Formulation: A solid
Formal Name: N-[(3S)-1-[(dimethylamino)carbonyl]-3-pyrrolidinyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Purity: ≥98%
Formula Markup: C23H26FN5O3
Formula Weight: 439,5
Shelf life (days): 1460
CAS Number: 1013920-15-4
Notes: X-82 is a multi-kinase inhibitor.{67653} It inhibits VEGFR2, PDGFRβ, FMS-related tyrosine kinase 3 (FLT3), and c-Kit (IC50s = 1.12, 0.13, 0.63, and 0.14 nM, respectively) and is selective for these kinases over RET and AMP-activated kinase α1 (AMPKα1; IC50s = 74.1 and 352.2 nM, respectively). X-82 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 31 nM).{67654} It decreases VEGF-induced capillary tube formation in HUVECs when used at a concentration of 1 µM and reduces FBS-induced migration of HUVECs at 0.01 or 0.1 µM. In vivo, X-82 (80 mg/kg per day), alone and in combination with the EGFR inhibitor gefitinib (Item No. 13166), reduces tumor volume and growth in an HCC827 non-small cell lung cancer (NSCLC) mouse xenograft model.
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