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1846570-31-7

中文名稱 化合物CM-272
英文名稱 CM-272
CAS 1846570-31-7
分子式 C28H38N4O3
分子量 478.63
MOL 文件 1846570-31-7.mol
更新日期 2025/02/05 09:52:14
1846570-31-7 結(jié)構(gòu)式 1846570-31-7 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
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]-

物理化學(xué)性質(zhì)

沸點(diǎn)631.9±55.0 °C(Predicted)
密度1.164±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
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)
酸度系數(shù)(pKa)10.09±0.20(Predicted)
形態(tài)結(jié)晶固體
顏色Light brown to brown

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
化合物CM-272價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/08HY-101925化合物CM-272
CM-272		1846570-31-71 mg823元
2025/02/08HY-101925化合物CM-272
CM-272		1846570-31-75mg1900元
2025/02/08HY-101925化合物CM-272
CM-272		1846570-31-710mM * 1mLin DMSO2001元

常見問題列表

生物活性
CM272是新型、一流的G9a (GLP) 和 DNMTs雙重可逆抑制劑，對G9a, DNMT1, DNMT3A, DNMT3B, GLP的IC50值分別為8?nM, 382 nM, 85 nM, 1200 nM, 2?nM。CM272通過至少部分誘導(dǎo)免疫原性細(xì)胞死亡，延長了血液系統(tǒng)惡性腫瘤體內(nèi)模型的存活時間。
靶點(diǎn)
TargetValue
G9a
(Cell-free assay) 		8 nM
DNMT3A
(Cell-free assay) 		85 nM
DNMT1
(Cell-free assay) 		382 nM
DNMT3B
(Cell-free assay) 		1200 nM
體外研究

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.
體內(nèi)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.
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