Sunitinib-d<sub>10</sub>

Sunitinib-d10

CAT N°: 22614
Price:

1,055.00 896.75

Sunitinib-d10 is intended for use as an internal standard for the quantification of sunitinib (Item No. 13159) by GC- or LC-MS. Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFR? (Ki = 8 nM), and FLT3.{17043,17045} It is at least 10-fold selective for FLK1 and PDGFR? over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl, and Src.{17045} Sunitinib inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFR? 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).{17043,17045} 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.{17045} Formulations containing sunitinib have been used in the treatment of gastrointestinal stromal tumors and metastatic renal cell carcinoma.

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