| Identification | Back Directory | [Name]
N-(2-(diMethylaMino)ethyl)-1-(3-((4-((2-Methyl-1H-indol-5-yl)oxy)pyriMidin-2-yl)aMino)phenyl)MethanesulfonaMide | [CAS]
1308672-74-3 | [Synonyms]
HMPL012
CS-2346
HMPL-012
KDR-IN-1
EOS-61498
Surufatinib
HMPL-012;SURUFATINIB;HMPL012
N-(2-(DIMETHYLAMINO)ETHYL)-1-(3-((4-((2-METHYL-1H-INDOL-5-YL)OXY)PYRIMIDIN-2-YL)AMINO)PHENYL)METHANE
Benzenemethanesulfonamide, N-[2-(dimethylamino)ethyl]-3-[[4-[(2-methyl-1H-indol-5-yl)oxy]-2-pyrimidinyl]amino]-
N-(2-(diMethylaMino)ethyl)-1-(3-((4-((2-Methyl-1H-indol-5-yl)oxy)pyriMidin-2-yl)aMino)phenyl)MethanesulfonaMide | [Molecular Formula]
C24H28N6O3S | [MOL File]
1308672-74-3.mol | [Molecular Weight]
480.58 |
| Chemical Properties | Back Directory | [Boiling point ]
712.9±70.0 °C(Predicted) | [density ]
1.332±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:98.0(Max Conc. mg/mL);203.92(Max Conc. mM) | [form ]
A solid | [pka]
5.22±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Sulfatinib is used in pharmaceutical compositions comprising of micronized drug. | [in vivo]
In animal studies, a single oral dosing of Sulfatinib inhibits VEGF stimulated VEGFR2 phosphorylation in lung tissues of nude mice in an exposure-dependent manner. Furthermore, elevation of FGF23 levels in plasma 24 hours post dosing suggests suppression of FGFR signaling. Sulfatinib demonstrates potent tumor growth inhibition in multiple human xenograft models and decreases CD31 expression remarkably, suggesting strong inhibition on angiogenesis through VEGFR and FGFR signaling. In a syngeneic murine colon cancer model CT-26, Sulfatinib demonstrates moderate tumor growth inhibition after single agent treatment[1]. After oral dosing of 10 mg/kg, the AUC and Cmax are 397 ng/mL and 138ng/mL in the mouse, respectively[1]. | [IC 50]
VEGFR1; VEGFR2; VEGFR3; FGFR1; CSF1R |
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