| Identification | Back Directory | [Name]
BAY-1125976. | [CAS]
1402608-02-9 | [Synonyms]
CS-2913
BAY1125976
BAY 1125976
BAY-1125976.
BAY-1125976; BAY 1125976
2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide
Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl- | [Molecular Formula]
C23H21N5O | [MDL Number]
MFCD30481340 | [MOL File]
1402608-02-9.mol | [Molecular Weight]
383.45 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:13.0(Max Conc. mg/mL);33.9(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);13.04(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.65(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Light yellow to yellow | [InChI]
InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29) | [InChIKey]
JBGYKRAZYDNCNV-UHFFFAOYSA-N | [SMILES]
C12=NC(C3=CC=C(C4(N)CCC4)C=C3)=C(C3=CC=CC=C3)N1N=C(C(N)=O)C=C2 |
| Hazard Information | Back Directory | [Description]
BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay). It is selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 μM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 μM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day. | [Uses]
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively. | [in vivo]
BAY 1125976 targets tumors displaying activation of the PI3K/Akt/mTOR pathway. BAY 1125976 exhibits 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[1]. | [IC 50]
Akt1: 5.2 nM (IC50, at 10 μM ATP); Akt2: 18 nM (IC50, at 10 μM ATP); Akt3: 427 nM (IC50, at 10 μM ATP) | [References]
[1] Politz O, 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. DOI:10.1002/ijc.30457 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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