化合物CM-272
| 中文名称 | 化合物CM-272 |
|---|---|
| 中文同义词 | 化合物CM-272;6-甲氧基-2-(5-甲基呋喃-2-基)-N-(1-甲基哌啶-4-基)-7-(3-(吡咯烷-1-基)丙氧基)喹啉-4-胺 |
| 英文名称 | CM-272 |
| 英文同义词 | CM-272; CM 272; CM272;CM-272;4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine;DNMT1,anti-tumour,DNMTs,immunogenic,DNA MTases,CM272,DNMT3A,CM 272,G9a,H3K9me2,Inhibitor,epigenetics,Histone Methyltransferase,GLP,Apoptosis,inhibit,substrate-competitive,CM-272,DNMT3B,DNA Methyltransferase |
| CAS号 | 1846570-31-7 |
| 分子式 | C28H38N4O3 |
| 分子量 | 478.63 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 1846570-31-7.mol |
| 结构式 |  |
化合物CM-272 性质
| 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(最大浓度 mg/mL);179.5(最大浓度 mM) 乙醇:63.0(最大浓度 mg/mL);131.63(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 10.09±0.20(Predicted) |
| 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 |
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101925 | CM-272 | 1 mg | 823元 | |
| 2024/04/30 | HY-101925 | 化合物CM-272 CM-272 | 1846570-31-7 | 5mg | 1900元 |