1380088-03-8

1380088-03-8 structure

Name: KB SRC 4
Chemical Name: 1-{3-[1-(3-Biphenylylmethyl)-1H-1,2,3-triazol-5-yl]phenyl}-3-(4-c hlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number: 1380088-03-8
Molecular Formula: C₃₂H₂₃ClN₈
Molecular Weight: 555.03200
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Src
Create Date: 2017-07-30 03:16:09
Modify Date: 2024-01-14 22:38:48
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.

Name	1-{3-[1-(3-Biphenylylmethyl)-1H-1,2,3-triazol-5-yl]phenyl}-3-(4-c hlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Synonyms	KB SRC 4

Description	KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src Research Areas >> Cancer
Target	Ki: 44 nM (c-Src)[1] Kd: 86 nM (c-Src)[1]
In Vitro	KB SRC 4 (Compound 4) is a potent, highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM. KB SRC 4 is selective between Src family members, with >2-fold selectivity over both Lck (Kd, 160 nM) and Fgr (Kd, 240 nM), 8-fold selectivity over c-Yes (Kd, 720 nM), and >40-fold selectivity over Lyn (Kd, 3200 nM), Hck (Kd, 4400 nM), and Fyn (Kd, >40000 nM). KB SRC 4 inhibits the growth of cancer cell lines, with GI50s of 11 μM, 12 μM, 11 μM, 6.0 μM against HT-29, SK-BR-3, MCF7, MDA-MB-453, and NIH-3T3, respectively[1].
References	[1]. Brandvold KR, et al. Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol. 2012 Aug 17;7(8):1393-8.