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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-Akt-BAY-1125976
BAY-1125976

Chemical Structure : BAY-1125976

CAS No.: 1402608-02-9

BAY-1125976 (BAY1125976)

货号: PC-42032Not For Human Use, Lab Use Only.

BAY-1125976 is a potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP.

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25 mg ¥3280 In stock
50 mg ¥5480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY-1125976 is a potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP.
BAY-1125976 binds to active AKT1 with Kd of 2.7 nM and inactive AKT1 with Kd of 1.3 nM.
BAY-1125976 displays >86-fold less potent against AKT3; inhibits the phosphorylation of AKT1 at T308 and S473 (IC50=0.9 and 1.1 nM, respectively), PRAS40 at T246 and 4EBP1 at T70.
BAY-1125976 targets tumors displaying PI3K/AKT/mTOR pathway activation, inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors.
BAY-1125976 exhibits strong in vivo patient-derived xenograft models.

物理化学性质&存储条件

分子量 383.4457
分子式 C23H21N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 10.33 mg/mL

Chemical Name/SMILES

Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-

参考文献

1. Politz O, et al. Int J Cancer. 2017 Jan 15;140(2):449-459.

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