Tafetinib

Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem 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), andFms-like tyrosine kinase-3 (FLT3) withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis[1].

Product Specifications

CAS Number

[1032265-57-8]

Product Name Alternative

SIM010603

UNSPSC

12352005

Target

C-Kit; RET; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tafetinib.html

Purity

96.20

Solubility

DMSO : < 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCN(CC)CCNC(C1=C(C)NC2=C1CCC/C2=C3C(NC4=CC=C(F)C=C/34)=O)=O

Molecular Formula

C24H29FN4O2

Molecular Weight

424.51

References & Citations

[1]Wang D, et al. Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor. Cancer Chemother Pharmacol. 2012;69 (1) :173-183.