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
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.
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.
N-Bromosuccinimide Price
- Product number
- 29425
- Product name
- Fruquintinib
- Packaging
- 10mg
- Price
- $50
- Updated
- 2024/03/01
- Product number
- 29425
- Product name
- Fruquintinib
- Packaging
- 250mg
- Price
- $849
- Updated
- 2024/03/01
- Product number
- 29425
- Product name
- Fruquintinib
- Packaging
- 50mg
- Price
- $220
- Updated
- 2024/03/01
- Product number
- 29425
- Product name
- Fruquintinib
- Packaging
- 100mg
- Price
- $389
- Updated
- 2024/03/01
- Product number
- CS-5558
- Product name
- Fruquintinib
- Purity
- 99.58%
- Packaging
- 5mg
- Price
- $55
- Updated
- 2021/12/16
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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View Lastest Price from Fruquintinib|HMPL-013 manufacturers
- 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
- 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
- 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