GDC-0575

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抑制剂描述：

产品名称：GDC-0575

产品别名：见爱必信官网

英文别名：GDC-0575

靶点：Chk

CAS：1196541-47-5

纯度：＞98%

外观：见爱必信官网

保存方法：Store at -20°C

描述：

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM.

溶解性：DMSO ：75 mg/mL (198.27 mM)
Ethanol :5 mg/mL (13.22 mM)

体外研究：

GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine. CHK1 inhibitor GDC-0575 in combination with AraC enhances the killing of primary acute myeloid leukemia cells ex vivo by inducing apoptosis.

体内研究：GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher drug dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered.

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