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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.
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
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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.

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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Fruquintinib|HMPL-013 Suppliers

Wuhan Jingkangen Biomedical Technology Co., Ltd
Tel
13720134139 13720134139
Email
orders@jknbiochem.com
Country
China
ProdList
5792
Advantage
58
Jinan Cen Ben Medical Technology Co., Ltd
Tel
14793566
Email
info@cenpharm.com
Country
China
ProdList
696
Advantage
58
Shandong utilizing biological technology co., LTD
Tel
15966937598
Fax
3407640895 3071519937
Email
3407650895@qq.com
Country
China
ProdList
1161
Advantage
58
Mancinor Technology Co., Ltd.
Tel
19719236623
Email
2885515945@qq.com
Country
China
ProdList
1461
Advantage
58
Chunchuang (Wuhan) Technology Co., Ltd
Tel
15342225168
Email
yutianchun2007@126.com
Country
China
ProdList
9999
Advantage
58
Jinan Demai Medical Technology Co., LTD
Tel
18669728830
Email
865681093@qq.com
Country
China
ProdList
523
Advantage
58
Nanjing Pope Bio-tech R&D Co., Ltd
Tel
025-87138562 18951783565
Email
sales@popebiotech.com
Country
China
ProdList
1112
Advantage
58
Anqing CHICO Pharmaceutical Co., Ltd.
Tel
18061456370 18951649510
Fax
+86-25-52261140
Email
sales@chicopharm.com
Country
China
ProdList
443
Advantage
65
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
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View Lastest Price from Fruquintinib|HMPL-013 manufacturers

Jinan Jianfeng Chemical Co., Ltd
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
Apeloa production Co.,Limited
Product
Fruquintinib 1194506-26-7
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
23000
Release date
2024-06-18
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
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

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


  • 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
  • API