Fruquintinib|HMPL-013
- 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
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 |
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4691 | 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 | 32715 | 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 | 12822 | 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 | 27644 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 | xie@china-sinoway.com | China | 992 | 58 |
Related articles
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- Dec 28,2023
View Lastest Price from Fruquintinib|HMPL-013 manufacturers
Image | 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