Icotinib

Icotinib is an inhibitor of EGFR (IC50 = 2 nM). It is selective for EGFR over Abl, Abl2, and c-Src tyrosine kinases at 1,000 nM. Icotinib inhibits EGFR-mediated tyrosine phosphorylation in A431 human epidermoid carcinoma cells with an IC50 value of 45 nM. It inhibits the growth of PC-9 and HCC827 non-small cell lung cancer (NSCLC) cells (IC50s = 50 = 8,800 nM), which do not. It also inhibits migration of HCC827 cells when used at a concentration of 100 nM and increases apoptosis by 43.7% at 10 nM. Icotinib reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 50 to 120 mg/kg per day.Formal Name: N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine. CAS Number: 610798-31-7. Synonyms: BPI 2009H. Molecular Formula: C22H21N3O4. Formula Weight: 391.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.25 mg/ml. lambdamax: 210, 212, 226, 247, 346 nm. SMILES: C#CC1=CC(NC2=NC=NC3=C2C=C4C(OCCOCCOCCO4)=C3)=CC=C1. InChi Code: 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.