BAY-1125976 is a potent and selective allosteric AKT1/2 inhibitor. BAY-1125976 exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY 1125976 potently and selectively inhibited the activity of full-length AKT1 and AKT2 by binding into an allosteric binding pocket formed by kinase and PH domain. In vitro, BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. BAY 1125976 exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (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.
MedKoo Cat#: 407996
Name: BAY-1125976
CAS#: 1402608-02-9 (free base)
Chemical Formula: C23H21N5O
Exact Mass: 383.1746
Molecular Weight: 383.45
Elemental Analysis: C, 72.04; H, 5.52; N, 18.26; O, 4.17
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.0 | 33.90 | |
| DMF | 5.0 | 13.04 | |
| DMF:PBS (pH 7.2) (1:3) | 0.3 | 0.65 |
The following data is based on the product molecular weight 383.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
