Formulation: A crystalline solid
Formal Name: 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-4-quinolinamine
Purity: ≥95%
Formula Markup: C28H38N4O3
Formula Weight: 478,6
Shelf life (days): 1460
CAS Number: 1846570-31-7
Notes: 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).{58366} 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.{44006,58376} 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.{58366,58377}
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