产品信息
抗原名称
Checkpoint Kinase (Chk)
商品描述
SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 50-fold selectivity against Chk2. Phase 2.
分子量
376.25
纯度
>98%
可溶性
DMSO : ≥ 100 mg/mL (265.78 mM)
外观
White to off white solid
In vitro(体外研究)
SCH900776 (300 nM) shows potent inhibitory activities against phosphorylation at ser296-Chk1. SCH900776 (1 μM) causes a 30-fold decrease in the IC50 for NSC-32065 in MDA-MB-231 cells. The Kd value of SCH 900776 for the CHK1 kinase domain is 2 nM. SCH 900776 exhibits an approximate EC50 of 60 nM in cells exposure to NSC-32065. SCH 900776 induces dose-dependent suppression of CHK1 pS296 and concomitant accumulation of phospho-RPA signal in U2OS cells.
In vivo(体内研究)
SCH 900776 induces the γ-H2AX biomarker at 4 mg/kg (i.p.), and enhances tumor pharmacodynamic and regression responses in A2780 xenograft model. SCH 900776 (16 and 32 mg/kg, i.p.) induces incremental improvements in tumor response. Escalation of SCH 900776 dose to 20 and 50 mg/kg in combination with gemcitabine results in improvements in TTP 10× in the A2780 xenograft systems.
背景
分子式
C15H18BrN7
CAS号
891494-63-6
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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