ChemicalBook CAS DataBase List Surufatinib

Surufatinib

Product NameSurufatinib
CAS1308672-74-3
CBNumberCB72711244
MFC24H28N6O3S
MW480.58
MOL File1308672-74-3.mol
MSDS FileSDS

Chemical Properties

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
InChIKey	TTZSNFLLYPYKIL-UHFFFAOYSA-N
SMILES	C1(CS(NCCN(C)C)(=O)=O)=CC=CC(NC2=NC=CC(OC3C=CC4=C(C=3)C=C(C)N4)=N2)=C1
FDA UNII	B2K5L1L8S9

Surufatinib Price

Product number	Packaging	Price	Product description	Buy
Cayman Chemical 34206	1mg	$41	Sulfatinib ≥98%	Buy
Cayman Chemical 34206	5mg	$119	Sulfatinib ≥98%	Buy
Cayman Chemical 34206	10mg	$178	Sulfatinib ≥98%	Buy
Cayman Chemical 34206	25mg	$245	Sulfatinib ≥98%	Buy
ChemScene CS-5949	1mg	$54	Sulfatinib 99.52%	Buy

Surufatinib Chemical Properties,Usage,Production

Uses

Sulfatinib is used in pharmaceutical compositions comprising of micronized drug.

Mechanism of action

Surufatinib can inhibit multiple targets related to angiogenesis and tumor growth, including VEGFR, FGFR1 and CSF-1R.

Synthesis

Treatment of sulfonyl chloride 358 at room temperature using triethylamine and 2,2,2-trifluoroethanol (TFE) as solvents followed by hydrogenation afforded aniline 360. Exposure of 360 to DBU under microwave conditions generated an intermediate sulfinyl group. This intermediate sulfinyl group subsequently underwent nucleophilic attack by a commercial diamine, of which diamine 361 afforded the desired sulfonamide 362. Dichloropyrimidine 363 underwent a substitution reaction with hydroxyindole 364 to afford diaryl ether 365. Diaryl ether 365 then underwent a second substitution reaction with amine 362 under acidic conditions. Exposure of the product to a base in aqueous solution ultimately afforded surufatinib in 50% yield.
Surufatinib synthesis

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 C_max are 397 ng/mL and 138ng/mL in the mouse, respectively^[1].

IC 50

VEGFR1; VEGFR2; VEGFR3; FGFR1; CSF1R

Surufatinib

Chemical Properties

Surufatinib Price

Surufatinib Chemical Properties,Usage,Production

Surufatinib synthesis

Preparation Products And Raw materials

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Surufatinib Spectrum

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