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Pazopanib

Cat. No. M1842
Pazopanib Structure
Synonym:

GW786034

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 55  USD55 In stock
50mg USD 110  USD110 In stock
100mg USD 160  USD160 In stock
200mg USD 260  USD260 In stock
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Quality Control & Documentation
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 (for reference only)
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
Chemical Information
Molecular Weight 437.52
Formula C21H23N7O2S
CAS Number 444731-52-6
Solubility (25°C) DMSO 62 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Sparidans et al. J Chromatogr B Analyt Technol Biomed Life Sci. Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the tyrosine kinase inhibitor pazopanib in human plasma.

[2] Zivi et al. Expert Opin Drug Saf. Safety and tolerability of pazopanib in the treatment of renal cell carcinoma.

[3] Necchi et al. Lancet Oncol. Pazopanib in advanced and platinum-resistant urothelial cancer: an open-label, single group, phase 2 trial.

[4] Sleijfer et al. Br J Cancer. Cytokine and angiogenic factors associated with efficacy and toxicity of pazopanib in advanced soft-tissue sarcoma: an EORTC-STBSG study.

[5] Podar K, et al. Proc Natl Acad Sci U S A. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma.

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


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