Surufatinib

Product Name: Surufatinib
CAS No.: 1308672-74-3
Chemical Name: Surufatinib
Synonyms: HMPL012;CS-2346;HMPL-012;KDR-IN-1;EOS-61498;Surufatinib;Surufatinib(HPML-012);Sulfatinib, 10 mM in DMSO;HMPL-012;SURUFATINIB;HMPL012;N-(2-(DIMETHYLAMINO)ETHYL)-1-(3-((4-((2-METHYL-1H-INDOL-5-YL)OXY)PYRIMIDIN-2-YL)AMINO)PHENYL)METHANE
CBNumber: CB72711244
Molecular Formula: C24H28N6O3S
Formula Weight: 480.58
MOL File: 1308672-74-3.mol

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Surufatinib Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC

Product number: S688948
Product name: Sulfatinib
Packaging: 1mg
Price: $60
Updated: 2021/12/16

TRC

Product number: S688948
Product name: Sulfatinib
Packaging: 10mg
Price: $340
Updated: 2021/12/16

ChemScene

Product number: CS-5949
Product name: Sulfatinib
Purity: 98.01%
Packaging: 1mg
Price: $50
Updated: 2021/12/16

ChemScene

Product number: CS-5949
Product name: Sulfatinib
Purity: 98.01%
Packaging: 5mg
Price: $90
Updated: 2021/12/16

ChemScene

Product number: CS-5949
Product name: Sulfatinib
Purity: 98.01%
Packaging: 10mg
Price: $120
Updated: 2021/12/16

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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.

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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Surufatinib Suppliers

China 79 India 1 United States 7 Global 87

Kaixin Chemical (Hong Kong) Limited

Tel: 010-88886666-01 13112345678
Fax: CDXH21@126.com
Email: loyson@tcypharm.com
Country: China
ProdList: 597
Advantage: 55

Taizhou Nanfeng Pharmaceutical Research Institute

Tel: nanfengdrug@163.com; 18616377689
Email: nanfengdrug@163.com
Country: China
ProdList: 20009
Advantage: 58

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
Advantage: 61

Shanghai MOF Chemical Tech Limited

Tel: 13661494087 18964793018
Fax: 86-021-51821718 QQ：2427604606
Email: sales@mof-chemicals.com
Country: China
ProdList: 293
Advantage: 55

Sichuan Wei Keqi Biological Technology Co., Ltd.

Tel: 028-81700200 18116577057
Fax: 028-81705658
Email: 3003855609@qq.com
Country: China
ProdList: 7778
Advantage: 56

Shanghai Macklin Biochemical Co.,Ltd.

Tel: 15221275939
Fax: 021-50706099
Email: shenlinxing@macklin.cn
Country: China
ProdList: 15873
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Chizhou Kailong Import and Export Trade Co., Ltd.

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Guangzhou Zhiya Chemdrugs Co.,Ltd

Tel: 18122150900
Fax: QQ:2869377561
Email: sculk28@163.com
Country: China
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SPIRO PHARMA

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Email: eric_feng1954@126.com
Country: China
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Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

1308672-74-3, SurufatinibRelated Search:

2-Methylindole 5-Hydroxyindol-3-acetic Acid 5-HYDROXYINDOLE-3-CARBOXYLIC ACID

N-(2-(diMethylaMino)ethyl)-1-(3-((4-((2-Methyl-1H-indol-5-yl)oxy)pyriMidin-2-yl)aMino)phenyl)MethanesulfonaMide

KDR-IN-1

EOS-61498

HMPL012

HMPL-012

HMPL-012;SURUFATINIB;HMPL012

Surufatinib

CS-2346

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]-

Surufatinib(HPML-012)

Sulfatinib, 10 mM in DMSO

1308672-74-3