KB SRC 4

Modify Date: 2024-01-14 22:38:48

KB SRC 4 Structure
KB SRC 4 structure
Common Name KB SRC 4
CAS Number 1380088-03-8 Molecular Weight 555.03200
Density N/A Boiling Point N/A
Molecular Formula C32H23ClN8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of KB SRC 4


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.

 Names

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
Synonym More Synonyms

 KB SRC 4 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C32H23ClN8
Molecular Weight 555.03200
Exact Mass 554.17300
PSA 100.33000
LogP 7.27310

 Synonyms

KB SRC 4