|(R)-N-(4-(3-氨基哌啶-1-基)-5-溴-1H-吡咯并[2,3-B]吡啶-3-基)环丙烷甲酰胺|CsnPharm

CAS No.: 1196541-47-5

Synonyms: ARRY-575;RG7741

GDC-0575 is a potent and selective CHK1 inhibitor.

规格	价格	促销价格	库存	数量

400-920-2911

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400-920-2911

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描述Chk1 (Checkpoint kinase 1), an important serine/threonine kinase, is responding to DNA damage and stall DNA replication. Chk1 plays a key role in maintaining the replication fork viability during exposure to DNA antimetabolites. Inhibition of Chk1 will lead to accumulation of double-strand DNA breaks and cell death in human tumor cell lines exposure to antimetabolite. GDC-0575 is a selective Chk1 inhibitor with IC50 value of 1.2 nM. GDC-0575 exhibited anti-proliferative effect on nine of ten soft-tissue sarcoma (STS) cell lines with IC50 values ranging in 0.025-5.9μM, with inhibition of the phosphorylation of Ser296 observed. GDC-0575 could synergy with gemcitabine. It abrogated DNA damage-induced S and G2–M checkpoints exacerbated DNA double-strand breaks and induced apoptosis in STS cells. Combined therapy of GDC-0575 (25mg/kg, orally) with gemcitabine twice a week for 3 weeks significantly reduced tumor growth increased progression-free survival of a P53mut UPS PDX model. GDC-0575 could enhance AraC-mediated killing of AML cells both in vitro and in vivo with abrogation of any potential chemoresistance mechanisms involving DNA repair.
作用机制GDC-0575 is an ATP-competitive CHK1 inhibitor.

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技术信息

CAS号	1196541-47-5	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C16H20BrN5O	运输	蓝冰
分子量	378.27	别名	ARRY-575;RG7741

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