马赛替尼

溶解度:DMSO

生物活性

Masitinib (AB1010) selectively inhibits wild-type and juxtamembranous mutated (JM) c-KIT(the mast cell growth factor receptor),PDGFR and FGFR3. Masitinib inhibits wild-type human and murine KIT in vitro with an IC50 of approximately 200 nM, and administered PO masitinib blocks the growth of tumors expressing juxtamembrane-mutated KIT in mice.

参考文献

1. Masitinib is safe and effective for the treatment of canine mast cell tumors. Hahn KA, J Vet Intern Med. 2008 22(6):1301-9. 2. Protein kinases as targets for cancer treatment. Giamas G, Pharmacogenomics. 2007 8(8):1005-16 3. Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors. K.A. Hahn, G. Oglivie, T. Rusk, P. Devauchelle, A. Leblanc, A. Legendre, B. Powers, P.S. Leventhal, J.-P. Kinet, F. Palmerini, P. Dubreuil, A. Moussy, and O. Hermine. J Vet Intern Med 2008;22:1301�C1309 4. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting c-kit. Dubreuil P, Letard S, Ciufolini M, et al.Cancer Res. Submitted.