sunitinib-malate

Description: Sunitinib Malate (formerly also known as SU11248 Malate; trade nameSutent)) is a potent, orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor with potent anticancer activities. It inhibits VEGFR2 (Flk-1) and PDGFRbeta with IC50s of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. It was approved by the FDA for the treatment of renal cell carcinoma and imatinib-resistant gastrointestinal stromal tumor on January 26, 2006. Sunitinib Malate is the malate salt of an indolinone-based tyrosine kinase inhibitor with potential antineoplastic activity. Sunitinib blocks the tyrosine kinase activities of VEGFR2, PDGFRb, and c-kit, thereby inhibiting angiogenesis and cell proliferation.

References: J Med Chem. 2003; 46(7):1116-9; Clin Cancer Res. 2003; 9(1):327-37; Blood. 2003; 101(9):3597-605.

Related CAS: 1332306-95-2 (oxalate); 1126641-10-8 (maleate); 1327155-72-5 (HCl); 557795-19-4 (free); 341031-54-7 (malate); 342641-94-5; 1221149-36-5 (acetate); 1275588-72-1 (mesylate)

Chemical Name: (Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2, 4-dimethyl-1H-pyrrole-3-carboxamide malate

InChi Key: LBWFXVZLPYTWQI-HBPAQXCTSA-N

InChi Code: InChI=1S/C22H27FN4O2.C4H6O5/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28; 5-2(4(8)9)1-3(6)7/h7-8, 11-12, 25H, 5-6, 9-10H2, 1-4H3, (H, 24, 29)(H, 26, 28); 2, 5H, 1H2, (H, 6, 7)(H, 8, 9)/b17-12-;

SMILES Code: O=C(C1=C(C)NC(/C=C2C(NC3=C\2C=C(F)C=C3)=O)=C1C)NCCN(CC)CC.OC(CC(O)=O)C(O)=O