Pazopanib

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Pazopanib is an approved drug, is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits vascular endothelial growth factor receptors (VEGFR)-1, -2 and -3, c-kit and platelet derived growth factor receptor (PDGF-R), which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Price and Availability

Pazopanib free base, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 202161Name: PazopanibCAS#: 444731-52-6Chemical Formula: C21H23N7O2SExact Mass: 437.16339Molecular Weight: 437.52Elemental Analysis: C, 57.65; H, 5.30; N, 22.41; O, 7.31; S, 7.33

Synonym:GW786034; GW786034; GW 786034; Pazopanib; US brand name: Votrient.

IUPAC/Chemical Name:5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide

InChi Key:CUIHSIWYWATEQL-UHFFFAOYSA-N

InChi Code:InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)

SMILES Code:O=S(C1=CC(NC2=NC=CC(N(C3=CC4=NN(C)C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

Technical Data

Additional Information

Pazopanib hydrochloride is a white to slightly yellow solid. It is very slightly soluble at pH 1 and practically insoluble above pH 4 in aqueous media. Tablets of VOTRIENT are for oral administration. Each 200 mg tablet of VOTRIENT contains 216.7 mg of pazopanib hydrochloride, equivalent to 200 mg of pazopanib free base. The inactive ingredients of VOTRIENT are: Tablet Core: Magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate. Coating: Gray film-coat: Hypromellose, iron oxide black, macrogol/polyethylene glycol 400 (PEG 400), polysorbate 80, titanium dioxide. Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR) -1 and -3, cytokine receptor (Kit), interleukin-2 receptor inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice  

References

  1: Jeldres C, Sun M, Perrotte P,Karakiewicz PI. Pazopanib trial data cannot support first-line use. NatRev Urol. 2010 Jun;7(6):307-8. PubMed PMID: 20535144.

2: Altorki N, Lane ME, Bauer T, Lee PC, Guarino MJ, Pass H, Felip E,Peylan-Ramu N, Gurpide A, Grannis FW, Mitchell JD, Tachdjian S, SwannRS, Huff A, Roychowdhury DF, Reeves A, Ottesen LH, Yankelevitz DF. PhaseII Proof-of-Concept Study of Pazopanib Monotherapy in Treatment-NaivePatients With Stage I/II Resectable Non-Small-Cell Lung Cancer. J ClinOncol. 2010 Jun 1. [Epub ahead of print] PubMed PMID: 20516450.

3: Sideras K, Menefee ME, Burton JK, Erlichman C, Bible KC, Ivy SP.Profound Hair and Skin Hypopigmentation in an African American WomanTreated With the Multi-Targeted Tyrosine Kinase Inhibitor Pazopanib. JClin Oncol. 2010 Jun 1. [Epub ahead of print] PubMed PMID: 20516434.

4: Tailor TD, Hanna G, Yarmolenko PS, Dreher MR, Betof AS, Nixon AB,Spasojevic I, Dewhirst MW. Effect of pazopanib on tumor microenvironmentand liposome delivery. Mol Cancer Ther. 2010 Jun;9(6):1798-808. Epub2010 Jun 1. PubMed PMID: 20515941.

5: Hamberg P, Verweij J, Sleijfer S. (Pre-)Clinical Pharmacology andActivity of Pazopanib, a Novel Multikinase Angiogenesis Inhibitor.Oncologist. 2010 May 28. [Epub ahead of print] PubMed PMID: 20511320.

6: Böhm S, Hess D, Gillessen S, Brändle M. Improved glycemic controlwith the multi-receptor tyrosine kinase inhibitor pazopanib. DiabetesCare. 2010 Jun;33(6):e82. PubMed PMID: 20508227.

7: Sternberg CN. Pazopanib in renal cell carcinoma. Clin Adv HematolOncol. 2010 Apr;8(4):232-3. PubMed PMID: 20505644.