competitive dual site (ATP- and peptide-binding) Src kinase inhibitor
CAS：179248-59-0
分子式：C22H19N3O3
分子量：373.4
纯度：98%
存储：Store at -20°C

Background:

Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].

参考文献:
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.