CAS:1402608-02-9BAY1125976

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BAY1125976 Cat No. FB09904Cas No. 1402608-02-9

BAY1125976 is a selective allosteric AKT1/2 inhibitor and inhibits AKT1 and AKT 2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6079 mL
- 13.0397 mL
- 26.0793 mL
- 5 mM
- 0.5216 mL
- 2.6079 mL
- 5.2159 mL
- 10 mM
- 0.2608 mL
- 1.3040 mL
- 2.6079 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号	1402608-02-9	储存条件	粉末 -20°C 3 年液体 -80°C 12 月
分子式	C23H21N5O	运输	蓝冰
分子量	383.45	别名

靶点数据

生物活性

描述BAY 1125976 is a potent and selective allosteric AKT1/2 inhibitor with IC50 values of 5.2nM and 18nM for full-length AKT1 and AKT2, respectively, and exhibits much less potency against AKT3. BAY 1125976 effectively inhibited the basal levels of AKT phosphorylation at both sites, T308 and S473 with IC50 values of 0.9 and 1.1 nM, respectively, accompanied with blocking phosphorylation of a downstream signaling molecule 4EBP1 by phosphorylation at mTOR substrate T70 with an IC50 of 35 nM, in KPL-4 cells. BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines with IC50 values ranging in 0.02-10μM, particularly with high activity against breast and prostate cancer cell lines expressing estrogen or androgen receptors. Administration of BAY 1125976, p.o., exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model carrying PIK3CA^H1074R mutant, the MCF7 and HBCx-2 breast cancer models and the AKTE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models at doses ranging in 10-50mg/kg.
作用机制BAY 1125976 binds into an allosteric binding pocket formed by kinase and PH domain.^[1]
动物研究
剂量
Mice: 5 mg/kg - 50 mg/kg^[1] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 5 mg/kg - 50 mg/kg^[1] (p.o.)
给药途径	p.o.