ERK5-IN-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ERK5-IN-2 是一种口服活性、亚微摩尔、选择性 ERK5 抑制剂，对于 ERK5 和 ERK5 MEF2D 的 IC50 值分别为 0.82 μM、3 μM。

ERK5-IN-2 is an orally active sub-micromolar selective ERK5 inhibitor with IC50s of 0.82 μM 3 μM for ERK5 and ERK5 MEF2D respectively.

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Animal Model:Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts Dosage:100?mg/kg Administration:P.o.; twice-daily; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days Result:Tumor volumes were significantly reduced. Animal Model:Female CD1 mice at 8-10 weeks of age Dosage:10 mg/kg Administration:I.v. or p.o.; 0.083-24?hours Result:The terminal plasma half-life was 38?min, with a plasma clearance of 27?mL/min/kg, and oral bioavailability of 68%.

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MAPK/ERK Signaling

ERK

ERK5

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1888305-96-1

388.19

C17H11BrFN3O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (644.01 mM)

Fc1cccc(Br)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1

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(-20℃)

With Ice Pack

≥ 2 years