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Ro-3306 CDK1 inhibitor

N. Cat.: S7747

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
Ro-3306 CDK inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 351.45

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.96%
99.96

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

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
KB-3-1 adenocarcinoma cell line qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
human H460a cells Proliferation assay Antiproliferative activity against human H460a cells, IC50=1.04 μM 17303421
human MDA435 cells Proliferation assay Antiproliferative activity against human MDA435 cells, IC50=1.14 μM 17303421
human HCT116 cells Proliferation assay Antiproliferative activity against human HCT116 cells, IC50=1.14 μM 17303421
human RKO cells Proliferation assay Antiproliferative activity against human RKO cells, IC50=2 μM 17303421
human SW480 cells Proliferation assay Antiproliferative activity against human SW480 cells, IC50=2.2 μM 17303421
human SJSA1 cells Proliferation assay Antiproliferative activity against human SJSA1 cells, IC50=4.55 μM 17303421
human HCT116 cells Cytotoxic assay 5 days Cytotoxicity against human HCT116 cells after 5 days by MTS assay, IC50=3.2 μM 22326168
NCI-SNU-1 Growth inhibition assay Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 0.73095 μM. SANGER
H4 Growth inhibition assay Inhibition of human H4 cell growth in a cell viability assay, IC50 = 1.15875 μM. SANGER
PA-1 Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50 = 1.22654 μM. SANGER
T98G Growth inhibition assay Inhibition of human T98G cell growth in a cell viability assay, IC50 = 1.36812 μM. SANGER
SW1710 Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50 = 1.61408 μM. SANGER
U251 Growth inhibition assay Inhibition of human U251 cell growth in a cell viability assay, IC50 = 1.63771 μM. SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 1.90813 μM. SANGER
SK-N-DZ Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 2.01876 μM. SANGER
A4-Fuk Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 2.05604 μM. SANGER
639-V Growth inhibition assay Inhibition of human 639-V cell growth in a cell viability assay, IC50 = 2.27537 μM. SANGER
Hs-578-T Growth inhibition assay Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50 = 2.27799 μM. SANGER
UM-UC-3 Growth inhibition assay Inhibition of human UM-UC-3 cell growth in a cell viability assay, IC50 = 2.73936 μM. SANGER
BPH-1 Growth inhibition assay Inhibition of human BPH-1 cell growth in a cell viability assay, IC50 = 2.97455 μM. SANGER
5637 Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50 = 3.08532 μM. SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50 = 3.14049 μM. SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 3.23501 μM. SANGER
KOSC-2 Growth inhibition assay Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50 = 3.44662 μM. SANGER
COR-L88 Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50 = 3.47583 μM. SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 4.10805 μM. SANGER
LXF-289 Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50 = 4.2176 μM. SANGER
MN-60 Growth inhibition assay Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 4.37623 μM. SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50 = 4.47076 μM. SANGER
NCI-H2405 Growth inhibition assay Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50 = 4.74493 μM. SANGER
YH-13 Growth inhibition assay Inhibition of human YH-13 cell growth in a cell viability assay, IC50 = 4.75776 μM. SANGER
SK-MEL-2 Growth inhibition assay Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 5.09632 μM. SANGER
NB13 Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 5.32786 μM. SANGER
GAMG Growth inhibition assay Inhibition of human GAMG cell growth in a cell viability assay, IC50 = 5.3715 μM. SANGER
NCI-H1792 Growth inhibition assay Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50 = 5.47954 μM. SANGER
KP-4 Growth inhibition assay Inhibition of human KP-4 cell growth in a cell viability assay, IC50 = 5.69823 μM. SANGER
HGC-27 Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50 = 5.73077 μM. SANGER
GCT Growth inhibition assay Inhibition of human GCT cell growth in a cell viability assay, IC50 = 5.85121 μM. SANGER
PFSK-1 Growth inhibition assay Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50 = 5.86168 μM. SANGER
A172 Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50 = 5.9079 μM. SANGER
HO-1-N-1 Growth inhibition assay Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50 = 5.95425 μM. SANGER
HN Growth inhibition assay Inhibition of human HN cell growth in a cell viability assay, IC50 = 5.97097 μM. SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50 = 5.97521 μM. SANGER
TGW Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50 = 6.05682 μM. SANGER
COR-L23 Growth inhibition assay Inhibition of human COR-L23 cell growth in a cell viability assay, IC50 = 6.3735 μM. SANGER
D-566MG Growth inhibition assay Inhibition of human D-566MG cell growth in a cell viability assay, IC50 = 6.78873 μM. SANGER
SKG-IIIa Growth inhibition assay Inhibition of human SKG-IIIa cell growth in a cell viability assay, IC50 = 6.85572 μM. SANGER
NCI-H446 Growth inhibition assay Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50 = 7.0181 μM. SANGER
KYSE-270 Growth inhibition assay Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50 = 7.03872 μM. SANGER
CAL-39 Growth inhibition assay Inhibition of human CAL-39 cell growth in a cell viability assay, IC50 = 7.3524 μM. SANGER
IST-SL1 Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50 = 7.43349 μM. SANGER
SF539 Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50 = 7.55197 μM. SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 7.89091 μM. SANGER
NB10 Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 7.98758 μM. SANGER
8505C Growth inhibition assay Inhibition of human 8505C cell growth in a cell viability assay, IC50 = 7.99817 μM. SANGER
DB Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50 = 8.01131 μM. SANGER
NCI-H28 Growth inhibition assay Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50 = 8.59884 μM. SANGER
LOXIMVI Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 8.63701 μM. SANGER
ME-180 Growth inhibition assay Inhibition of human ME-180 cell growth in a cell viability assay, IC50 = 8.80395 μM. SANGER
ES3 Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 9.12794 μM. SANGER
SK-N-FI Growth inhibition assay Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 9.41699 μM. SANGER
NBsusSR Growth inhibition assay Inhibition of human NBsusSR cell growth in a cell viability assay, IC50 = 10.2318 μM. SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50 = 10.2783 μM. SANGER
A704 Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50 = 10.3318 μM. SANGER
HuP-T4 Growth inhibition assay Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50 = 10.4271 μM. SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50 = 11.1574 μM. SANGER
MCF7 Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50 = 11.1849 μM. SANGER
A549 Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50 = 11.206 μM. SANGER
HD-MY-Z Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50 = 11.206 μM. SANGER
HCC1395 Growth inhibition assay Inhibition of human HCC1395 cell growth in a cell viability assay, IC50 = 11.5596 μM. SANGER
SK-NEP-1 Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 11.7332 μM. SANGER
HSC-2 Growth inhibition assay Inhibition of human HSC-2 cell growth in a cell viability assay, IC50 = 11.7842 μM. SANGER
HCC1937 Growth inhibition assay Inhibition of human HCC1937 cell growth in a cell viability assay, IC50 = 11.8473 μM. SANGER
RS4-11 Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 11.8836 μM. SANGER
CAL-27 Growth inhibition assay Inhibition of human CAL-27 cell growth in a cell viability assay, IC50 = 12.1637 μM. SANGER
NCI-H23 Growth inhibition assay Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50 = 12.4155 μM. SANGER
A431 Growth inhibition assay Inhibition of human A431 cell growth in a cell viability assay, IC50 = 12.7233 μM. SANGER
HT-1080 Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50 = 12.7373 μM. SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 12.7716 μM. SANGER
BFTC-909 Growth inhibition assay Inhibition of human BFTC-909 cell growth in a cell viability assay, IC50 = 13.1068 μM. SANGER
CAL-33 Growth inhibition assay Inhibition of human CAL-33 cell growth in a cell viability assay, IC50 = 13.6518 μM. SANGER
JVM-3 Growth inhibition assay Inhibition of human JVM-3 cell growth in a cell viability assay, IC50 = 14.2627 μM. SANGER
AN3-CA Growth inhibition assay Inhibition of human AN3-CA cell growth in a cell viability assay, IC50 = 14.9578 μM. SANGER
VM-CUB-1 Growth inhibition assay Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50 = 15.1364 μM. SANGER
A253 Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay, IC50 = 15.2834 μM. SANGER
RPMI-7951 Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50 = 16.1981 μM. SANGER
NCI-H1563 Growth inhibition assay Inhibition of human NCI-H1563 cell growth in a cell viability assay, IC50 = 16.8253 μM. SANGER
LB831-BLC Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50 = 17.1929 μM. SANGER
ES8 Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50 = 17.3157 μM. SANGER
NCI-H292 Growth inhibition assay Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50 = 17.4749 μM. SANGER
OAW-42 Growth inhibition assay Inhibition of human OAW-42 cell growth in a cell viability assay, IC50 = 17.8823 μM. SANGER
RCC10RGB Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 17.9578 μM. SANGER
PC-3 Growth inhibition assay Inhibition of human PC-3 cell growth in a cell viability assay, IC50 = 18.0043 μM. SANGER
HCC38 Growth inhibition assay Inhibition of human HCC38 cell growth in a cell viability assay, IC50 = 18.1031 μM. SANGER
DEL Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50 = 18.387 μM. SANGER
ABC-1 Growth inhibition assay Inhibition of human ABC-1 cell growth in a cell viability assay, IC50 = 18.5627 μM. SANGER
SW756 Growth inhibition assay Inhibition of human SW756 cell growth in a cell viability assay, IC50 = 19.1351 μM. SANGER
TE-6 Growth inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 19.2103 μM. SANGER
H-EMC-SS Growth inhibition assay Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50 = 19.4359 μM. SANGER
HCT-116 Growth inhibition assay Inhibition of human HCT-116 cell growth in a cell viability assay, IC50 = 19.668 μM. SANGER
CHP-212 Growth inhibition assay Inhibition of human CHP-212 cell growth in a cell viability assay, IC50 = 19.7478 μM. SANGER
SK-LU-1 Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50 = 19.753 μM. SANGER
HT-3 Growth inhibition assay Inhibition of human HT-3 cell growth in a cell viability assay, IC50 = 20.028 μM. SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 20.206 μM. SANGER
ES1 Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 21.0048 μM. SANGER
Ramos-2G6-4C10 Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 21.7756 μM. SANGER
IA-LM Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay, IC50 = 21.9694 μM. SANGER
BHT-101 Growth inhibition assay Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 22.0629 μM. SANGER
OVCAR-4 Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 22.47 μM. SANGER
SW1573 Growth inhibition assay Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 22.7934 μM. SANGER
CHL-1 Growth inhibition assay Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 23.2833 μM. SANGER
BFTC-905 Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 23.2892 μM. SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 23.5782 μM. SANGER
NCI-H358 Growth inhibition assay Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50 = 23.6477 μM. SANGER
OVCAR-5 Growth inhibition assay Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50 = 24.104 μM. SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 25.0804 μM. SANGER
SNU-423 Growth inhibition assay Inhibition of human SNU-423 cell growth in a cell viability assay, IC50 = 25.366 μM. SANGER
CP50-MEL-B Growth inhibition assay Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 25.7399 μM. SANGER
NCI-H2087 Growth inhibition assay Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 25.8655 μM. SANGER
RMG-I Growth inhibition assay Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 25.9219 μM. SANGER
KP-N-YS Growth inhibition assay Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 26.202 μM. SANGER
OMC-1 Growth inhibition assay Inhibition of human OMC-1 cell growth in a cell viability assay, IC50 = 26.508 μM. SANGER
DMS-114 Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50 = 27.3966 μM. SANGER
SHP-77 Growth inhibition assay Inhibition of human SHP-77 cell growth in a cell viability assay, IC50 = 27.488 μM. SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 27.9438 μM. SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 28.4535 μM. SANGER
D-283MED Growth inhibition assay Inhibition of human D-283MED cell growth in a cell viability assay, IC50 = 28.4674 μM. SANGER
MOLT-4 Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 28.9072 μM. SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 29.6436 μM. SANGER
NB6 Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50 = 29.8638 μM. SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 29.9407 μM. SANGER
A388 Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50 = 29.9422 μM. SANGER
OAW-28 Growth inhibition assay Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 30.2278 μM. SANGER
SK-MES-1 Growth inhibition assay Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 31.2208 μM. SANGER
NCI-H441 Growth inhibition assay Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 31.9868 μM. SANGER
HOP-92 Growth inhibition assay Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 32.2356 μM. SANGER
NB14 Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50 = 32.7251 μM. SANGER
MS-1 Growth inhibition assay Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 32.7604 μM. SANGER
YKG-1 Growth inhibition assay Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 32.8336 μM. SANGER
SiHa Growth inhibition assay Inhibition of human SiHa cell growth in a cell viability assay, IC50 = 33.3829 μM. SANGER
HAL-01 Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 34.2376 μM. SANGER
Ca-Ski Growth inhibition assay Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50 = 34.7669 μM. SANGER
NCI-H747 Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 34.9875 μM. SANGER
KYSE-510 Growth inhibition assay Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50 = 35.6485 μM. SANGER
A204 Growth inhibition assay Inhibition of human A204 cell growth in a cell viability assay, IC50 = 35.7209 μM. SANGER
HSC-3 Growth inhibition assay Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 36.0086 μM. SANGER
HuP-T3 Growth inhibition assay Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 36.4832 μM. SANGER
RPMI-8226 Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 36.6208 μM. SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 36.644 μM. SANGER
HuH-7 Growth inhibition assay Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 38.6184 μM. SANGER
CAL-12T Growth inhibition assay Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 38.9416 μM. SANGER
GT3TKB Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 39.1921 μM. SANGER
OC-314 Growth inhibition assay Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 39.7125 μM. SANGER
NCI-H2228 Growth inhibition assay Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 40.1403 μM. SANGER
NCI-H727 Growth inhibition assay Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 40.2531 μM. SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 40.4706 μM. SANGER
MMAC-SF Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50 = 40.9235 μM. SANGER
HTC-C3 Growth inhibition assay Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 41.4169 μM. SANGER
SF295 Growth inhibition assay Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 41.5379 μM. SANGER
U-2-OS Growth inhibition assay Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 41.8567 μM. SANGER
HPAF-II Growth inhibition assay Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 41.9382 μM. SANGER
KYSE-450 Growth inhibition assay Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 42.4707 μM. SANGER
DMS-273 Growth inhibition assay Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 43.2836 μM. SANGER
HT-1376 Growth inhibition assay Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 43.3156 μM. SANGER
786-0 Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 43.6261 μM. SANGER
NCI-H810 Growth inhibition assay Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50 = 44.0136 μM. SANGER
8305C Growth inhibition assay Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 44.645 μM. SANGER
DSH1 Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50 = 45.7042 μM. SANGER
KYSE-520 Growth inhibition assay Inhibition of human KYSE-520 cell growth in a cell viability assay, IC50 = 46.5721 μM. SANGER
TYK-nu Growth inhibition assay Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 46.7092 μM. SANGER
EPLC-272H Growth inhibition assay Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 46.7283 μM. SANGER
T-24 Growth inhibition assay Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 47.9292 μM. SANGER
BHY Growth inhibition assay Inhibition of human BHY cell growth in a cell viability assay, IC50 = 47.999 μM. SANGER
NCI-H82 Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 48.217 μM. SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50 = 48.6189 μM. SANGER
C-33-A Growth inhibition assay Inhibition of human C-33-A cell growth in a cell viability assay, IC50 = 48.7554 μM. SANGER
MIA-PaCa-2 Growth inhibition assay Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 48.8388 μM. SANGER
HCC1954 Growth inhibition assay Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 49.0871 μM. SANGER
NCI-H1666 Growth inhibition assay Inhibition of human NCI-H1666 cell growth in a cell viability assay, IC50 = 49.3642 μM. SANGER
GR-ST Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 49.3695 μM. SANGER
Ca9-22 Growth inhibition assay Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 49.4013 μM. SANGER
D-502MG Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 49.417 μM. SANGER
SCC-4 Growth inhibition assay Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 49.5602 μM. SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50 = 49.8356 μM. SANGER
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 351.45 Formula

C18H13N3OS2

Conservazione (Dalla data di ricezione)
N. CAS 872573-93-8 Scarica SDF Conservazione delle soluzioni stock

Sinonimi N/A Smiles C1=CC2=C(C=CC(=C2)C=C3C(=O)NC(=NCC4=CC=CS4)S3)N=C1

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 70 mg/mL (199.17 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:

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)

mg/kg g μL

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)

Targets/IC50/Ki
CDK1
(Cell-free assay)
20 nM(Ki)
PKCδ
(Cell-free assay)
318 nM(Ki)
SGK
(Cell-free assay)
497 nM(Ki)
ERK
(Cell-free assay)
1980 nM(Ki)
In vitro

RO-3306 inhibits CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D activity with Ki of 35 nM, 110 nM, 340 nM, and over 2000 nM, respectively. Treatment of HCT116, SW480, and HeLa cells with RO-3306 for 20 h leads to a complete block of the cell cycle in the G2/M phase. The proliferation of both HCT116 and SW480 is effectively blocked by RO-3306. RO-3306 appears to be more proapoptotic in cancer cells (HCT116 and SW480) than nontumorigenic cells (MCF 10A and MCF 12A).

RO-3306 effectively arrests oocyte maturation at a concentration of 10 μM.

Saggio chinasico
Saggio CDK
L'attività di CDK1 ciclina B1, CDK1 ciclina A, CDK2 ciclina E e CDK4 ciclina D viene misurata mediante un saggio di fluorescenza risolta nel tempo omogeneo in un formato a 96 pozzetti. Il tampone di saggio conteneva 25 mM Hepes, 6,25 mM MgCl2, 0,003% Tween 20, 0,3 mg/mL BSA, 1,5 mM DTT e ATP come segue: 162 μM (CDK1), 90 mM (CDK2) o 135 μM (CDK4). Il tampone CDK1 e CDK2 conteneva 10 mM MgCl2. I composti di prova vengono diluiti nel tampone di saggio a 3 volte la loro concentrazione finale in 20 μL, e la reazione viene avviata con l'aggiunta di 40 μL di tampone di saggio contenente il substrato pRB (0,185 μM). Le piastre vengono incubate a 37°C per 30 min con agitazione costante, e la reazione viene terminata con l'aggiunta di 15 μL di anticorpo anti-pRB fosforilato (Ser-780) 1,6 μM in 25 mM Hepes, 24 mM EDTA e 0,2 mg/mL BSA. Dopo un'ulteriore incubazione di 30 min con agitazione, vengono aggiunti 15 μL di IgG anti-coniglio marcata con Lance-Eu-W1024 3 nM e 60 nM di anticorpo anti-His-6 coniugato con alloficocianina in 25 mM Hepes e 0,5 mg/mL BSA e incubati per 1 ora. Le piastre vengono lette nel lettore multi-etichette Victor-V con eccitazione a 340 nm ed emissione a 615 nm e 665 nm. I valori IC50 vengono calcolati dalle letture a 665 nm e normalizzati per le letture dell'Europio a 615 nm. I valori Ki vengono calcolati secondo l'equazione: Ki= IC50/(1 + S/Km ), dove S è la concentrazione di ATP nel saggio e Km è la costante di Michaelis-Menten per l'ATP. L'attività inibitoria contro il pannello di chinasi è determinata dalla tecnologia di saggio IMAP.
In vivo

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor.

Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/35367281/

Applicazioni (Applications)

Metodi Biomarcatori Immagini PMID
Western blot p-Cdk1 / Cdk1 / Cleaved PARP / Cleaved caspase-3 / p-p38 / Bad / Apaf1-1 / p-H2Ax / Bim / Bad
S7747-WB1
27385216
Immunofluorescence PARP1 / Plk1
S7747-IF1
28069876
Growth inhibition assay Cell viability
S7747-viability1
27385216