LY3177833 产品说明书 Chemicals
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产品编号 DC9766
名称 LY3177833

化学性质

CAS 1627696-51-8
分子式 C16H12FN5O
分子量 309.3
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


LY3177833 is a novel CDC7 inhibitor,CDC7/DBF4 IC50 = 3.3 nM, pMCM2 (S53) IC50 = 290 nM and IVTI TEC70 = 1.6 mcM. LY-3177833 showed MED = 5 mg/kg (p.o.) in vivo. LY-3177833 strongly impacted chromosome dynamics. In mouse xenograft models, broad antitumor activity was associated with robust dose/exposure-dependent in vivo target inhibition. In addition, the preclinical profile of LY-3177833 was different from nonselective CDC7 inhibitors and cytotoxic agents, something that supports its clinical development with a continuos dosing regime
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