| Hazard Information | Back Directory | [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. | [Uses]
Tafetinib (SIM010603) analogue 1 is an analog of the tyrosine kinase receptor inhibitor Tafetinib (SIM010603).[1]. | [References]
[1] Mao Y, et al. Evaluation of subchronic toxicity of SIM010603, a potent inhibitor of receptor tyrosine kinase, after 28-day repeated oral administration in SD rats and beagle dogs. Food Chem Toxicol. 2012 May;50(5):1256-70. DOI:10.1016/j.fct.2012.02.007 |
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