Name | Pazopanib |
Synonyms | CS-1857 Pazopanib Pazopanib(GW786034) Pazopanib for research Pazopanib (free base) (GW786034, Votrient) 5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzenesulfonamide 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide 5-[(4-{[(2,3-diMethyl-2H-indazol-6-yl)Methyl]aMino}pyriMidin-2-yl)aMino]-2-Methylbenzene-1-sulfonaMide 5-(4-((2,3-diMethyl-3,3a-dihydro-2H-indazol-6-yl)(Methyl)aMino)pyriMidin-2-ylaMino)-2-MethylbenzenesulfonaMide |
CAS | 444731-52-6 |
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 |
Molar Mass | 437.52 |
Density | 1.40 |
Melting Point | 285-289°C (dec.) |
Boling Point | 728.8±70.0 °C(Predicted) |
Flash Point | 359℃ |
Solubility | DMSO 88 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
Vapor Presure | 4.26E-21mmHg at 25°C |
Appearance | Yellow powder. |
Color | White to Beige |
pKa | 10.19±0.60(Predicted) |
Storage Condition | Refrigerator |
Use | A potent and selective inhibitor of Flk-1, PDGFR and c-kit |
In vitro study | Pazopanib effectively inhibited VEGFR2 phosphorylation in HUVEC cells induced by VEGF with IC50 of 8 nM. Pazopanib showed dose-dependent growth inhibition in All synovial sarcoma cell lines, including SYO-1 and HS-SY-II cells. The proliferation of SYO-1 and HS-SY-II cells was inhibited at 1 μg/ml Pazopanib and completely abolished at 5 μg/ml Pazopanib. Pazopanib causes a Arrest in G1 phase and thus inhibits the growth of synovial sarcoma cells. Phosphorylation of Akts,GSK-3β,JNKs,p70 S6 kinase, and mTOR was inhibited in Pazopanib-treated SYO-1 cells compared to vector-treated cells. Pazopanib showed a gradually increasing decrease in RPE cell activity between 20 mg/mL and 22.5 mg/ml. |
In vivo study | Tumor burden was significantly reduced in mice treated with 30 mg/kg or 100 mg/kg Pazopanib compared to mice treated with vehicle or 10 mg/kg Pazopanib. The Pazopanib treatment was well tolerated and there was no significant difference in the body weight of each group of mice. |
Risk Codes | R43 - May cause sensitization by skin contact R62/63 - |
Safety Description | S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S28B - |
HS Code | 29350090 |