An allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM

BAY-1125976 – 5 mg

Brand:
Cayman
CAS:
1402608-02-9
Storage:
-20
UN-No:
Non-Hazardous - /

BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay).{46495} 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.  

 

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SKU: 28913 - 5 mg Category:

Description

An allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay); selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of FLT1, -3, -4, and Mer by >50% in a panel of 227 kinases at 1 µM; inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 µM) and reduces tumor growth in KPL-4, MCF-7, and PDX mouse xenograft models at 50 mg/kg per day

Formal name: 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-imidazo[1,2-b]pyridazine-6-carboxamide

Synonyms: 

Molecular weight: 383.5

CAS: 1402608-02-9

Purity: ≥98%

Formulation: A crystalline solid

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