Anlotinib (hydrochloride)

Anlotinib is an orally bioavailable tyrosine kinase inhibitor that inhibits human VEGFR1, VEGFR2, VEGFR3, PDGFRbeta, and c-Kit (IC50s = 26.9, 0.2, 0.7, 115, and 14.8 nM, respectively). It is selective for these kinases over c-Met, c-Src, HER2, and EGFR (IC50s = >2,000 nM). It also inhibits FGFR1 (IC50 = 11.7 nM for the human receptor). Anlotinib inhibits the growth of SW620 and HT-29 colorectal, 786-O and Caki-1 renal, A549 and NCI H526 lung, MDA-MB-231 breast, HMC-1 leukemia, A375 melanoma, and U-87 MG glioblastoma cancer cells (IC50s = 3-12.5 µM). It inhibits VEGF-induced migration (IC50 = 0.1 nM) and FBS-induced tube formation in human umbilical vein endothelial cells (HUVECs). Anlotinib (1.5 nmol) inhibits VEGF-induced angiogenesis in a chicken chorioallantoic membrane (CAM) assay. It also decreases tumor volume by 83% and tumor angiogenesis by 91.2% in a SW620 xenograft mouse model when administered at a dose of 3 mg/kg per day.Formal Name: 1-[[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-quinolinyl]oxy]methyl]-cyclopropanamine, monohydrochloride. CAS Number: 1058157-76-8. Molecular Formula: C23H22FN3O3 . HCl. Formula Weight: 443.9. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 0.5 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 233, 321 nm. SMILES: COC1=C(OCC2(N)CC2)C=C3C(C(OC4=C(F)C5=C(NC(C)=C5)C=C4)=CC=N3)=C1.Cl. InChi Code: InChI=1S/C23H22FN3O3.ClH/c1-13-9-15-16(27-13)3-4-19(22(15)24)30-18-5-8-26-17-11-21(20(28-2)10-14(17)18)29-12-23(25)6-7-23,/h3-5,8-11,27H,6-7,12,25H2,1-2H3,1H. InChi Key: GTAUHBAHFJIAQT-UHFFFAOYSA-N.