ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > protein tyrosine kinase > Unii-33Y9anm545
Unii-33Y9anm545 Chemical Properties
- form Yellow powder.
Unii-33Y9anm545 Usage And Synthesis
- DescriptionThe 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.
- OriginatorGlaxoSmithKline (US)
- UsesPazopanib Hydrochloride (GW786034, Votrient, Armala) 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.
- UsesPazopanib (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
- DefinitionChEBI: A hydrochloride salt prepared from equimolar amounts of pazopanib and hydrochloric acid. Used for treatment of kidney cancer.
- brand nameVotrient
- Side effectsPazopanib is synthesized in five chemical steps starting from 3-methyl-6-nitroindazole, which is converted to the corresponding 2,3-dimethylindazole analog via N-methylation with trimethyloxonium tetrafluoroborate. Subsequent reduction of the nitro group to the amino group using tin chloride followed by condensation with 2,4dichloropyrimidine yields a chloropyrimidinylaminoindazole intermediate. The final two steps leading up to pazopanib consist of an N-methylation reaction using iodomethane and cesium carbonate followed by condensation with 5-amino-2-methylbenzenesulfonamide.
- Palonosetron Hydrochloride Afatinib 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate Cabazitaxel Lapatinib ditosylate BIBW2992 DiMaleate AZD-9291 Nintedanib Ethanesulfonate Salt Pazopanib 2,3-DIMETHYL-6-NITRO-2H-INDAZOLE 2,3-dimethyl-2H-indazol-6-amine hydrochloride 2-Ethyl-5-nitrobenzenamine ,98% 3-Methyl-6-nitroindazole Sorafenib tosylate Gefitinib Axitinib Dasatinib Regorafenib
- Company Name:Shanghai Payne Pharmaceutical Technology Co.Ltd Gold
- Tel:18678586262 021-58123769
- Company Name:Yangzhou QinYuan Pharmaceutical Co., Ltd. Gold
- Tel:13773367191 0514-80939770
- Company Name:Taizhou Ruixin Chemical Co., Ltd. Gold
- Tel:15867635987 0576-89085261
- Company Name:Jiaxing Triview Biochemical Products Co., Ltd. Gold
- Tel:13806705416 0573-87228088-
- Company Name:Nanjing Wedo Pharm Tech Co., Ltd. Gold