Pazopanib

Catalog No.S3012

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 in cell-free assays, respectively.

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Pazopanib Chemical Structure

Pazopanib Chemical Structure
Molecular Weight: 437.52

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Pazopanib is available in the following compound libraries:

Product Information

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Product Description

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 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] PPazopanib 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

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Animal Study: [2]

Animal Models Immunodeficient mice bearing SYO-1 cells
Formulation
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)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

References

[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 http://clinicaltrials.gov, updated on 2016-06-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02342600 Not yet recruiting Gastrointestinal Stromal Tumors Sarcoma Alliance for Research through Collaboration|Novartis January 2017 Phase 2
NCT02348398 Not yet recruiting Cervical Cancer M.D. Anderson Cancer Center|GlaxoSmithKline August 2016 Phase 2
NCT02795819 Not yet recruiting Renal Cell Carcinoma|Soft Tissue Sarcoma|Metastatic Disease Virginia Commonwealth University|Arno Therapeutics|Nation  ...more Virginia Commonwealth University|Arno Therapeutics|National Cancer Institute (NCI) July 2016 Phase 1
NCT02691767 Not yet recruiting Refractory Solid Tumors Samsung Medical Center May 2016 --
NCT02729194 Not yet recruiting Carcinoma, Renal Cell University of Michigan Cancer Center April 2016 Phase 0

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Chemical Information

Download Pazopanib SDF
Molecular Weight (MW) 437.52
Formula

C21H23N7O2S

CAS No. 444731-52-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms GW786034
Solubility (25°C) * In vitro DMSO 87 mg/mL warming (198.84 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <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

Customer Product Validation(2)


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Rating
Source J Virol 2011 85(5), 2296-303. Pazopanib purchased from Selleck
Method Assessment of monolayer permeability
Cell Lines Endothelial cells
Concentrations 100 nM
Incubation Time 15 min
Results VEGFR2-Src inhibitor pazopanib block ANDV-induced permeability.

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Rating
Source Expert Opin Pharmacother 2014 15(11), 1489-99. Pazopanib purchased from Selleck
Method Microscopic images
Cell Lines RCC cells
Concentrations 10, 20 ug/ml
Incubation Time 48 h
Results The apoptosis rate did not differ between IL-2 and sunitinib-treated cells and this was similar to that of the background. On the other hand, 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.

Tech Support

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