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.
- InChI
- InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
- InChIKey
- BALLNEJQLSTPIO-UHFFFAOYSA-N
- SMILES
- O1C2=CC(OC3=C4C(=NC=N3)C=C(OC)C(OC)=C4)=CC=C2C(C(NC)=O)=C1C
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
- API0026222
- Product name
- FRUQUINTINIB
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $501.66
- 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.
Uses
Fruquintinib (HMPL-013) is a highly selective VEGFR-1/2/3 tyrosine kinase inhibitor. It was approved by the FDA on 8 November 2023 for the treatment of adult patients with metastatic colorectal cancer. and these patients had previously received fluoropyrimidine, oxaliplatin and irinotecan chemotherapy, anti-vascular endothelial growth factor therapy, and anti-epidermal growth factor receptor (EGFR) therapy. Fruquintinib has also been shown to improve cognitive deficits and pathological changes in a mouse model of cerebral amyloid angiopathy (CAA).
Mechanism of action
By blocking the vascular endothelial growth factor signalling pathway, Fruquintinib inhibits the formation of new blood vessels in tumours, thereby reducing blood supply and inhibiting tumour growth.
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 $0.00-0.00/g
- Min. Order
- 2g
- Purity
- 99%
- Supply Ability
- 1000kg
- Release date
- 2024-08-07
- Product
- Fruquintinib 1194506-26-7
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 23000
- Release date
- 2024-06-18
- Product
- Fruquintinib 1194506-26-7
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-03