Pazopanib (GW-786034)Catalog No. A11518

Quick Overview

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
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Pazopanib (GW-786034)

Pazopanib (GW-786034)  Citations(3)
  • Koide H,et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 29034773
  • Ellawatty WEA,et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 29089306
  • Fujita KI,et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 28479358
  • Product Information
    Catalog Num A11518
    M. Wt 437.5
    Formula C21H23N7O2S
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 444731-52-6
    Synonyms GW 786034, Votrient,GW786034
    Chemical Name 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzolsulfonamide
    SMILES Code CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N

    Biological activity
    Introduction
    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
    Targets
    Target Value
    VEGFR1IC50: 10nM
    VEGFR2IC50: 30nM
    VEGFR3IC50: 47nM
    FGFRIC50: 74nM
    PDGFRIC50: 84nM
    c-KitIC50: 140nM
    c-FmsIC50: 146nM
    Solubility
    Solubility (25C)* In vitro DMSO 88 mg/mL (201.13 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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