1846570-31-7
1846570-31-7 結(jié)構(gòu)式
基本信息
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
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]-
物理化學(xué)性質(zhì)
Ethanol:63.0(Max Conc. mg/mL);131.63(Max Conc. mM)
常見問題列表
| 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. |