Pazopanib

Pazopanib is a multi-kinase inhibitor that inhibits the VEGF receptors VEGFR1, VEGFR2, and VEGFR3 (IC50s = 10, 30, and 47 nM, respectively, in a cell-free enzyme assay). It also inhibits PDGFRalpha, PDGFRbeta, and c-Kit (IC50s = 71, 84, and 74 nM, respectively, in a cell-free enzyme assay) as well as additional receptor tyrosine kinases. Pazopanib inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells cocultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs. It also inhibits proliferation of multiple myeloma cells cocultured with HUVECs. Pazopanib (30 and 100 mg/kg) reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer.Formal Name: 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide. CAS Number: 444731-52-6. Synonyms: GSK-VEG10003, GW786034B. Molecular Formula: C21H23N7O2S. Formula Weight: 437.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16.6 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.17 mg/ml, DMSO: 16.6 mg/ml. lambdamax: 214, 271, 308 nm. SMILES: CN(C1=CC2=NN(C)C(C)=C2C=C1)C3=CC=NC(NC4=CC=C(C)C(S(N)(=O)=O)=C4)=N3. InChi Code: InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25). InChi Key: CUIHSIWYWATEQL-UHFFFAOYSA-N.