WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 401915
Description: SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.
MedKoo Cat#: 401915
Chemical Formula: C22H25FN4O2
Exact Mass: 396.19615
Molecular Weight: 396.46
Elemental Analysis: C, 66.65; H, 6.36; F, 4.79; N, 14.13; O, 8.07
Synonym: SIM010603; SIM 010603; SIM-010603
IUPAC/Chemical Name: (Z)-N-(2-(dimethylamino)ethyl)-7-(5-fluoro-2-oxoindolin-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
InChi Key: CARLZFLTQJQGIP-CYVLTUHYSA-N
InChi Code: InChI=1S/C22H25FN4O2/c1-12-18(21(28)24-9-10-27(2)3)14-5-4-6-15(20(14)25-12)19-16-11-13(23)7-8-17(16)26-22(19)29/h7-8,11,25H,4-6,9-10H2,1-3H3,(H,24,28)(H,26,29)/b19-15-
SMILES Code: O=C(C1=C(C)NC2=C1CCC/C2=C3C(NC4=C/3C=C(F)C=C4)=O)NCCN(C)C
Although SIM010603 exhibited lower activity in regard to proliferation of NCI-H460, MDA-MB-435, and T241-VEGF-A cells (IC(50) > 1 μmol/l), SIM010603 inhibited tumor growth in these xenograft tumor growth models. SIM010603 reduced tumor MVD in T241-VEGF-A tumor xenograft models and decreased positive signals of CD31, NG2 in MDA-MB-435, and LLC-SW-44 xenograft tumor models. (source: Cancer Chemother Pharmacol. 2012 Jan;69(1):173-83) (last updated: 6/23/2015)
1: Wang D, Tang F, Wang S, Jiang Z, Zhang L. Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor. Cancer Chemother Pharmacol. 2012 Jan;69(1):173-83. doi: 10.1007/s00280-011-1681-1. Epub 2011 Jun 3. PubMed PMID: 21638122.