	SANGER
BT-20	Growth inhibition assay		Inhibition of human BT-20 cell growth in a cell viability assay, IC50 = 24.7178 μM.	SANGER
MS-1	Growth inhibition assay		Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 25.0498 μM.	SANGER
HCC1187	Growth inhibition assay		Inhibition of human HCC1187 cell growth in a cell viability assay, IC50 = 25.4451 μM.	SANGER
TE-1	Growth inhibition assay		Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 25.6953 μM.	SANGER
MKN7	Growth inhibition assay		Inhibition of human MKN7 cell growth in a cell viability assay, IC50 = 25.7913 μM.	SANGER
NCI-H727	Growth inhibition assay		Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 26.0513 μM.	SANGER
H4	Growth inhibition assay		Inhibition of human H4 cell growth in a cell viability assay, IC50 = 26.3768 μM.	SANGER
647-V	Growth inhibition assay		Inhibition of human 647-V cell growth in a cell viability assay, IC50 = 26.8811 μM.	SANGER
KM-H2	Growth inhibition assay		Inhibition of human KM-H2 cell growth in a cell viability assay, IC50 = 26.924 μM.	SANGER
ABC-1	Growth inhibition assay		Inhibition of human ABC-1 cell growth in a cell viability assay, IC50 = 27.1974 μM.	SANGER
HCC1806	Growth inhibition assay		Inhibition of human HCC1806 cell growth in a cell viability assay, IC50 = 27.3422 μM.	SANGER
ES5	Growth inhibition assay		Inhibition of human ES5 cell growth in a cell viability assay, IC50 = 27.4999 μM.	SANGER
C3A	Growth inhibition assay		Inhibition of human C3A cell growth in a cell viability assay, IC50 = 27.5694 μM.	SANGER
TE-10	Growth inhibition assay		Inhibition of human TE-10 cell growth in a cell viability assay, IC50 = 27.6356 μM.	SANGER
S-117	Growth inhibition assay		Inhibition of human S-117 cell growth in a cell viability assay, IC50 = 27.7571 μM.	SANGER
TGBC1TKB	Growth inhibition assay		Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50 = 27.9902 μM.	SANGER
NCI-H1793	Growth inhibition assay		Inhibition of human NCI-H1793 cell growth in a cell viability assay, IC50 = 28.3076 μM.	SANGER
ES4	Growth inhibition assay		Inhibition of human ES4 cell growth in a cell viability assay, IC50 = 28.7352 μM.	SANGER
AN3-CA	Growth inhibition assay		Inhibition of human AN3-CA cell growth in a cell viability assay, IC50 = 28.8593 μM.	SANGER
NMC-G1	Growth inhibition assay		Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50 = 29.111 μM.	SANGER
NCI-H226	Growth inhibition assay		Inhibition of human NCI-H226 cell growth in a cell viability assay, IC50 = 29.2701 μM.	SANGER
NCI-H522	Growth inhibition assay		Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50 = 29.8339 μM.	SANGER
SW48	Growth inhibition assay		Inhibition of human SW48 cell growth in a cell viability assay, IC50 = 29.9252 μM.	SANGER
OE33	Growth inhibition assay		Inhibition of human OE33 cell growth in a cell viability assay, IC50 = 30.7954 μM.	SANGER
NCI-H2228	Growth inhibition assay		Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 31.0344 μM.	SANGER
D-423MG	Growth inhibition assay		Inhibition of human D-423MG cell growth in a cell viability assay, IC50 = 31.0564 μM.	SANGER
IST-MEL1	Growth inhibition assay		Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50 = 31.1528 μM.	SANGER
A388	Growth inhibition assay		Inhibition of human A388 cell growth in a cell viability assay, IC50 = 31.6236 μM.	SANGER
LN-405	Growth inhibition assay		Inhibition of human LN-405 cell growth in a cell viability assay, IC50 = 31.7983 μM.	SANGER
DMS-273	Growth inhibition assay		Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 31.9138 μM.	SANGER
KS-1	Growth inhibition assay		Inhibition of human KS-1 cell growth in a cell viability assay, IC50 = 33.1321 μM.	SANGER
NCI-H209	Growth inhibition assay		Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50 = 33.4517 μM.	SANGER
HOS	Growth inhibition assay		Inhibition of human HOS cell growth in a cell viability assay, IC50 = 33.7253 μM.	SANGER
GI-1	Growth inhibition assay		Inhibition of human GI-1 cell growth in a cell viability assay, IC50 = 33.8071 μM.	SANGER
RERF-LC-MS	Growth inhibition assay		Inhibition of human RERF-LC-MS cell growth in a cell viability assay, IC50 = 34.0315 μM.	SANGER
NCI-H526	Growth inhibition assay		Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50 = 34.076 μM.	SANGER
RPMI-2650	Growth inhibition assay		Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50 = 34.4334 μM.	SANGER
KYSE-70	Growth inhibition assay		Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50 = 34.8426 μM.	SANGER
Capan-2	Growth inhibition assay		Inhibition of human Capan-2 cell growth in a cell viability assay, IC50 = 36.4652 μM.	SANGER
OVCAR-4	Growth inhibition assay		Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 37.2176 μM.	SANGER
OVCAR-8	Growth inhibition assay		Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50 = 37.9823 μM.	SANGER
NCI-H1355	Growth inhibition assay		Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50 = 38.1051 μM.	SANGER
COLO-680N	Growth inhibition assay		Inhibition of human COLO-680N cell growth in a cell viability assay, IC50 = 38.2429 μM.	SANGER
NCI-H2122	Growth inhibition assay		Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50 = 39.3363 μM.	SANGER
Saos-2	Growth inhibition assay		Inhibition of human Saos-2 cell growth in a cell viability assay, IC50 = 39.7053 μM.	SANGER
HCC2157	Growth inhibition assay		Inhibition of human HCC2157 cell growth in a cell viability assay, IC50 = 40.7734 μM.	SANGER
VMRC-RCZ	Growth inhibition assay		Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50 = 41.2962 μM.	SANGER
ETK-1	Growth inhibition assay		Inhibition of human ETK-1 cell growth in a cell viability assay, IC50 = 41.5751 μM.	SANGER
RCC10RGB	Growth inhibition assay		Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 42.018 μM.	SANGER
KP-N-YS	Growth inhibition assay		Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 42.0641 μM.	SANGER
T98G	Growth inhibition assay		Inhibition of human T98G cell growth in a cell viability assay, IC50 = 42.6733 μM.	SANGER
A431	Growth inhibition assay		Inhibition of human A431 cell growth in a cell viability assay, IC50 = 45.1831 μM.	SANGER
HDLM-2	Growth inhibition assay		Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50 = 45.2617 μM.	SANGER
CHP-134	Growth inhibition assay		Inhibition of human CHP-134 cell growth in a cell viability assay, IC50 = 46.1779 μM.	SANGER
J-RT3-T3-5	Growth inhibition assay		Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50 = 46.4461 μM.	SANGER
NCI-H1650	Growth inhibition assay		Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50 = 46.5104 μM.	SANGER
MHH-PREB-1	Growth inhibition assay		Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50 = 46.5266 μM.	SANGER
SJRH30	Growth inhibition assay		Inhibition of human SJRH30 cell growth in a cell viability assay, IC50 = 46.7775 μM.	SANGER
SF295	Growth inhibition assay		Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 48.519 μM.	SANGER
YAPC	Growth inhibition assay		Inhibition of human YAPC cell growth in a cell viability assay, IC50 = 48.942 μM.	SANGER
EFM-19	Growth inhibition assay		Inhibition of human EFM-19 cell growth in a cell viability assay, IC50 = 49.5085 μM.	SANGER
MIAPaCa2	Proliferation assay		Antiproliferative activity against human MIAPaCa2 cells, IC50=142 nM.	23474388
A375	Proliferation assay	72 h	Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=31 nM.	23474388
A549	Antiproliferative assay		Antiproliferative activity against human A549 cells, IC50 = 1.75 μM.	23474388
LoVo	Antiproliferative assay		Antiproliferative activity against human LoVo cells, IC50 = 2.83 μM.	23474388
HCT116	Antiproliferative assay		Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant, IC50 = 3.1 μM.	23474388
HeLa-MaTu	Function assay		Inhibition of MEK1 in human HeLa-MaTu matched pair cells assessed as reduction in ERK phosphorylation, IC50 = 0.014 μM.	26611920
HepG2	Antiproliferative assay		Antiproliferative activity against human HepG2 cells harboring N-Ras mutation, IC50 = 0.032 μM.	26611920
COLO205	Antiproliferative assay		Antiproliferative activity against human COLO205 cells harboring BRAF mutation, IC50 = 0.069 μM.	26611920
A549	Antiproliferative assay		Antiproliferative activity against human A549 cells harboring K-Ras mutation, IC50 = 1.75 μM.	26611920
HCT116	Antiproliferative assay		Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation, IC50 = 3 μM.	26611920
HeLa-MaTu-ADR	Function assay		Inhibition of MEK1 in human HeLa-MaTu-ADR matched pair cells assessed as reduction in ERK phosphorylation, IC50 = 3.7 μM.	26611920
SW480	Antiproliferative assay	72 hrs	Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay, IC50 = 0.422 μM.	27448918
SW620	Antiproliferative assay	72 hrs	Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.015 μM.	28038940
AsPC1	Antiproliferative assay	72 hrs	Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.0642 μM.	28038940
BA/F3	Antiproliferative assay	72 hrs	Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.1 μM.	28038940
SKCO1	Antiproliferative assay	72 hrs	Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.117 μM.	28038940
COLO205	Antiproliferative assay	72 hrs	Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay, IC50 = 0.059 μM.	29317148
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	457.68	Formula	C₁₇H₁₅BrClFN₄O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	606143-52-6	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	ARRY-142886			Smiles	CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 91 mg/mL (198.82 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	5.000mg/ml (10.92mM)	Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Caratteristiche	First MEK inhibitor being tested in Phase II clinical trials.
Targets/IC₅₀/Ki	MEK1 (Cell-free assay) 14 nM MEK1 (Cell-free assay) 99 nM(Kd) MEK2 (Cell-free assay) 530 nM(Kd)
In vitro	Selumetinib (AZD6244) non è competitivo con l'ATP e inattiva la fosforilazione di ERK1/2 con concentrazioni IC50 inferiori a 40 nM. Inoltre, inibisce la crescita delle cellule primarie di HCC attraverso l'inibizione della fosforilazione di ERK1/2 e p90^RSK, accompagnata dall'aumento della scissione di caspasi-3 e caspasi-7 e della poli(ADP)ribosio polimerasi scissa. Questo composto ha pochi effetti sulle vie p38, c-Jun-NH₂-chinasi, fosfatidilinositolo 3-chinasi e MEK5/ERK5. È sensibile alle mutazioni Raf nelle linee cellulari di carcinoma mammario e alle mutazioni Ras nelle linee cellulari di NSCLC.
Saggio chinasico	Saggio dell'attività della chinasi MEK
Saggio chinasico	Selumetinib (AZD6244) viene utilizzato per immunopreparare le molecole di MEK1. L'attività della chinasi MEK viene misurata come la capacità di MEK1 immuno-isolata di attivare ERK1 ricombinante in un saggio accoppiato utilizzando MBP come punto finale del saggio. L'MBP fosforilato viene risolto su un gel SDS-PAGE al 14% ed essiccato sotto vuoto prima dell'esposizione al film a raggi X.
In vivo	Selumetinib (AZD6244) inibisce significativamente la fosforilazione di ERK1/2 in xenotrapianti 2-1318, 5-1318, 26-1004 e 4-1318 e induce l'apoptosi nelle cellule primarie 2-1318 attivando la via delle caspasi. Potrebbe inibire la crescita tumorale negli xenotrapianti HT-29, che è un modello di tumore colorettale portatore di una mutazione B-Raf, a una dose di 100 mg/kg e l'inibizione della crescita tumorale di questo composto è migliore. Altrimenti, potrebbe inibire la crescita tumorale degli xenotrapianti di HCC, che è associata ad un aumento dell'apoptosi e ad una downregulation dei regolatori del ciclo cellulare, tra cui ciclina D1, Cdc-2, CDK2 e 4, ciclina B1 e c-Myc.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/17237274/ [2] https://pubmed.ncbi.nlm.nih.gov/20587667/ [3] https://pubmed.ncbi.nlm.nih.gov/17332304/ [4] https://pubmed.ncbi.nlm.nih.gov/17876044/ [5] https://pubmed.ncbi.nlm.nih.gov/17699718/ [6] https://pubmed.ncbi.nlm.nih.gov/22173548/ [7] https://pubmed.ncbi.nlm.nih.gov/22641227/ [8] https://pubmed.ncbi.nlm.nih.gov/18381570/ [9] https://pubmed.ncbi.nlm.nih.gov/19915144/ [10] https://pubmed.ncbi.nlm.nih.gov/18676837/ [11] https://pubmed.ncbi.nlm.nih.gov/18676837/ [12] https://pubmed.ncbi.nlm.nih.gov/21385921/ [13] https://pubmed.ncbi.nlm.nih.gov/22037378/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	p-ERK / ERK / β-catenin / E-cadherin / Vimentin / Fibronection pS6(235/236) / pS6(240/244) pVEGFR(Y1175) / VEGFR2 / pPDGFRβ(Y751) / pPDGFRβ / pAXL(Y702) / AXL / pMEK / MEK Bak / Bad / Bcl-xl / BimEL / BimL / BimS / PUMA / NOXA	26384399
Immunofluorescence	β-catenin FOXO3a	26384399
Growth inhibition assay	Cell viability	26384399

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05253131	Not yet recruiting	MPNST\|NF1\|Sarcoma	University of Alabama at Birmingham\|United States Department of Defense	June 15 2024	Phase 2
NCT06175637	Recruiting	Neurofibroma Plexiform	AstraZeneca	December 20 2023	--
NCT05891847	Recruiting	Neurofibroma	AstraZeneca	March 21 2023	--
NCT05101148	Active not recruiting	Neurofibromatosis Type 1	AstraZeneca\|Merck Sharp & Dohme LLC	July 21 2021	Phase 1
NCT04879160	Completed	Neurofibromatosis 1	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 12 2021	--

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
How about the solubility of it? How to prepare for the solution if I need to do the in vivo experiments?

Risposta:
It will be a suspension for oral administration in vehicle 5% DMSO+30% PEG 300+ddH2O. If you want a clear solution for injection, you can dissolve it in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O.

C1=C0/X	C1:	LOG(C1):
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C4=C3/X	C4:	LOG(C4):
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C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):