WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202161
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).
MedKoo Cat#: 202161
Chemical Formula: C21H23N7O2S
Exact Mass: 437.16339
Molecular Weight: 437.52
Elemental 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
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
1: Jeldres C, Sun M, Perrotte P, Karakiewicz PI. Pazopanib trial data cannot support first-line use. Nat Rev 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, Swann RS, Huff A, Roychowdhury DF, Reeves A, Ottesen LH, Yankelevitz DF. Phase II Proof-of-Concept Study of Pazopanib Monotherapy in Treatment-Naive Patients With Stage I/II Resectable Non-Small-Cell Lung Cancer. J Clin Oncol. 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 Woman Treated With the Multi-Targeted Tyrosine Kinase Inhibitor Pazopanib. J Clin 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 microenvironment and liposome delivery. Mol Cancer Ther. 2010 Jun;9(6):1798-808. Epub 2010 Jun 1. PubMed PMID: 20515941.
5: Hamberg P, Verweij J, Sleijfer S. (Pre-)Clinical Pharmacology and Activity of Pazopanib, a Novel Multikinase Angiogenesis Inhibitor. Oncologist. 2010 May 28. [Epub ahead of print] PubMed PMID: 20511320.
6: BÃ¶hm S, Hess D, Gillessen S, BrÃ¤ndle M. Improved glycemic control with the multi-receptor tyrosine kinase inhibitor pazopanib. Diabetes Care. 2010 Jun;33(6):e82. PubMed PMID: 20508227.
7: Sternberg CN. Pazopanib in renal cell carcinoma. Clin Adv Hematol Oncol. 2010 Apr;8(4):232-3. PubMed PMID: 20505644.