GW786034B

SKU: orb1300336

Description

Pazopanib Hydrochloride

Research Area

Product Categories/Products/Small Molecules,Autophagy|||Angiogenesis|||Tyrosine Kinase/Adaptors

Key Properties

• CAS Number: 635702-64-6
• MW: 473.98
• Purity: 99.69%
• Formula: C₂₁H₂₄ClN₇O₂S
• SMILES: Cl.CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=NC=C1

Bioactivity

• Target IC50:
  c-Kit:140 nM|PDGFR:84 nM|c-Fms:146 nM|VEGFR1:10 nM|VEGFR2:30 nM|VEGFR3:47 nM|FGFR:74 nM
• 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.
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• In Vitro:
  Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. 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. Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability.
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• Cell Research:
  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. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

11525740