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
SIM010603 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to firstname.lastname@example.org to inquire quote.
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
The following data is based on the product molecular weight 396.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.
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)