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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

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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.

Related Biological Data

Pazopanib

Related Biological Data

Pazopanib

Biological Activity

Description Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Targets VEGFR1 VEGFR2 VEGFR3 PDGFR FGFR  
IC50 10 nM 30 nM 47 nM 84 nM 74 nM  

Protocol

Cell experiment: [1]

Cell lines

Primary human brain microvascular endothelial cells (HBMEC)

Preparation method

Pazopanib was reconstituted in DMSO and stored at −80°C.

Reacting condition

IC50: 2 μM, 48 hours

Applications

The IC50 for pazopanib for anchorage-dependent growth was 2 μM and 1 μM after 48 h and 72 h, respectively. Pazopanib abrogated the phosphorylation of VEGFR2 with disruption of downstream PLCγ1. It also disrupted the Ras-Raf-ERK pathway through decreased phosphorylated MEK1/2 and ERK1/2 and affected the phosphorylation of 70S6K. Our findings confirmed that pazopanib targeted endothelial cells, affecting cell growth, VEGFR-induced signaling, and tube formation.

Animal experiment: [2]

Animal models

Immune-deficient beige-nude-xid (BNX) mice injected with MM.1S cells

Dosage form

Oral administration, 30 mg/kg and 100 mg/kg, daily for five weeks

Application

Tumor growth in treated mice was significantly delayed (30 mg/kg) or almost totally inhibited (100 mg/kg) compared with the control group. However, tumors rapidly regrew after cessation of treatment at day 30. Using Kaplan–Meier and log-rank analysis, the mean overall survival (OS) was 20 days in the control cohort versus 41 days and 51 days in groups treated with 30 mg/kg and 100 mg/kg pazopanib, respectively. Statistically significant prolongation in mean OS compared with control mice was observed in animals treated with 30 mg/kg and 100 mg/kg. Importantly, treatment with either the vehicle alone or pazopanib did not affect body weight.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Gril B, Palmieri D, Qian Y, et al. Pazopanib reveals a role for tumor cell B-Raf in the prevention of HER2+ breast cancer brain metastasis. Clinical Cancer Research, 2011, 17(1): 142-153.

[2] 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.

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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.