Sunitinib-d10

Sunitinib-d10 is intended for use as an internal standard for the quantification of sunitinib (Cay-13159) by GC- or LC-MS. 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-[di(ethyl-1,1,2,2,2-d5)amino]ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. CAS Number: 1126721-82-1. Molecular Formula: C22H17D10FN4O2. Formula Weight: 408.5. Purity: >99% deuterated forms (d1-d10). Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: CC1=C(/C=C2C(NC3=C\2C=C(F)C=C3)=O)NC(C)=C1C(NCCN(C([2H])([2H])C([2H])([2H])[2H])C([2H])([2H])C([2H])([2H])[2H])=O. InChi Code: InChI=1S/C22H27FN4O2/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/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-/i1D3,2D3,5D2,6D2. InChi Key: WINHZLLDWRZWRT-BLSNYXODSA-N.