BAY1125976

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Chemical Structure| 1402608-02-9 同义名 : -
CAS号 : 1402608-02-9
货号 : A653519
分子式 : C23H21N5O
纯度 : 99%
分子量 : 383.446
MDL号 : N/A
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(65.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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 PIK3CAH1074R 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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL
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.