Pelitinib

Pelitinib is a cyanoquinoline that irreversibly inhibits the EGFR receptor tyrosine kinase (IC50 = 39 nM). It inhibits HER2 with a much weaker potency (IC50 = 1.2 µM). By disrupting Akt and MAPK pathways, pelitinib can induce apoptosis and suppress the growth of tumor cell lines, displaying particularly strong efficacy against hepatocellular carcinoma cells (IC50s = ~2 µM).Formal Name: N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2E-butenamide. CAS Number: 257933-82-7. Synonyms: EKB-569. Molecular Formula: C24H23ClFN5O2. Formula Weight: 467.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20mg/mL, DMF:PBS (pH 7.2) (1:5): 0.16 mg/mL, DMSO: 10 mg/mL. lambdamax: 209, 260, 283 nm. SMILES: FC(C=C1)=C(Cl)C=C1NC2=C(C#N)C=NC3=C2C=C(NC(/C=C/CN(C)C)=O)C(OCC)=C3. InChi Code: InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+. InChi Key: WVUNYSQLFKLYNI-AATRIKPKSA-N.