货号	规格	价格	上海	北京	珠海	重庆	武汉
S88520-5mg	98%	￥1598.00 S88520-5mg ￥1598.00 现货	10 0 10	-	-	-	-
S88520-10mg	98%	￥2557.00 S88520-10mg ￥2557.00 现货	10 10	-	2	-	-
S88520-25mg	98%	￥4424.00 S88520-25mg ￥4424.00 现货	6 6	-	-	-	-
S88520-50mg	98%	￥7880.00 S88520-50mg ￥7880.00 现货	4 4	-	-	-	-

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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：

G9a(Cell-free assay):8 nM;DNMT3A(Cell-free assay):85 nM;DNMT1(Cell-free assay): 382 nM;DNMT3B(Cell-free assay): 1200 nM;Apoptosis; DNAMethyltransferase; HistoneMethyltransferase

体内研究：

CM272 therapy induces a statistically significant increase in overall survival (OS) in mice in comparison with control animals. Global H3K9me2 and 5mC levels are reduced in leukaemic cells obtained from mice engrafted with ALL-derived CEMO-1 cells after 1 week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5 mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells

细胞实验：

Cell lines: ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines Concentrations: -- Incubation Time: 24, 48, 72 and 96h Method: 100.000 cells of CEMO-1, LAL-CUN-2, MV4-11 and OCI-AML-2 cell lines are cultured at a density of 1x106 cells/mL and treated for 12, 24, 48 and 72 hours with CM-272 at different concentrations (GI25, GI50 and GI75). In the case of OCI-Ly3 and OCI-Ly10, cells are treated with 100, 400 and 1000 nM for 24, 48, 72 and 96h. Cells are washed twice with phosphatebuffered saline (PBS) and resuspended in 1X Binding Buffer at a concentration of 1x106 cells/mL. 1 µL of FITC Annexin V antibody and 2 µL of propidium iodide are added and incubated for 15 min at RT in the dark. Finally, 400 µL of 1X Binding Buffer are added to each tube and analyzed by flow cytometry within 1 h.

动物实验：

Animal Models: 6–8-week-old female BALB/cA−Rag2 γc mice Dosages: 1, 2.5 mg/kg Administration: IV

参考文献：

1. San José-Enériz E, et al. Nat Commun. 2017 May 26;8:15424.

溶解性：

Soluble in DMF、Ethanol

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.089 ml	10.446 ml	20.893 ml
5 mM	0.418 ml	2.089 ml	4.179 ml
10 mM	0.209 ml	1.045 ml	2.089 ml
50 mM	0.042 ml	0.209 ml	0.418 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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