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Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRbeta (Ki = 8 nM), and FLT3. It is at least 10-fold selective for FLK1 and PDGFRbeta over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl, and Src. Sunitinib inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFRbeta phosphorylation (IC50s = 10 and 10 nM, respectively) as well as phosphorylation of FLT3 and FLT3 carrying the activating internal tandem duplication mutation (FLT3-ITD, IC50s = 250 and 50 nM, respectively). It decreases VEGF- and FGF-induced proliferation of human umbilical vein endothelial cells (HUVECs, IC50s = 30 and 700 nM, respectively) and reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 20 to 80 mg/kg per day. Formulations containing sunitinib have been used in the treatment of gastrointestinal stromal tumors and metastatic renal cell carcinoma.Formal Name: N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, (2S)-hydroxy-butanedioic acid. CAS Number: 341031-54-7. Synonyms: SU11248. Molecular Formula: C22H27FN4O2 . C4H6O5. Formula Weight: 532.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 267, 427 nm. SMILES: CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2\C(=O)Nc3ccc(F)cc/23)c1COC(=O)C[C@H](O)C(=O)O. 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-,. InChi Key: LBWFXVZLPYTWQI-HBPAQXCTSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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