化合物CM-272 T7194

Product Introduction
Bioactivity


英文名: CM-272

描述: CM-272 是一种可逆底物竞争性双重G9a/DNA 甲基转移酶选择性抑制剂，具有抗肿瘤活性。它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。它抑制G9a、DNMT1、DNMT3A、DNMT3B 和GLP，IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。

细胞实验: 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

动物实验: 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

体外活性: CM-272, inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death. CM-272 significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.

体内活性: 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.Induced a statistically significant increase in overall survival (OS) in mice.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 96 mg/mL (200.57 mM)
Ethanol : 96 mg/mL (200.57 mM)


关键字: DNMT1 | anti-tumour | DNMTs | immunogenic | DNA MTases | CM-272 | DNMT3A | G9a | H3K9me2 | Inhibitor | epigenetics | Histone Methyltransferase | GLP | Apoptosis | inhibit | substrate-competitive | DNMT3B | CM272 | DNA Methyltransferase | CM 272

相关产品: Y-27632 | Lomustine | BK60106 | Lacidipine | Polyphyllin II | Meclizine dihydrochloride | UC-514321 | Obacunone | Cabozantinib S-malate | Fosbretabulin Disodium

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Stem Cell Differentiation Compound Library | Methylation Compound Library | Chromatin Modification Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途