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Pazopanib

Cat. No. M1842

Pazopanib Structure

Synonym: GW786034

Size Price Availability Quantity
50mg USD 110 In stock
100mg USD 175 In stock
200mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Pazopanib is an oral angiogenesis inhibitor of tyrosine kinases, targeting vascular endothelial growth factor receptor, platelet-derived growth factor receptor, and c-Kit. Two clinical trials met the inclusion criteria for the use of pazopanib in RCC (a Phase II and a Phase III trial). Pazopanib is an inhibitor of numerous tyrosine kinases, including vascular endothelial growth factor receptor and platelet-derived growth factor receptors. It is involved in inhibiting signaling pathways, angiogenesis, and cell proliferation. A 2-fold increase in AUC was seen when pazopanib was administered with a high-fat meal as well as when crushing the tablet. Thus, pazopanib should be administered on an empty stomach at least 1 hour before or 2 hours after a meal. Pazopanib is primarily metabolized by cytochrome P-450 3A4, and caution should be used with concomitant administration of cytochrome P-450 inducers and/or inhibitors. In a Phase III trial of pazopanib in metastatic RCC, pazopanib reportedly improved progression-free survival from a median of 4.2 to 9.2 months compared with placebo (P < 0.0001). The most common adverse effects of pazopanib were hypertension, hair depigmentation, diarrhea, nausea, anorexia, and vomiting. Many of the grade 3/4 toxicities were hepatic in nature, with elevations occurring in aspartate aminotransferase, alanine aminotransferase, and bilirubin. Pazopanib is reportedly effective in the treatment of metastatic RCC. Although there are currently no direct comparisons between pazopanib and other tyrosine kinase inhibitors, the data suggest that pazopanib may be a first-line option in the treatment of RCC. The only Phase III trial of pazopanib suggests improvement of progression-free survival in RCC as well as tolerability in the selected population.

Protocol
Cell Experiment
Cell lines MM.1S, MM.1R, RPMI-Dox40 (Dox40), and OPM2 cells
Preparation method Cell Proliferation Assay
Cell growth was assessed by measuring [3H]thymidine uptake as described.
Concentrations 0~10 μg/ml
Incubation time 48 h
Animal Experiment
Animal models MM.1S MM cells tumor xenograft mouse model in Beige-nude Xid mice
Formulation 0.5% hydroxypropylmethyl cellulose (Sigma-Aldrich, St. Louis, MO) and 0.1% Tween-80 (Sigma-Aldrich) in water
Dosages 30 and 100mg/kg daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 437.52
Formula C21H23N7O2S
CAS Number 444731-52-6
Purity >99%
Solubility DMSO ≥90 mg/mL
Storage at -20°C
References

Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the tyrosine kinase inhibitor pazopanib in human plasma.
Sparidans et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Aug 10. PMID: 22917595.

Safety and tolerability of pazopanib in the treatment of renal cell carcinoma.
Zivi et al. Expert Opin Drug Saf. 2012 Sep;11(5):851-9. PMID: 22861374.

Pazopanib in advanced and platinum-resistant urothelial cancer: an open-label, single group, phase 2 trial.
Necchi et al. Lancet Oncol. 2012 Aug;13(8):810-6. PMID: 22819172.

Cytokine and angiogenic factors associated with efficacy and toxicity of pazopanib in advanced soft-tissue sarcoma: an EORTC-STBSG study.
Sleijfer et al. Br J Cancer. 2012 Aug 7;107(4):639-45. PMID: 22805326.

The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma.
Podar K, et al. Proc Natl Acad Sci U S A. 2006 Dec 19;103(51):19478-83. PMID: 17164332.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pazopanib, GW786034 supplier, VEGFR/PDGFR, inhibitors

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