Formulation: A solid
Formal Name: N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-1-naphthalenecarboxamide
Purity: ≥98%
Formula Markup: C27H21N3O3
Formula Weight: 435,5
Shelf life (days): 1460
CAS Number: 1256349-48-0
Notes: CS 2164 is a multi-kinase inhibitor.{68649} It inhibits VEGFR1, -2, and -3 (IC50s = 8, 7, and 9 nM, respectively), PDGFRα and PDGFRβ (IC50s = 1 and 93 nM), c-Kit (IC50 = 4 nM), Aurora B kinase (IC50 = 9 nM), and CSF-1 receptor tyrosine kinase (FMS; IC50 = 7 nM). CS 2164 is selective for these kinases over a panel of 72 additional kinases, 76 GPCRs, two phosphatases, and nine ion channels (IC50s = >100 nM for all). It inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; GI50 = 20.7 nM) and PDGF-induced proliferation of NIH3T3 cells (GI50 = 44.16 nM). In vivo, CS 2164 (20 mg/kg) reduces tumor vascularization and tumor growth in a COLO 320 colon cancer mouse xenograft model. It also reduces tumor volume in A549, HCT-8, SMMC-7721, and MGC803 mouse xenograft models when administered at doses ranging from 2.5 to 40 mg/kg.
English
Deutsch
