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CAS No.: 1402608-02-9

BAY1125976 Catalog No. CSN18817

Synonyms: Bay1125976

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.

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靶点选择性

生物活性

实验方案

技术信息

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.
临床研究

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

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01915576	Neoplasms	Phase 1	Completed	-	United States, California ... more >> Santa Monica, California, United States, 90404 United States, Massachusetts Boston, Massachusetts, United States, 02215 United States, Missouri St. Louis, Missouri, United States, 63110 United States, Texas Houston, Texas, United States, 77030 France Villejuif Cedex, France, 94805 Germany Heidelberg, Baden-Württemberg, Germany, 69120 Switzerland St. Gallen, Sankt Gallen, Switzerland, 9007 Collapse <<

参考文献

[1] Politz O, Siegel F, et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. Int J Cancer. 2017 Jan 15;140(2):449-459.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
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

技术信息

CAS号	1402608-02-9	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C23H21N5O	运输	蓝冰
分子量	383.45	别名	Bay1125976

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