Icotinib, Catalog: B3003

Alternate Names BPI-2009; BPI-2009H; N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine; Conmana; (3-Ethynyl-phenyl)(7,8,10,11,13,14-hexahydro-6,9,12,15-tetraoxa-1,3-diazacyclododeca[b]naphthalen-4-yl)-amine; N-(3-ethynylphenyl)-2,5,8,11-tetraoxa-15,17-diazatricyclo[10.8.0.014,19]icosa-1(12),13,15,17,19-pentaen-18-amine

Appearance Solid

CAS # 610798-31-7

Molecular Formula C₂₂H₂₁N₃O₄

Molecular Weight 391.4

Purity >99%

Solubility ~75 mg/ml in DMSO

SMILES C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4

InChi InChI=1S/C22H21N3O4/c1-2-16-4-3-5-17(12-16)25-22-18-13-20-21(14-19(18)23-15-24-22)29-11-9-27-7-6-26-8-10-28-20/h1,3-5,12-15H,6-11H2,(H,23,24,25)

InChi Key QQLKULDARVNMAL-UHFFFAOYSA-N

PubChem CID 22024915

MDL Number MFCD22124501

Storage Conditions -20ºC

Shipping Conditions RT

USAGE For Research Use Only! Not For Use in Humans.

Handling Do not take it internally. Wear a glove and mask when handling the product. Protect from air and moisture.

Icotinib is a potent epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC₅₀ of 5 nM. It blocks EGFR-mediated intracellular tyrosine phosphorylation with an IC₅₀ of 45 nM in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. Icotinib shows potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment.