CM-272|cas:1846570-31-7|西域试剂

CM-272,99.27%

产品编号：Bellancom-101925| CAS NO：1846570-31-7| 分子式：C₂₈H₃₈N₄O₃| 分子量：478.63

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101925	￥1900.00	杭州北京（现货）
Bellancom-101925	￥3325.00	杭州北京（现货）
Bellancom-101925	￥7600.00	杭州北京（现货）
Bellancom-101925	￥12160.00	杭州北京（现货）

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CM-272

产品介绍

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 dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.

体外研究

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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