化合物CM-272
|
|
|
- CAS号:
- 1846570-31-7
- 英文名:
- CM-272
- 英文别名:
- CM-272;CM-272; CM 272; CM272;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine;4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-;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
- 中文名:
- 化合物CM-272
- 中文别名:
- 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
- CBNumber:
- CB14632529
- 分子式:
- C28H38N4O3
- 分子量:
- 478.63
- MOL File:
- 1846570-31-7.mol
|
|
|
化合物CM-272化学性质
-
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(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)
-
|
化合物CM-272性质、用途与生产工艺
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。
| 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.
|
化合物CM-272
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
1846570-31-7, 化合物CM-272 相关搜索:
- 药靶配体
- 抑制剂
- 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
- 化合物CM-272
- 1846570-31-7
- 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
- 6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine
- 4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-
- CM-272
- CM-272; CM 272; CM272