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1. Gastrointestinal stromal tumors (GIST) that fail to be treated with imatinib mesylate or are not tolerated.
2. Inoperable advanced renal cell carcinoma (RCC).
3. Treatment of advanced endocrine tumors such as pancreas.
Uses of Sunitinib Malate.
In vitro study of Sunitinib Malate.
Sunitinib is also a potent c-Kit inhibitor with an IC50 of 211nM. Sunitinib is a potent ATP-competitive VEGFR2(Flk1) and PDGFRβ inhibitor with Ki of 9nM and 8nM, respectively, and its action on VEGFR2 and PDGFR is more than 10 times more selective than that on FGFR-1,EGFR,Cdk2,Met,IGFR-1,Abl, and src. Sunitinib acts on serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, inhibiting VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10nM and 10nM, respectively. Sunitinib inhibited the proliferation of VEGF-induced serum starved HUVECs with an IC50 of 40nM, and NIH-3T3 cells induced by PDGF overexpressing PDGFRβ or PDGFRα with IC50 of 39nM and 69nM, respectively. Sunitinib inhibits wild-type FLT3,FLT3-ITD, and FLT3-ASP835 phosphorylation with IC50 of 250nM,50nM, and 30nM, respectively. Sunitinib inhibited MV4; 11 and OC1-AML5 cells proliferated with IC50 of 8nM and 4nM, respectively, and induced apoptosis in a dose-dependent manner
Product Method of Bulk Sunitinib Malate Powder.
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