HLM006474

HLM006474 is a non-selective inhibitor of the transcription factor E2F (IC50 = 29.8 µM for E2F4). It inhibits DNA binding to E2F1, E2F2, and E2F4 in A375 melanoma cells when used at a concentration of 40 µM. HLM006474 (40 µM) decreases protein levels of E2F4 and cyclin D3 and induces apoptosis in A375 cells. It also induces apoptosis in MDA-MB-231, but not MCF-7, cells and inhibits the growth of cancer cells in a panel of 17 lung cancer cell lines (IC50s = 15.5-75.1 µM). HLM006474 reduces tumor growth in retinoblastoma-prone Chx10Cre,Rbfl/fl,p107-/- mice and in an A375 mouse xenograft model when administered at a dose of 100 mg/kg and 2 mg per mouse, respectively.Formal Name: 7-[(4-ethoxy-3-methylphenyl)(2-pyridinylamino)methyl]-2-methyl-8-quinolinol. CAS Number: 353519-63-8. Molecular Formula: C25H25N3O2. Formula Weight: 399.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 206, 250, 306 nm. SMILES: CCOC1=CC=C(C(NC2=NC=CC=C2)C3=CC=C(C=CC(C)=N4)C4=C3O)C=C1C. InChi Code: InChI=1S/C25H25N3O2/c1-4-30-21-13-11-19(15-16(21)2)23(28-22-7-5-6-14-26-22)20-12-10-18-9-8-17(3)27-24(18)25(20)29/h5-15,23,29H,4H2,1-3H3,(H,26,28). InChi Key: CYNZBLNMIJNBSF-UHFFFAOYSA-N.