Pazopanib

For research use only.

Catalog No.S3012 Synonyms: GW786034

60 publications

Pazopanib Chemical Structure

CAS No. 444731-52-6

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.

Selleck's Pazopanib has been cited by 60 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

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)
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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SNU-449 NF\RcW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVziPXFyUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDlwMkK4Oe69VQ>? M4njWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / PUMA ; 

PubMed: 27924057     


The expression of p53 or PUMA by western blotting analysis in HCT-116 cells treated with (left) 20 μM pazopanib for indicated hours or (right) with 1-20 μM pazopanib for 24 hours.

p-Akt / Akt ; 

PubMed: 27924057     


Akt is inhibited after pazopanib treatment in colon cells. The expression of P-Akt (S473) was detected by western blotting in (A) RKO or HT-29 cells after 20 μM pazopanib treatment for indicated times.

27924057
Growth inhibition assay
Cell viability; 

PubMed: 27924057     


Cell viability was analyzed using Cell Counting Kit-8 at 0, 3, 6, 12 and 24 hours after 1, 5, 10, or 20 μM pazopanib treatment in HCT-116 cells. Data represent the mean ± SEM of four independent experiments.

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

Animal Research:

[2]

- Collapse
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL warmed (198.84 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 437.52
Formula

C21H23N7O2S

CAS No. 444731-52-6
Storage powder
in solvent
Synonyms GW786034
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

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 Recruiting 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
NCT03149120 Withdrawn Biological: Nivolumab|Drug: Pazopanib Soft Tissue Sarcomas NYU Langone Health|Bristol-Myers Squibb August 2017 Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID