产品
编 号：F236164
分子式：C17H11BrFN3O2
分子量：388.19
分子式：C17H11BrFN3O2
分子量：388.19
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1888305-96-1
产品详情
生物活性：
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. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
体内研究：
ERK5-IN-2 (化合物 46) (口服；100 mg/kg；CD1 小鼠 7 天和 CD1 裸 (nu/nu) 小鼠 10 天) 具有抗血管生成作用和低浓度的血红蛋白。 ERK5-IN-2 (iv 或 口服10 mg/kg，持续 0.083-24 小时) 在 caco-2 细胞渗透性测定中表现出低内在清除率和高通量和低外排比 (ER) 人类和小鼠。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%.
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. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
体内研究：
ERK5-IN-2 (化合物 46) (口服；100 mg/kg；CD1 小鼠 7 天和 CD1 裸 (nu/nu) 小鼠 10 天) 具有抗血管生成作用和低浓度的血红蛋白。 ERK5-IN-2 (iv 或 口服10 mg/kg，持续 0.083-24 小时) 在 caco-2 细胞渗透性测定中表现出低内在清除率和高通量和低外排比 (ER) 人类和小鼠。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%.
产品资料
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