A multi-kinase inhibitor
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Labeled Version(s)
25446Pazopanib-d6
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Pazopanib

Item No. 12097

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 16.6 mg/mlDMF:PBS (pH 7.2) (1:5): 0.17 mg/mlDMSO: 16.6 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Product Description

    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).1 It also inhibits PDGFRα, PDGFRβ, 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kumar, R., Knick, V.B., Rudolph, S.K., et al. Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity. Mol. Cancer Ther. 6(7), 2012-2021 (2007).

    2. Podar, K., Tonon, G., Satler, M., et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proc. Natl. Acad. Sci. USA 103(5), 19478-19483 (2006).