CM-272

CM-272 is a reversible inhibitor of the histone methyltransferases G9a and GLP, as well as DNA methyltransferase 1 (DNMT1), DNMT3A, and DNMT3B (IC50s = 8, 2, 382, 85, and 1,200 nM, respectively). It inhibits the growth of, and induces apoptosis in, CEMO-1, MV4-11, and OCI-LY10 cancer cells (GI50s = 218, 269, and 455 nM, respectively). It also induces the expression of IFN-stimulated genes, as well as increases the expression of calreticulin and secretion of high-mobility group protein B1 (HMGB1), markers of immunogenic cell death, in the same cells. CM-272 (2.5 mg/kg) reduces tumor growth in MV4-11 acute myeloid leukemia (AML) and EGI-1 cholangiocarcinoma mouse xenograft models. It increases survival in CEMO-1 acute lymphocytic leukemia (ALL) and RT112 bladder cancer mouse xenograft models when administered at doses of 2.5 and 5 mg/kg, respectively.Formal Name: 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-4-quinolinamine. CAS Number: 1846570-31-7. Molecular Formula: C28H38N4O3. Formula Weight: 478.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:6): 0.15 mg/ml. lambdamax: 223, 246, 284, 295, 336, 350 nm. SMILES: COC1=C(OCCCN2CCCC2)C=C(N=C(C3=CC=C(C)O3)C=C4NC5CCN(C)CC5)C4=C1. InChi Code: InChI=1S/C28H38N4O3/c1-20-7-8-26(35-20)25-18-23(29-21-9-14-31(2)15-10-21)22-17-27(33-3)28(19-24(22)30-25)34-16-6-13-32-11-4-5-12-32/h7-8,17-19,21H,4-6,9-16H2,1-3H3,(H,29,30). InChi Key: RLQLKZTYUYIWDB-UHFFFAOYSA-N.