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Fruquintinib|HMPL-013

Fruquintinib|HMPL-013 Structure
CAS No.
1194506-26-7
Chemical Name:
Fruquintinib|HMPL-013
Synonyms
CS-1643;R-228060;HMPL-013;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
Molecular Weight:
393.39
MOL File:
1194506-26-7.mol
MSDS File:
SDS
Modify Date:
2024/7/3 13:03:20
Request For Quotation

Fruquintinib|HMPL-013 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

Fruquintinib|HMPL-013 Chemical Properties,Uses,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.

Fruquintinib|HMPL-013 Preparation Products And Raw materials

Raw materials

Preparation Products

Fruquintinib|HMPL-013 Suppliers

Global( 163)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Dr. Reddy's Laboratories Ltd +91-4049002900 +91-4049002900 Hyderabad, India 165 58 Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
Wuhan Jingkang en Biomedical Technology Co., Ltd +8613720134139 China 4692 58 Inquiry
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. +86-18600796368 +86-18600796368 China 73 58 Inquiry
Zhengzhou Anbu Chem Co.,Ltd +86-0371-88006763; +8615988602810 China 3000 58 Inquiry
Apeloa production Co.,Limited +8619933239880 China 853 58 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
BOC Sciences +1-631-485-4226 United States 19553 58 Inquiry
Zhengzhou Alfa Chemical Co.,Ltd +8618530059196 China 13035 58 Inquiry
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 United States 19892 58 Inquiry
Supplier Advantage
Dr. Reddy's Laboratories Ltd 58
A.J Chemicals 58
Wuhan Jingkang en Biomedical Technology Co., Ltd 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 58
Zhengzhou Anbu Chem Co.,Ltd 58
Apeloa production Co.,Limited 58
ATK CHEMICAL COMPANY LIMITED 60
BOC Sciences 58
Zhengzhou Alfa Chemical Co.,Ltd 58
TargetMol Chemicals Inc. 58

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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 Fruquintinib|HMPL-013 USP/EP/BP EOS-61054 CS-1643 BMS-986472 1194506-26-7 Inhibitors API