A multi-kinase inhibitor; inhibits FLK1 (Ki = 9 nM)

Sunitinib (malate) – 5 mg

Brand:
Cayman
CAS:
341031-54-7
Storage:
-20
UN-No:
Non-Hazardous - /

Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3.{17043,17045} 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.{17045} 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).{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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Description

A multi-kinase inhibitor; inhibits FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3; 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; inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFRβ phosphorylation (IC50s = 10 and 10 nM, respectively); inhibits phosphorylation of FLT3 and FLT3-ITD (IC50s = 250 and 50 nM, respectively); decreases VEGF- and FGF-induced proliferation of HUVECs; IC50s = 30 and 700 nM, respectively); reduces tumor growth in a variety of mouse xenograft models at 20-80 mg/kg per day

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

Synonyms:  SU11248

Molecular weight: 532.6

CAS: 341031-54-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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