| product Name | Sunitinib malate |
|---|---|
| Synonyms | SUNITINIB MALEATE; 1H-Pyrrole-3-carboxamide, N-(2-(diethylamino)ethyl)-5-((Z)- (5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4- dimethyl-, (2S)-hydroxybutanedioate (1:1); Butanedioic acid, hydroxy-, (2S)-, compd. with 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 (1:1); 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)-hydroxybutanedioate; (2S)-2-hydroxybutanedioic acid – N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (1:1); 2-hydroxypentanedioic acid – N-[2-(diethylamino)ethyl]-2,4-dimethyl-5-[(Z)-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-1H-pyrrole-3-carboxamide (1:1); Sunitinib Mablate |
| Molecular Formula | C28H38N4O7 |
| Molecular Weight | 542.62392 |
| InChI | InChI=1/C23H30N4O2.C5H8O5/c1-6-27(7-2)11-10-24-23(29)21-15(4)20(25-16(21)5)13-18-17-12-14(3)8-9-19(17)26-22(18)28;6-3(5(9)10)1-2-4(7)8/h8-9,12-13,25H,6-7,10-11H2,1-5H3,(H,24,29)(H,26,28);3,6H,1-2H2,(H,7,8)(H,9,10)/b18-13-;/t;3-/m.0/s1 |
| CAS Registry Number | 341031-54-7 |
| Molecular Structure | 
|
| Description | Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ 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 PDGFRβ 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. |
| Chemical Properties | Yellow Solid |
| Uses | 1.Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
2.Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit 3.A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic. |
Reviews
There are no reviews yet.