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Anlotinib

CAS No.
1360460-82-7
Chemical Name:
Anlotinib
Synonyms
Anlotinib HC;Anlotinib HCl;Anlotinib 2HCl;AL3818 DIHYDROCHLORIDE;Anlotinib HCl ( AL-3818 );Anlotinib(AL3818)dihydrochloride;Anlotinib dihydrochloride. Catequentinib;1-(((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropanamine dihydrochloride;Cyclopropanamine, 1-[[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-quinolinyl]oxy]methyl]-, hydrochloride (1:2)
CBNumber:
CB93159863
Molecular Formula:
C23H24Cl2FN3O3
Molecular Weight:
480.3593632
MDL Number:
MOL File:
1360460-82-7.mol
Last updated:2023-05-15 10:43:56

Anlotinib Properties

solubility DMSO: 48 mg/mL (99.93 mM);Ethanol: Insoluble
form Solid
color Off-White to Pale Brown
Water Solubility Water: 96 mg/mL (199.85 mM)
FDA UNII A3749M6582

Anlotinib Chemical Properties,Uses,Production

Uses

Anlotinib Dihydrochloride, is a novel inhibitor of tyrosine kinase that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRa/b, c-Kit, and Ret.

Biological Activity

Anlotinib Hydrochloride is a highly potent and selective inhibitor of VEGFR2 with IC50 of less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use normal saline for dilution, do not use PBS for dilution, which may cause precipitation.

in vitro

Anlotinib can occupy the ATP-binding domain of VEGFR tyrosine kinase, and has high selectivity and inhibitory activity for VEGFR2 compared to other tyrosine kinases (IC50<1 nM). Anlotinib inhibits VEGFR2 and VEGFR3 with IC50 of 0.2 nM and 0.7 nM, respectively. Anlotinib has low inhibitory activity against VEGFR1 with IC50 of 26.9 nM. Anlotinib inhibits PDGFR-related kinases c-Kit and PDGFRβ with IC50s of 14.8 and 115 nM, respectively. It has less activity against other kinases such as c-Met, c-Src, EGFR and HER2. Anlotinib inhibits VEGF-induced signaling and cell proliferation in HUVEC cells at picomolar concentrations. However, in vitro tumor cells require micromolar concentrations of anlotinib to directly inhibit their proliferation. Anlotinib significantly inhibited HUVEC migration and tubulogenesis, and also inhibited vascular growth in rat aortic grafts in vitro.

target

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> c-Kit
(Cell-free assay)
TargetValue
VEGFR2
(Cell-free assay)
0.2 nM
VEGFR3
(Cell-free assay)
0.7 nM
14.8 nM
c-Kit
(Cell-free assay)
14.8 nM
c-Kit
(Cell-free assay)
14.8 nM

Anlotinib Preparation Products And Raw materials

Raw materials

Preparation Products

Anlotinib HCl AL3818 DIHYDROCHLORIDE Anlotinib 2HCl Cyclopropanamine, 1-[[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-quinolinyl]oxy]methyl]-, hydrochloride (1:2) Anlotinib(AL3818)dihydrochloride Anlotinib HC Anlotinib dihydrochloride. Catequentinib Anlotinib HCl ( AL-3818 ) 1-(((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropanamine dihydrochloride 1360460-82-7