Name | Pazopanib Hydrochloride |
Synonyms | ArMala 786034 Votrient GW786034B Pazopanib HCl Unii-33Y9anm545 UNII-33Y9ANM545 Pazopanib hydrochloride Pazopanib Hydrochloride Pazopanib Hydrochloride (GW786034) 5-(4-((2,3-diMethyl-2H-indazol-6-yl)(Methyl)aMino)pyriMidin-2-ylaMino)-2-MethylbenzenesulfonaMide hydrochloride BenzenesulfonaMide, 5-[[4-[(2,3-diMethyl-2H-indazol-6-yl)MethylaMino]-2-pyriMidinyl]aMino]-2-Methyl-, hydrochloride 5-((4-((2,3-Dimethyl-2H-indazol-6-yl)methylamino)pyrimidin-2-yl)amino)-2-methylbenzenesulfonamide monohydrochloride Benzenesulfonamide, 5-((4-((2,3-dimethyl-2H-indazol-6-yl)methylamino)-2-pyrimidinyl)amino)-2-methyl-,monohydrochloride |
CAS | 635702-64-6 |
EINECS | 619-728-0 |
InChI | InChI=1/C21H23N7O2S.ClH/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);1H |
Molecular Formula | C21H23N7O2S.ClH |
Molar Mass | 473.987 |
Melting Point | >290°C (dec.) |
Solubility | Acetonitrile (Slightly), DMSO (Slightly) |
Appearance | Yellow powder. |
Color | White to Off-White |
Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
Stability | Hygroscopic |
Use | Pazopanib HCl (GW786034 HCl) is a new inhibitor targeting multiple targets such as VEGFR-1, VEGFR-2, VEGFR-3, PDGFR, FGFR, c-Kit and c-fms. IC50 is 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM respectively. |
In vitro study | In HUVEC cells, Pazopanib significantly inhibited VEGF-induced phosphorylation of VEGFR-2 with an IC50 of 8nm. Pazopanib exhibited growth inhibition in All synovial sarcoma cell lines, including SYO-1 and HS-SY-II cells, in a dose-dependent manner. 1 µg/mL Pazopanib can inhibit the proliferation of SYO-1 and HS-SY-II cells, while 5 µg/mL Pazopanib can completely block their proliferation. Pazopanib induces synovial sarcoma cells to stay in the G1 phase and thus inhibit their growth. AKTs, GSK-3β, JNKs, p70 S6 kinase, and phosphorylation of mTOR were inhibited in Pazopanib-treated SYO-1 cells compared to control cells. Between concentrations of 20 mg/mL and 22.5 mg/mL, Pazopanib caused a progressive decline in RPE cell viability. |
In vivo study | Mice treated with 30 mg/kg or 100 mg/kg Pazopanib had significantly less tumor symptoms than mice treated with no Pazopanib or with only 10 mg/kg Pazopanib. The Pazopanib treatment was well tolerated and there was no significant difference in body weight between the groups. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.11 ml | 10.549 ml | 21.098 ml |
5 mM | 0.422 ml | 2.11 ml | 4.22 ml |
10 mM | 0.211 ml | 1.055 ml | 2.11 ml |
5 mM | 0.042 ml | 0.211 ml | 0.422 ml |