Pazopanib

Catalog No.S3012 Synonyms: GW786034

For research use only.

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

Pazopanib Chemical Structure

CAS No. 444731-52-6

Selleck's Pazopanib has been cited by 67 publications

Purity & Quality Control

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Biological Activity

Description Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Targets
VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
Click to View More Targets
10 nM 30 nM 47 nM 74 nM 84 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Assay
Methods Test Index PMID
Western blot p53 / PUMA ; p-Akt / Akt 27924057
Growth inhibition assay Cell viability 27924057
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]

Protocol (from reference)

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 437.52
Formula

C21H23N7O2S

CAS No. 444731-52-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05180695 Not yet recruiting Drug: Pazopanib|Drug: HDM201 Advanced Soft-tissue Sarcoma|Metastatic Soft-tissue Sarcoma Centre Leon Berard|Novartis|National Cancer Institute France January 2022 Phase 1|Phase 2
NCT04659343 Recruiting Drug: Medical treatment for metastatic renal cell carcinoma Kidney Cancer|Renal Cell Carcinoma Metastatic|Drug Toxicity|Drug Side Effect|Drug Mechanism Frede Donskov|Odense University Hospital|Herlev Hospital|Rigshospitalet Denmark|University of Aarhus November 1 2020 --
NCT03735758 Terminated Drug: pazopanib or guideline conform chemotherapy Soft Tissue Sarcoma Adult GWT-TUD GmbH November 2 2018 Phase 4
NCT03334409 Terminated Drug: Ascorbic Acid|Drug: Pazopanib Hydrochloride Clear Cell Renal Cell Carcinoma|Metastatic Clear Cell Renal Cell Carcinoma|Stage III Renal Cell Cancer AJCC v8|Stage IV Renal Cell Cancer AJCC v7|Unresectable Renal Cell Carcinoma Academic and Community Cancer Research United|National Cancer Institute (NCI) February 16 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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