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Chemical Structure : BAY-1125976
CAS No.: 1402608-02-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $548 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 383.4457 | |
| Formula | C23H21N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 10.33 mg/mL |
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| Chemical Name/SMILES |
Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl- |
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1. Politz O, et al. Int J Cancer. 2017 Jan 15;140(2):449-459.
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