CM-272 是一种可逆底物竞争性双重G9a/DNA 甲基转移酶选择性抑制剂，具有抗肿瘤活性。它抑制细胞增殖并促进细胞凋亡，诱导干扰素刺激的基因和免疫原性细胞死亡。它抑制G9a、DNMT1、DNMT3A、DNMT3B和GLP，IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

CM-272, inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death. CM-272 significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.

CM-272 (2.5 mg/kg; intravenous injection; daily; for 28 days; female Rag2?/?γc?/? mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models.Induced a statistically significant increase in overall survival (OS) in mice.

Cell Line:CEMO-1, MV4-11 and OCI-Ly10 cell lines. Concentration:125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells). Incubation Time:12 hours, 24 hours, 48 hours and 72?hours

CM-272 (2.5 mg/kg; intravenous injection; daily; for 28 days; female Rag2?/?γc?/? mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models. Animal Model:Female BALB/Ca-Rag2?/?γc?/? mice (6–8-week-old) with CEMO-1 cells. Dosage:2.5 mg/kg. Administration:Intravenous injection; daily; for 28 days

1846570-31-7

C28H38N4O3

478.637

DMSO:96 mg/mL (200.57 mM)
Ethanol:96 mg/mL (200.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years