化合物CM-272
- CAS号:1846570-31-7
- 英文名:CM-272
- 中文名:化合物CM-272
- CBNumber:CB14632529
- 分子式:C28H38N4O3
- 分子量:478.63
- MOL File:1846570-31-7.mol
- 沸点 :631.9±55.0 °C(Predicted)
- 密度 :1.164±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:84.0(Max Conc. mg/mL);179.5(Max Conc. mM)
Ethanol:63.0(Max Conc. mg/mL);131.63(Max Conc. mM) - 形态 :A crystalline solid
- 酸度系数(pKa) :10.09±0.20(Predicted)
- 颜色 :Light brown to brown
化合物CM-272性质、用途与生产工艺
- 生物活性 CM272是新型、一流的G9a (GLP) 和 DNMTs双重可逆抑制剂，对G9a, DNMT1, DNMT3A, DNMT3B, GLP的IC50值分别为8 nM, 382 nM, 85 nM, 1200 nM, 2 nM。CM272通过至少部分诱导免疫原性细胞死亡，延长了血液系统恶性肿瘤体内模型的存活时间。
-
靶点
Target Value G9a
(Cell-free assay)8 nM DNMT3A
(Cell-free assay)85 nM DNMT1
(Cell-free assay)382 nM DNMT3B
(Cell-free assay)1200 nM -
体外研究
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment inhibits cell proliferation in a dose- and time-dependent manner.
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression.
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment induces apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.
CM-272 after 48 h of treatment CEMO-1 acute lymphoblastic leukaemia (ALL) cell line, MV4-11 acute myeloid leukaemia (AML) cell line and OCI-Ly10 diffuse large B-cell lymphoma (DLBCL) cell line, the GI 50 values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC.
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumour cells, potentially leading to the induction of cell autonomous immunogenic death in tumour cells.Cell Proliferation Assay
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 Result: Inhibited cell proliferation in a dose- and time-dependent manner. Cell Cycle Analysis
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: 24 hours Result: Blocked cell cycle progression. Apoptosis Analysis
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 Result: Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner. -
体内研究
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 Result: Induced a statistically significant increase in overall survival (OS) in mice.
- 更新日期：2024/11/08
- 产品编号：HY-101925
- 产品名称：CM-272
- CAS编号：
- 包装：1 mg
- 价格：823元
- 更新日期：2024/11/08
- 产品编号：HY-101925
- 产品名称：化合物CM-272 CM-272
- CAS编号：1846570-31-7
- 包装：5mg
- 价格：1900元
- 公司名称：InvivoChem
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