A VEGFR inhibitor (IC50s = 33

Fruquintinib – 100 mg

Brand:
Cayman
CAS:
1194506-26-7
Storage:
-20
UN-No:
Non-Hazardous - /

Fruquintinib is a VEGFR inhibitor (IC50s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively).{46672} 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.  

 

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SKU: 29425 - 100 mg Category:

Description

A VEGFR inhibitor (IC50s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively); inhibits RET, FGFR1, and c-Kit (IC50s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases; inhibits VEGF-A- induced proliferation of HUVECs and VEGF-C-induced proliferation of HLECs (IC50s = 1.7 and 4.2 nM, respectively); decreases tube formation by HUVECs by 74 and 94% at 30 and 300 nM, respectively; reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models at 0.5-20 mg/kg per day for 21 days

Formal name: 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide

Synonyms:  HMPL-013

Molecular weight: 393.4

CAS: 1194506-26-7

Purity: ≥98%

Formulation: A solid

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