Pazopanib HCl (GW786034 HCl)

Pazopanib HCl (GW786034 HCl) 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 in cell-free assays, respectively.

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Pazopanib HCl (GW786034 HCl) Chemical Structure

Pazopanib HCl (GW786034 HCl) Chemical Structure
Molecular Weight: 473.98

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

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  • Research Area
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    Combination Therapy

Product Description

Biological Activity

Description Pazopanib HCl (GW786034 HCl) 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 in cell-free assays, respectively.
Targets VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
FGFR [1]
(Cell-free assay)

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IC50 10 nM 30 nM 47 nM 74 nM
In vitro Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1] Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of Pazopanib and is completely abolished at 5 µg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. [2] Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. [3]
In vivo The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group. [2]
Features A multi-kinase inhibitor.

Protocol(Only for Reference)

Kinase Assay:


Kinase enzyme assays VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs.

Cell Assay:


Cell lines HUVEC cells
Concentrations 0-10 μM
Incubation Time 1 hour

Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level.

Animal Study:


Animal Models Immunodeficient mice bearing SYO-1 cells
Dosages 0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
Administration Oral administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Harris PA, et al. J Med Chem. 2008, 51(15), 4632-4640.

[2] Hosaka S, et al. J Orthop Res. 2012.

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Clinical Trial Information( data from, updated on 2015-11-14)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02307474 Not yet recruiting Clear Cell Renal Cell Carcinoma|Renal Cell Carcinoma Case Comprehensive Cancer Center|National Cancer Institut  ...more Case Comprehensive Cancer Center|National Cancer Institute (NCI) February 2016 --
NCT02348398 Not yet recruiting Cervical Cancer M.D. Anderson Cancer Center|GlaxoSmithKline February 2016 Phase 2
NCT02575066 Not yet recruiting Sarcoma|Soft Tissue Sarcomas The Netherlands Cancer Institute January 2016 Phase 2
NCT02535351 Not yet recruiting Clear-cell Metastatic Renal Cell Carcinoma Fondazione IRCCS Istituto Nazionale dei Tumori, Milano October 2015 Phase 3
NCT02560012 Not yet recruiting Carcinoma, Renal Cell The University of Texas Health Science Center, Houston October 2015 Phase 2

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Chemical Information

Download Pazopanib HCl (GW786034 HCl) SDF
Molecular Weight (MW) 473.98


CAS No. 635702-64-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 17 mg/mL (35.86 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck 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.
Chemical Name 5-(4-((2,3-dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-2-ylamino)-2-methylbenzenesulfonamide hydrochloride

Customer Product Validation (2)

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Source J Virol, 2011, 85(5): 2296-303. Pazopanib HCl (GW786034 HCl) purchased from Selleck
Method Endothelial Cell Permeability Assay
Cell Lines Endothelial cells
Concentrations 0-100 nM
Incubation Time 15-60 min
Results Figure A defines concentrations of kinase inhibitors which block ANDV-induced EC permeability approximately 50% (IC50s).The IC50s of pazopanib is 100 nM. we assessed the abilities of VEGFR2 and SFK inhibitors to block ANDV-induced permeability at their IC50s from 15 to 60 min after VEGF addition. Pazopanib inhibited ANDV-induced permeability by 40 to 60% at nanomolar IC50 levels (Figure B).

Click to enlarge
Source Expert Opin Pharmacother 2014 15(11), 1489-99. Pazopanib HCl (GW786034 HCl) purchased from Selleck
Method Microscopic images
Cell Lines RCC cells
Concentrations 10, 20 ug/ml
Incubation Time 48 h
Results 31% of the cells treated with high-dose pazopanib and 27% of cells treated with low-dose pazopanib became apoptotic, which is a significant proportion of cells compared to the other two drugs and the background. Interestingly, the combination of IL-2 did not affect the level of apoptosis induced by pazopanib.

Product Use Citation (4)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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