Pazopanib

Catalog No.S3012 Synonyms: GW786034

Pazopanib Chemical Structure

Molecular Weight(MW): 437.52

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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USD 210 In stock

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2 Customer Reviews

  • J Virol 2011 85(5), 2296-303. Pazopanib purchased from Selleck.

    Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).

    Expert Opin Pharmacother 2014 15(11), 1489-99. Pazopanib purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
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]

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

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.84 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 437.52
Formula

C21H23N7O2S

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

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Clinical Trial Information

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
NCT02810756 Not yet recruiting Pharmacokinetics of Pazopanib The Netherlands Cancer Institute September 2016 Phase 0
NCT02348398 Not yet recruiting Cervical Cancer M.D. Anderson Cancer Center|GlaxoSmithKline August 2016 Phase 2
NCT02795819 Recruiting Renal Cell Carcinoma|Soft Tissue Sarcoma|Metastatic Disease 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

Tech Support

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Handling Instructions

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID