产品信息
抗原名称
Chk2
商品描述
BML-277 (C 3742) is a selective Chk2 (checkpoint kinase 2) inhibitor with an IC50 of 15 nM.
分子量
363.8
纯度
>98%
可溶性
DMSO : ≥ 55 mg/mL
外观
Powder
In vitro(体外研究)
The CHK2 Inhibitor II shows 1,000-fold greater selectivity for the CHK2 serine/threonine kinase than for the Cdk1/B and CK1 kinases and was first discovered to be a potent, selective small molecule showing radioprotection towards human T cells. Different doses of CHK2 inhibitor II specifically inhibit CHK2 phosphorylation at Thr68 at different time course, but not CHK1 phosphorylation. Treatment with combination of CHK2 inhibitor II and ERK inhibitor results in substantially more apoptosis compared with treatment of either drug alone.
In vivo(体内研究)
SUDHL6 DLBCL xenografts mice treated every other day intraperitoneally with either vehicle, ERK inhibitor (5 mg kg−1), CHK2 inhibitor II (1 mg kg−1), or both ERK inhibitor and CHK2 inhibitor II for 20 days show no lethal toxicity, significant weight loss or any gross abnormalities. Both 5 mg/kg ERK inhibitor and 1 mg/kg CHK2 inhibitor II modestly inhibit tumour growth but combined treatment with ERK inhibitor and CHK2 inhibitor II results in a statistically significant suppression of tumour growth.
背景
别名
Chk2 Inhibitor II; C 3742; BML277; BML 277
分子式
C20H14ClN3O2
CAS号
516480-79-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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