1194506-26-7 Usage
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
Check Digit Verification of cas no
The CAS Registry Mumber 1194506-26-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,9,4,5,0 and 6 respectively; the second part has 2 digits, 2 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1194506-26:
(9*1)+(8*1)+(7*9)+(6*4)+(5*5)+(4*0)+(3*6)+(2*2)+(1*6)=157
157 % 10 = 7
So 1194506-26-7 is a valid CAS Registry Number.
1194506-26-7Relevant articles and documents
Synthetic method of VEGFR inhibitor furoquitinib and benzofuran intermediate thereof
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, (2021/05/01)
The invention discloses a synthetic method of a VEGFR inhibitor furoquitinib and a benzofuran intermediate thereof. The synthetic method of the VEGFR inhibitor furoquitinib comprises the following steps of S1, halogenation, S2, acylation, S3, coupling, S4
