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WH-4-023 Inibitore di Lck/Src

Name: WH-4-023
Brand: Selleck Chemicals
SKU: S7565
Rating: 5 (32 reviews)

N. Cat.S7565

WH-4-023 (KIN001-112, KIN112, inibitore doppio LCK/SRC) è un potente inibitore di Lck/Src attivo per via orale con IC50s di 2 nM e 6 nM in saggi senza cellule, rispettivamente. Mostra una selettività >300 volte superiore contro p38α e KDR. Inoltre, inibisce potentemente SIK (i valori di IC50 sono 10, 22 e 60 nM per SIK 1, 2 e 3 rispettivamente) e mostra selettività su una serie di chinasi strettamente correlate.

WH-4-023 Src inibitore Chemical Structure

Struttura chimica

Peso molecolare: 568.67

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Controllo Qualità

Lotto: Purezza: 99.93%

99.93

Target correlati	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Altro Src Inibitori	Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466 Myristic Acid

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Descrizione dellattività	PMID
EM-2	Growth inhibition assay	Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0μM	SANGER
LAMA-84	Growth inhibition assay	Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.0000038μM	SANGER
EoL-1-cell	Growth inhibition assay	Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000095μM	SANGER
MEG-01	Growth inhibition assay	Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.0000163μM	SANGER
CTV-1	Growth inhibition assay	Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.0000318μM	SANGER
BL-70	Growth inhibition assay	Inhibition of human BL-70 cell growth in a cell viability assay, IC50=0.0000472μM	SANGER
K-562	Growth inhibition assay	Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.0001617μM	SANGER
BV-173	Growth inhibition assay	Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.0005143μM	SANGER
DOHH-2	Growth inhibition assay	Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=0.0005969μM	SANGER
A704	Growth inhibition assay	Inhibition of human A704 cell growth in a cell viability assay, IC50=0.001268μM	SANGER
NCI-SNU-16	Growth inhibition assay	Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50=0.01572μM	SANGER
LC-2-ad	Growth inhibition assay	Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=0.02033μM	SANGER
LB2518-MEL	Growth inhibition assay	Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.04667μM	SANGER
D-336MG	Growth inhibition assay	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.04681μM	SANGER
LB996-RCC	Growth inhibition assay	Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=0.05668μM	SANGER
Becker	Growth inhibition assay	Inhibition of human Becker cell growth in a cell viability assay, IC50=0.06381μM	SANGER
LB1047-RCC	Growth inhibition assay	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=0.07592μM	SANGER
KS-1	Growth inhibition assay	Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.07758μM	SANGER
MPP-89	Growth inhibition assay	Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=0.08229μM	SANGER
RXF393	Growth inhibition assay	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.10633μM	SANGER
LB831-BLC	Growth inhibition assay	Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=0.12715μM	SANGER
HUTU-80	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.17529μM	SANGER
A498	Growth inhibition assay	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.18945μM	SANGER
MZ1-PC	Growth inhibition assay	Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.22716μM	SANGER
TE-8	Growth inhibition assay	Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.23924μM	SANGER
MFH-ino	Growth inhibition assay	Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.23925μM	SANGER
TE-15	Growth inhibition assay	Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.24276μM	SANGER
NTERA-S-cl-D1	Growth inhibition assay	Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=0.28855μM	SANGER
COLO-829	Growth inhibition assay	Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.31212μM	SANGER
SW684	Growth inhibition assay	Inhibition of human SW684 cell growth in a cell viability assay, IC50=0.32588μM	SANGER
OS-RC-2	Growth inhibition assay	Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.35011μM	SANGER
IST-MES1	Growth inhibition assay	Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=0.35723μM	SANGER
SNB75	Growth inhibition assay	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=0.35774μM	SANGER
SW954	Growth inhibition assay	Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.37163μM	SANGER
RCC10RGB	Growth inhibition assay	Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=0.42631μM	SANGER
VA-ES-BJ	Growth inhibition assay	Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=0.46261μM	SANGER
NCI-H1648	Growth inhibition assay	Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.51582μM	SANGER
PF-382	Growth inhibition assay	Inhibition of human PF-382 cell growth in a cell viability assay, IC50=0.70763μM	SANGER
Daudi	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=0.71411μM	SANGER
SW982	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.85819μM	SANGER
SW872	Growth inhibition assay	Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.86458μM	SANGER
TE-12	Growth inhibition assay	Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.88831μM	SANGER
HOP-62	Growth inhibition assay	Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.91599μM	SANGER
NOS-1	Growth inhibition assay	Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.95045μM	SANGER
BL-41	Growth inhibition assay	Inhibition of human BL-41 cell growth in a cell viability assay, IC50=1.00013μM	SANGER
TGBC24TKB	Growth inhibition assay	Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50=1.03831μM	SANGER
KGN	Growth inhibition assay	Inhibition of human KGN cell growth in a cell viability assay, IC50=1.0521μM	SANGER
TK10	Growth inhibition assay	Inhibition of human TK10 cell growth in a cell viability assay, IC50=1.08418μM	SANGER
GB-1	Growth inhibition assay	Inhibition of human GB-1 cell growth in a cell viability assay, IC50=1.16064μM	SANGER
GCIY	Growth inhibition assay	Inhibition of human GCIY cell growth in a cell viability assay, IC50=1.2301μM	SANGER
LXF-289	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.27256μM	SANGER
RL95-2	Growth inhibition assay	Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=1.32436μM	SANGER
SW962	Growth inhibition assay	Inhibition of human SW962 cell growth in a cell viability assay, IC50=1.33742μM	SANGER
HT-144	Growth inhibition assay	Inhibition of human HT-144 cell growth in a cell viability assay, IC50=1.44517μM	SANGER
IST-SL2	Growth inhibition assay	Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=1.47421μM	SANGER
NB6	Growth inhibition assay	Inhibition of human NB6 cell growth in a cell viability assay, IC50=1.69698μM	SANGER
SF126	Growth inhibition assay	Inhibition of human SF126 cell growth in a cell viability assay, IC50=1.73178μM	SANGER
BOKU	Growth inhibition assay	Inhibition of human BOKU cell growth in a cell viability assay, IC50=1.80527μM	SANGER
BB30-HNC	Growth inhibition assay	Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.85472μM	SANGER
KLE	Growth inhibition assay	Inhibition of human KLE cell growth in a cell viability assay, IC50=1.86232μM	SANGER
MLMA	Growth inhibition assay	Inhibition of human MLMA cell growth in a cell viability assay, IC50=1.9231μM	SANGER
KINGS-1	Growth inhibition assay	Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=1.96897μM	SANGER
ES6	Growth inhibition assay	Inhibition of human ES6 cell growth in a cell viability assay, IC50=2.05401μM	SANGER
SH-4	Growth inhibition assay	Inhibition of human SH-4 cell growth in a cell viability assay, IC50=2.12055μM	SANGER
EB-3	Growth inhibition assay	Inhibition of human EB-3 cell growth in a cell viability assay, IC50=2.15824μM	SANGER
KURAMOCHI	Growth inhibition assay	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=2.24236μM	SANGER
D-263MG	Growth inhibition assay	Inhibition of human D-263MG cell growth in a cell viability assay, IC50=2.28853μM	SANGER
SF268	Growth inhibition assay	Inhibition of human SF268 cell growth in a cell viability assay, IC50=2.48682μM	SANGER
NB17	Growth inhibition assay	Inhibition of human NB17 cell growth in a cell viability assay, IC50=2.62875μM	SANGER
DMS-114	Growth inhibition assay	Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=2.79022μM	SANGER
MC116	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=2.85704μM	SANGER
MZ2-MEL	Growth inhibition assay	Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=3.08643μM	SANGER
GI-ME-N	Growth inhibition assay	Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=3.25166μM	SANGER
697	Growth inhibition assay	Inhibition of human 697 cell growth in a cell viability assay, IC50=3.39644μM	SANGER
ACN	Growth inhibition assay	Inhibition of human ACN cell growth in a cell viability assay, IC50=4.22607μM	SANGER
TE-10	Growth inhibition assay	Inhibition of human TE-10 cell growth in a cell viability assay, IC50=4.2795μM	SANGER
LS-123	Growth inhibition assay	Inhibition of human LS-123 cell growth in a cell viability assay, IC50=4.35584μM	SANGER
TE-9	Growth inhibition assay	Inhibition of human TE-9 cell growth in a cell viability assay, IC50=4.39183μM	SANGER
CAS-1	Growth inhibition assay	Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=4.4023μM	SANGER
BB65-RCC	Growth inhibition assay	Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=4.69952μM	SANGER
MRK-nu-1	Growth inhibition assay	Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=4.71792μM	SANGER
NCI-H1355	Growth inhibition assay	Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.87685μM	SANGER
KP-N-YS	Growth inhibition assay	Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50=4.92086μM	SANGER
MZ7-mel	Growth inhibition assay	Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=5.09269μM	SANGER
NCI-H747	Growth inhibition assay	Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=5.74159μM	SANGER
C2BBe1	Growth inhibition assay	Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=5.78469μM	SANGER
RPMI-6666	Growth inhibition assay	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.9621μM	SANGER
PSN1	Growth inhibition assay	Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.16376μM	SANGER
TE-1	Growth inhibition assay	Inhibition of human TE-1 cell growth in a cell viability assay, IC50=6.71768μM	SANGER
ETK-1	Growth inhibition assay	Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=7.6356μM	SANGER
ST486	Growth inhibition assay	Inhibition of human ST486 cell growth in a cell viability assay, IC50=8.27227μM	SANGER
KU812	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.38738μM	SANGER
EHEB	Growth inhibition assay	Inhibition of human EHEB cell growth in a cell viability assay, IC50=9.0509μM	SANGER
IMR-5	Growth inhibition assay	Inhibition of human IMR-5 cell growth in a cell viability assay, IC50=9.28459μM	SANGER
BB49-HNC	Growth inhibition assay	Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=9.96548μM	SANGER
NCI-H1581	Growth inhibition assay	Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=10.3373μM	SANGER
CP66-MEL	Growth inhibition assay	Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=10.6469μM	SANGER
NMC-G1	Growth inhibition assay	Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.0324μM	SANGER
SIMA	Growth inhibition assay	Inhibition of human SIMA cell growth in a cell viability assay, IC50=11.2916μM	SANGER
A101D	Growth inhibition assay	Inhibition of human A101D cell growth in a cell viability assay, IC50=11.8487μM	SANGER
IST-MEL1	Growth inhibition assay	Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=12.5986μM	SANGER
no-10	Growth inhibition assay	Inhibition of human no-10 cell growth in a cell viability assay, IC50=13.1434μM	SANGER
KALS-1	Growth inhibition assay	Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=13.16μM	SANGER
GI-1	Growth inhibition assay	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=13.2491μM	SANGER
ONS-76	Growth inhibition assay	Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.3728μM	SANGER
D-247MG	Growth inhibition assay	Inhibition of human D-247MG cell growth in a cell viability assay, IC50=13.7709μM	SANGER
NCI-H446	Growth inhibition assay	Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50=14.1409μM	SANGER
NALM-6	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=14.2358μM	SANGER
SK-N-DZ	Growth inhibition assay	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=14.442μM	SANGER
QIMR-WIL	Growth inhibition assay	Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=14.5247μM	SANGER
MHH-NB-11	Growth inhibition assay	Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=14.6569μM	SANGER
A388	Growth inhibition assay	Inhibition of human A388 cell growth in a cell viability assay, IC50=14.6758μM	SANGER
EVSA-T	Growth inhibition assay	Inhibition of human EVSA-T cell growth in a cell viability assay, IC50=15.2484μM	SANGER
JVM-2	Growth inhibition assay	Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=16.4704μM	SANGER
EW-16	Growth inhibition assay	Inhibition of human EW-16 cell growth in a cell viability assay, IC50=17.7718μM	SANGER
CP67-MEL	Growth inhibition assay	Inhibition of human CP67-MEL cell growth in a cell viability assay, IC50=18.5863μM	SANGER
NB13	Growth inhibition assay	Inhibition of human NB13 cell growth in a cell viability assay, IC50=19.0437μM	SANGER
NCCIT	Growth inhibition assay	Inhibition of human NCCIT cell growth in a cell viability assay, IC50=20.0093μM	SANGER
SNU-C2B	Growth inhibition assay	Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=20.5124μM	SANGER
SK-NEP-1	Growth inhibition assay	Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=22.2335μM	SANGER
TE-6	Growth inhibition assay	Inhibition of human TE-6 cell growth in a cell viability assay, IC50=22.3864μM	SANGER
HCE-4	Growth inhibition assay	Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=22.927μM	SANGER
TGBC1TKB	Growth inhibition assay	Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50=23.3177μM	SANGER
L-540	Growth inhibition assay	Inhibition of human L-540 cell growth in a cell viability assay, IC50=23.3231μM	SANGER
8-MG-BA	Growth inhibition assay	Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.9588μM	SANGER
OPM-2	Growth inhibition assay	Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=25.106μM	SANGER
MHH-PREB-1	Growth inhibition assay	Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=26.2134μM	SANGER
ALL-PO	Growth inhibition assay	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=26.6132μM	SANGER
LB771-HNC	Growth inhibition assay	Inhibition of human LB771-HNC cell growth in a cell viability assay, IC50=27.8393μM	SANGER
NEC8	Growth inhibition assay	Inhibition of human NEC8 cell growth in a cell viability assay, IC50=29.0389μM	SANGER
MSTO-211H	Growth inhibition assay	Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=29.059μM	SANGER
ATN-1	Growth inhibition assay	Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=29.7028μM	SANGER
LB373-MEL-D	Growth inhibition assay	Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=29.7129μM	SANGER
NB69	Growth inhibition assay	Inhibition of human NB69 cell growth in a cell viability assay, IC50=30.374μM	SANGER
LOXIMVI	Growth inhibition assay	Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.8334μM	SANGER
HC-1	Growth inhibition assay	Inhibition of human HC-1 cell growth in a cell viability assay, IC50=32.8423μM	SANGER
SK-UT-1	Growth inhibition assay	Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=32.9447μM	SANGER
KARPAS-422	Growth inhibition assay	Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=33.2528μM	SANGER
KP-N-RT-BM-1	Growth inhibition assay	Inhibition of human KP-N-RT-BM-1 cell growth in a cell viability assay, IC50=33.8198μM	SANGER
SIG-M5	Growth inhibition assay	Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=34.6805μM	SANGER
TE-11	Growth inhibition assay	Inhibition of human TE-11 cell growth in a cell viability assay, IC50=38.0936μM	SANGER
RKO	Growth inhibition assay	Inhibition of human RKO cell growth in a cell viability assay, IC50=38.4067μM	SANGER
LS-411N	Growth inhibition assay	Inhibition of human LS-411N cell growth in a cell viability assay, IC50=38.8809μM	SANGER
OCUB-M	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=40.2533μM	SANGER
OVCAR-4	Growth inhibition assay	Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=40.5786μM	SANGER
JiyoyeP-2003	Growth inhibition assay	Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=41.2672μM	SANGER
no-11	Growth inhibition assay	Inhibition of human no-11 cell growth in a cell viability assay, IC50=41.8283μM	SANGER
NCI-H1694	Growth inhibition assay	Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=43.3351μM	SANGER
IST-SL1	Growth inhibition assay	Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=46.6838μM	SANGER
T cells	Function assay	Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells, IC50=1.9μM	16884310
SJ-GBM2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
LAN-5	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
OHS-50	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	568.67	Formula	C₃₂H₃₆N₆O₄	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	837422-57-8	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	KIN001-112, KIN112, Dual LCK/SRC inhibitor			Smiles	CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C

Solubilità

In vitro
Lotto:

DMSO : 12 mg/mL (21.1 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 6 mg/mL

Water : 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.
Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	1.000mg/ml (1.76mM)	Taking the 1 mL working solution as an example, add 50 μL 20 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 600 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

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 cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	Lck (Cell-free assay) 2 nM Src (Cell-free assay) 6 nM
In vitro	WH-4-023 mostra scarsa attività su p38 e KDR.
Saggio chinasico	Saggio chinasi Lck
Saggio chinasico	Il saggio chinasi Lck HTRF prevede la fosforilazione ATP-dipendente di un peptide substrato biotinilato di gastrina in presenza o assenza di un composto inibitore. La concentrazione finale di gastrina è 1,2 μM. La concentrazione finale di ATP è 0,5 μM (Km app = 0,6 ± 0,1 μM), e la concentrazione finale di Lck (una fusione del dominio GST-chinasi (AA 225−509)) è 250 pM. Le condizioni del tampone sono le seguenti: 50 mM HEPES pH = 7,5, 50 mM NaCl, 20 mM MgCl₂, 5 mM MnCl, 2 mM DTT, 0,05% BSA. Il saggio viene spento e bloccato con 160 μL di reagente di rilevamento. I reagenti di rilevamento sono i seguenti: Tampone composto da 50 mM Tris, pH = 7,5, 100 mM NaCl, 3 mM EDTA, 0,05% BSA, 0,1% Tween20. Prima della lettura, la streptavidina alloficocianina (SA-APC) viene aggiunta ad una concentrazione finale nel saggio di 0,0004 mg/mL, insieme all'anticorpo anti-fosfotirosina europilato (Eu-anti-PY) ad una concentrazione finale di 0,025 nM. La piastra del saggio viene letta in un lettore di piastre a fluorescenza Discovery con eccitazione a 320 nm ed emissione a 615 e 655 nm. I saggi per altre chinasi vengono eseguiti in modo simile a quanto descritto sopra, variando le concentrazioni di enzima, substrato peptidico e ATP aggiunti alla reazione, a seconda dell'attività specifica della chinasi e dei Km misurati per i substrati.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/16884310/ [2] https://pubmed.ncbi.nlm.nih.gov/34848870/ [3] https://pubmed.ncbi.nlm.nih.gov/28618271/

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