Chemical Property of Pazopanib Hydrochloride
Chemical Property:
- Boiling Point:728.8 °C at 760 mmHg
- Flash Point:394.6 °C
- PSA：127.41000
- LogP:5.79510
- Storage Temp.:Hygroscopic, Refrigerator, under inert atmosphere
- Solubility.:Acetonitrile (Slightly), DMSO (Slightly)
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:8
- Rotatable Bond Count:5
- Exact Mass:473.1400719
- Heavy Atom Count:32
- Complexity:717
- Purity/Quality:
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99% *data from raw suppliers
5-{4-[(2,3-Dimethyl-2H-indazol-6-yl)-methyl-amino]-pyrimidin-2-ylamino}-2-methyl-benzenesulfonamide hydrochloride *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl
- Recent ClinicalTrials:Pazopanib Hydrochloride in Treating Patients With Progressive Carcinoid Tumors
- Recent EU Clinical Trials:RAR-Immune: A randomised, comparative, prospective, multicentre study of the efficacy of nivolumab + ipilimumab versus pazopanib alone in patients with metastatic or unresectable advanced sarcoma of rare subtype
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Description
The growth of solid tumors is dependent on angiogenesis, the process
wherein new capillaries are formed from existing blood vessels. VEGF is
one of the most important inducers of angiogenesis and expressed at high
levels by most tumors. Hence, the inhibition of VEGF or its receptor
signaling system is an attractive target for cancer therapeutics. The most
studied and developed inhibitors are monoclonal antibodies that neutralize VEGF (e.g., bevacizumab), anti-VEGF ribozymes (e.g., angiozyme),
and small-molecule VEGFR kinase inhibitors (e.g., sunitinib, sorafenib).
Pazopanib is the latest VEGFR kinase inhibitor to reach the market. It is
indicated for the oral treatment of advanced RCC. The biological functions of the VEGF family are mediated by activation of three structurally
homologous tyrosine kinase receptors, VEGFR-1, VEGFR-2, and VEGFR3. In vitro, pazopanib inhibits VEGFR-1, VEGFR-2, and VEGFR-3 with
IC50 values of 10, 30, and 47 nM, respectively.
In addition, it inhibits
several of the closely related tyrosine receptor kinases, including platelet-derived growth-factor receptor β(PDGFR-β), c-kit, and fibroblast
growth factor receptor-1 (FGFR1) with IC50 values of 84, 74, and
140 nM, respectively. In human umbilical vein endothelial cells
(HUVEC), pazopanib inhibits VEGF-induced proliferation more potently
than basic fibroblast growth factor (bFGF)-stimulated proliferation
(IC50 = 21 nM vs. 721 nM) and concentration-dependently inhibits
VEGF-induced VEGFR-2 phosphorylation (IC50 = 7 nM). It also potently
inhibits angiogenesis in Matrigel plug and corneal micropocket assays. The most common adverse events associated with pazopanib
were diarrhea, hypertension, hair depigmentation, nausea, anorexia,
and vomiting.
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Uses
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively - See more at: http://www.selleckchem.com/products/Pazopanib-Hyd The Hydrochloride salt of Pazopanib (P210925) a oral angiogenesis inhibitor targeting VEGFR and PDGFR.
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Clinical Use
Pazopanib is a potent and selective multi-targeted receptor
tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3,
PDGFR-a/b, and c-kit that blocks tumor growth and inhibits angiogenesis.
It was approved for renal cell carcinoma by the U.S. Food
and Drug Administration in 2009 and is marketed under the trade
name Votrient by the drug’s manufacturer, GlaxoSmithKline.
