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Pazopanib (GW-786034)

Multi-target kinase inhibitor, inhibits VEGFR, PDGFR, and FGFR

Pazopanib (GW-786034)

Catalog No. A3022
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
10mg $110.00 In stock
25mg $180.00 In stock
100mg $280.00 In stock
500mg $480.00 In stock

All inclusive: Shipping and all other fees included

Tel: +1-832-696-8203

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Pazopanib (GW-786034)

Related Biological Data

Pazopanib
Effect of oral administration of pazopanib hydrochloride vs vehicle on the development of choroidal neovascularization (CNV). Bars represent mean (SEM) area of CNV and show marked suppression of CNV in eyes of mice treated with pazopanib. *P<.001 by analysis of variance.

Biological Activity

Targets VEGFR1 VEGFR2 VEGFR3 PDGFR FGFR  
IC50 10 nM 30 nM 47 nM 84 nM 74 nM  

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Chemical Properties

Cas No. 635702-64-6 SDF Download SDF
Synonyms Pazopanib, Votrient, GW786034B, GW 786034, GW-786034
Chemical Name 5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide;hydrochloride
Canonical SMILES CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl
Formula C21H23N7O2S M.Wt 437.52
Solubility Soluble in DMSO Storage Desiccate at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Research Update

3. Combination metronomic oral topotecan and pazopanib: a pharmacokinetic study in patients with gynecological cancer. Anticancer Res. 2013 Sep;33(9):3823-9.
Abstract
Pazopanib is a substrate for ATP-binding cassette family transporter that exhibits anti-gynecological cancer activity in combination with metronomic topotecan.
4. Pazopanib versus sunitinib in metastatic renal-cell carcinoma. N Engl J Med. 2013 Aug 22;369(8):722-31. doi: 10.1056/NEJMoa1303989.
Abstract
Due to a progression-free survival observed in previous studies, pazopanib and sunitinib have been assessed for efficacy and safety in a randomized trial.

Background

Pazopanib is a potent and selective second generation multi-targeted receptor tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and c-kit tyrosine kinases. It is involved in inhibiting signaling pathways, angiogenesis, and cell proliferation. Pazopanib exhibited excellent anti-angiogenic and anti-tumor activity and synergism was observed in combination with chemotherapeutic drugs in several mouse models of a variety of tumors, accompanied by desirable pharmacokinetics and oral bioavailability. It inhibits the intracellular tyrosine kinase portion of all the VEGFR subtypes, and exhibits distinct pharmacokinetic and toxicity profiles compared with other agents among VEGF signaling pathway inhibitors. Recent studies elucidated its importance of signaling cascades related to angiogenesis in the management of RCC.

Reference

Sonpavde G, Hutson T E. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Current oncology reports. 2007; 9(2): 115 - 119.

Podar K, Tonon G, Sattler M, et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proceedings of the National Academy of Sciences. 2006; 103(51): 19478 - 19483.