CM-272

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CM-272

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1846570-31-7

CM-272 是一种首创的，有效的，选择性的，底物竞争性的且可逆的双重G9a/DNA 甲基转移酶 (DNMTs) 抑制剂。CM-272 具有抗肿瘤活性。CM-272 抑制G9a，DNMT1，DNMT3A，DNMT3B和GLP，IC₅₀分别为 8 nM，382 nM，85 nM，1200 nM 和 2 nM。CM-272 抑制细胞增殖并促进细胞凋亡，诱导干扰素刺激的基因和免疫原性细胞死亡。

生物活性

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dualG9a/DNA methyltransferases (DNMTs)inhibitor with antitumor activities. CM-272 inhibitsG9a,DNMT1,DNMT3A,DNMT3BandGLPwithIC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotesapoptosis, inducing IFN-stimulated genes and immunogenic cell death^[1].

IC₅₀& Target^[1]

G9a

8 nM (IC₅₀)

DNMT1

382 nM (IC₅₀)

DNMT3A

85 nM (IC₅₀)

DNMT3B

1200 nM (IC₅₀)

体外研究
(In Vitro)

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^[1].
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression^[1].
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^[1].
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 GI₅₀values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC^[1].
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^[1].

Cell Proliferation Assay^[1]

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^[1]

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^[1]

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.

体内研究
(In Vivo)

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^[1].

Animal Model:	Female BALB/Ca-Rag2^–/–γc^–/–mice (6–8-week-old) with CEMO-1 cells^[1]
Dosage:	2.5 mg/kg
Administration:	Intravenous injection; daily; for 28 days
Result:	Induced a statistically significant increase in overall survival (OS) in mice.

分子量

478.63

性状

Solid

Formula

C₂₈H₃₈N₄O₃

CAS 号

1846570-31-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL(261.16 mM;Need ultrasonic)

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在本网站选购。