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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

MDL Number:: MFCD28502149

MOL File:: 1194506-26-7.mol

MSDS File:: SDS

Last updated:2024-05-16 17:35:16

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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
FDA UNII	49DXG3M5ZW
NCI Drug Dictionary	fruquintinib

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 price More Price(15)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	29425	Fruquintinib	1194506-26-7	10mg	$50	2024-03-01	Buy
Cayman Chemical	29425	Fruquintinib	1194506-26-7	250mg	$849	2024-03-01	Buy
Cayman Chemical	29425	Fruquintinib	1194506-26-7	50mg	$220	2024-03-01	Buy
Cayman Chemical	29425	Fruquintinib	1194506-26-7	100mg	$389	2024-03-01	Buy
American Custom Chemicals Corporation	API0026222	FRUQUINTINIB 95.00%	1194506-26-7	5MG	$501.66	2021-12-16	Buy

Product number	Packaging	Price	Buy
29425	10mg	$50	Buy
29425	250mg	$849	Buy
29425	50mg	$220	Buy
29425	100mg	$389	Buy
API0026222	5MG	$501.66	Buy

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.

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

Fruquintinib|HMPL-013 Suppliers

Global( 154)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Wuhan Jingkang en Biomedical Technology Co., Ltd	+8613720134139	orders@jknbiochem.com	China	4664	58
Zhengzhou Anbu Chem Co.,Ltd	+86-0371-88006763; +8615988602810	sales@anbuchem.com	China	3000	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32686	60
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Zhengzhou Alfa Chemical Co.,Ltd	+8618530059196	sale04@alfachem.cn	China	12770	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	28098	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58

Supplier	Advantage
Wuhan Jingkang en Biomedical Technology Co., Ltd	58
Zhengzhou Anbu Chem Co.,Ltd	58
ATK CHEMICAL COMPANY LIMITED	60
Hubei xin bonus chemical co. LTD	58
BOC Sciences	58
Zhengzhou Alfa Chemical Co.,Ltd	58
TargetMol Chemicals Inc.	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58
Dideu Industries Group Limited	58
Sinoway Industrial co., ltd.	58

The pharmacodynamics and Synthetic method of Fruquintinib
Fruquintinib, a highly potent and selective vascular endothelial growth factor (VEGFR)-1, -2, and -3 tyrosine kinase inhibitor....
Dec 28，2023

View Lastest Price from Fruquintinib|HMPL-013 manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2023-07-15	Fruquintinib\|HMPL-013 1194506-26-7	US $0.00 / KG	0.1KG	98%	1000KGS	Zhengzhou Anbu Chem Co.,Ltd
2022-10-01	Fruquintinib\|HMPL-013 1194506-26-7	US $100.00 / kg	1kg	99%	100 tons	Hebei Duling International Trade Co. LTD
2021-07-07	Fruquintinib\|HMPL-013 USP/EP/BP 1194506-26-7	US $1.10 / g	1g	99.9%	100 Tons Min	Dideu Industries Group Limited

Fruquintinib|HMPL-013
1194506-26-7
US $0.00 / KG
98%
Zhengzhou Anbu Chem Co.,Ltd

Fruquintinib|HMPL-013
1194506-26-7
US $100.00 / kg
99%
Hebei Duling International Trade Co. LTD

Fruquintinib|HMPL-013 USP/EP/BP
1194506-26-7
US $1.10 / g
99.9%
Dideu Industries Group Limited

Fruquintinib|HMPL-013 Spectrum

Fruquintinib|HMPL-013(1194506-26-7)¹HNMR

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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