Description
An inhibitor of CK1δ and CK1ε (IC50s = 44 and 260 nM, respectively); selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by >90% at 10 µM; inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 (IC50s = 576, 368, 428, 427, and 3,000 nM, respectively); inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM); reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models at 20 mg/kg per day; reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue
Formal name: N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine
Synonyms:
Molecular weight: 480.5
CAS: 1454585-06-8
Purity: ≥98%
Formulation: A solid
Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Kinase Inhibitors|CK1||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|Casein Kinase Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling