分子量

478.63

储存条件

3年-20°C 粉状
2年-80°C 溶于溶剂

化学式

C28H38N4O3

CAS号

1846570-31-7

别名

N/A

化学名

4-Quinolinamine,6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-

Solubility (25°C) *

体外

DMSO

96 mg/mL (200.57 mM)

Ethanol

96 mg/mL (200.57 mM)

Water

Insoluble

体内（现配现用）

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

浓度 / 溶剂体积 / 质量

1 mg

5 mg

10 mg

1 mM

2.0893 mL

10.4465 mL

20.8930 mL

5 mM

0.4179 mL

2.0893 mL

4.1786 mL

10 mM

0.2089 mL

1.0446 mL

2.0893 mL

50 mM

0.0418 mL

0.2089 mL

0.4179 mL

产品描述

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/IC50

G9a

GLP

DNMT1

DNMT3A

DNMT3B

8 nM (IC50)

2 nM (IC50)

382 nM (IC50)

85 nM (IC50)

1200 nM (IC50)

体外研究

M-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 GI50 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

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.