Fruquintinib

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.Formal Name: 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide. CAS Number: 1194506-26-7. Synonyms: HMPL-013. Molecular Formula: C21H19N3O5. Formula Weight: 393.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5mg/mL, DMF:PBS (pH 7.2) (1:3): 0.25mg/mL, DMSO: 2mg/mL. lambdamax: 237 nm. SMILES: COC(C(OC)=C1)=CC2=C1N=CN=C2OC3=CC(OC(C)=C4C(NC)=O)=C4C=C3. InChi Code: 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). InChi Key: BALLNEJQLSTPIO-UHFFFAOYSA-N.