Fruquintinib|HMPL-013

Product Name: Fruquintinib|HMPL-013
CAS No.: 1194506-26-7
Chemical Name: Fruquintinib|HMPL-013
Synonyms: CS-1643;HMPL-013;R-228060;EOS-61054;BMS-986472;Fruquintinib;Fruquintinib|HMPL-013;Fruquintinib|HMPL-013 USP/EP/BP;6-(6,7-dimethoxyquinazolin-4-yloxy)-N,2-dimethylbenzofuran-3-carboxamide;6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide
CBNumber: CB23037638
Molecular Formula: C21H19N3O5
Formula Weight: 393.39
MOL File: 1194506-26-7.mol

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Fruquintinib|HMPL-013 Property

Boiling point:: 600.5±55.0 °C(Predicted)
Density: 1.302±0.06 g/cm3(Predicted)
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: Soluble in DMSO (up to 5 mg/ml).
pka: 14.35±0.46(Predicted)
form: solid
color: White
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 29425
Product name: Fruquintinib
Packaging: 10mg
Price: $50
Updated: 2024/03/01

Cayman Chemical

Product number: 29425
Product name: Fruquintinib
Packaging: 250mg
Price: $849
Updated: 2024/03/01

Cayman Chemical

Product number: 29425
Product name: Fruquintinib
Packaging: 50mg
Price: $220
Updated: 2024/03/01

Cayman Chemical

Product number: 29425
Product name: Fruquintinib
Packaging: 100mg
Price: $389
Updated: 2024/03/01

American Custom Chemicals Corporation

Product number: API0026222
Product name: FRUQUINTINIB
Purity: 95.00%
Packaging: 5MG
Price: $501.66
Updated: 2021/12/16

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Fruquintinib|HMPL-013 Chemical Properties,Usage,Production

Description

Fruquintinib is a VEGFR inhibitor (IC₅₀s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively). It also inhibits RET, FGFR1, and c-Kit (IC₅₀s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases. Fruquintinib inhibits VEGF-A-induced proliferation of human umbilical vein endothelial cells (HUVECs) and VEGF-C-induced proliferation of human lymphatic endothelial cells (HLECs; IC₅₀s = 1.7 and 4.2 nM, respectively). It decreases tube formation by HUVECs by 74 and 94% when used at concentrations of 30 and 300 nM, respectively. Fruquintinib (0.5-20 mg/kg per day for 21 days) reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models.

Uses

Fruquintinib is a multi-targeted tyrosine kinase inhibitor, a third-line regimen involved in the treatment of advanced non-small cell lung cancer in humans. Fruquintinib is a potent, highly selective and orally active inhibitor of VEGFR1, 2, 3 tyrosine kinases.

in vitro

fruquintinib was found to inhibit vegfr2 with an ic50 of 25 nmol/l. the kinase selectivity of fruquintinib was evaluated against a panel of 253 kinases. the results showed that fruquintinib inhibited vegfr family members with weak inhibition of ret, fgfr-1 and c-kit kinases [1].

in vivo

anti-tumor activity of fruquintinib was evaluated in a variety of tumor xenografts. the results from gastric cancer bgc-823 model seemed to indicate that the drug concentration needs to be at least maintained above ec85 for around 8 hours in order to achieve >80% tumor growth inhibition. bgc-823 was found to be most sensitive to fruquintinib [1].

IC 50

33 nmol/l, 35 nmol/l and 0.5 nmol/l for vegfr1, 2, 3

References

1) Sun?et al.?(2014)?Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1,2,3 tyrosine kinases for cancer therapy; Cancer Biol. Ther.?15?1635 2) Li?et al.?(2018)?Effect of Fruquintinib vs Placebo on Overall Survival in Patients With Previously Treated Metastatic Colorectal Cancer: The FRESCO Randomized Clinical Trial; JAMA?319?2486 3) Lu?et al.?(2018)?Randomized, Double-Blind, Placebo-Controlled, Multicenter Phase II Study of Fruquintinib After Two Prior Chemotherapy Regimens in Chinese Patients With Advanced Nonsquamous Non-Small-cell Lung Cancer; J. Clin. Oncol.?36?1207

Fruquintinib|HMPL-013 Preparation Products And Raw materials

Raw materials

Preparation Products

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Fruquintinib|HMPL-013 Suppliers

Canada 1 China 132 India 2 United Kingdom 1 United States 13 Global 149

MedChemexpress LLC

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Target molecule Corp.

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Musechem

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TargetMol Chemicals Inc.

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InvivoChem

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Cckinase, Inc.

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BOC Sciences

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Aladdin Scientific

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BOC Sciences

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View Lastest Price from Fruquintinib|HMPL-013 manufacturers

Hebei Duling International Trade Co. LTD

Product: Fruquintinib|HMPL-013 1194506-26-7
Price: US $100.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100 tons
Release date: 2022-09-30

Zhengzhou Anbu Chem Co.,Ltd

Product: Fruquintinib|HMPL-013 1194506-26-7
Price: US $0.00/KG
Min. Order: 0.1KG
Purity: 98%
Supply Ability: 1000KGS
Release date: 2023-07-14

Dideu Industries Group Limited

Product: Fruquintinib|HMPL-013 1194506-26-7
Price: US $1.10/g
Min. Order: 1g
Purity: 99.9%
Supply Ability: 100 Tons Min
Release date: 2021-07-06

1194506-26-7, Fruquintinib|HMPL-013Related Search:

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CS-1643

Fruquintinib|HMPL-013

Fruquintinib

6-(6,7-dimethoxyquinazolin-4-yloxy)-N,2-dimethylbenzofuran-3-carboxamide

HMPL-013

3-Benzofurancarboxamide, 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-

6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide

R-228060

6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-1-benzofuran-3-carboxamide

EOS-61054

Fruquintinib|HMPL-013 USP/EP/BP

BMS-986472

1194506-26-7

Inhibitors