Formulation: A solid
Formal Name: N4-1H-indazol-6-yl-N2-[3-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-5-methyl-2,4-pyrimidinediamine
Purity: ≥98%
Formula Markup: C24H28N8O
Formula Weight: 444,5
Shelf life (days): 1095
CAS Number: 2644673-04-9
Notes: CYY292 is an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, (IC50s = 5.35, 4.6, 28, 28, and 78 nM, respectively).{51530,51529} It is selective for these kinases over FGFR4 (IC50 = >1,000 nM) but also inhibits c-Kit, VEGFR2, VEGFR1, and insulin-like growth factor 1 receptor (IGF-1R; IC50s = 67, 33, 36, and 75 nM, respectively), as well as EGFR, Bruton’s tyrosine kinase (BTK), cyclin-dependent kinase 4 (Cdk4)/cyclin D3, and MET (IC50s = 128, 198, 214, and 396 nM, respectively).{51529} CYY292 inhibits the proliferation of MG-63, U2OS, MNNG/HOS, and Saos-2 osteosarcoma cells (IC50s = 0.84, 0.76, 1.36, and 0.72 µM, respectively).{51530} It inhibits the migration and invasion of U87MG and LN-229 glioblastoma cells when used at concentrations of 0.3 and 0.5 µM.{51529} CYY292 (30 mg/kg) decreases tumor volume and increases survival in a U87MG orthotopic mouse xenograft model.
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