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。 Information CM272 CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a , DNMT1 , DNMT3A , DNMT3B , GLP , respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death. Targets G9a (Cell-free assay); DNMT3A (Cell-free assay); DNMT1 (Cell-free assay); DNMT3B (Cell-free assay) 8 nM ;85 nM; 382 nM; 1200 nM In vitro The GI 50 for CM-272 after 48\u2009h of treatment in ALL, AML and DLBCL-derived cell lines is in the nM range and is associated with a decrease in global levels of H3K9me2 and 5mC. CM-272 inhibits cell proliferation, blocks cell cycle progression and induces apoptosis in ALL, AML and DLBCL cell lines in a dose-dependent manner. CM-272 induces IFN response and immunogenic cell death.. In vivo 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\u2009week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5\u2009mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells.. Cell Research(from reference) Cell lines：ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines Incubation Time：24, 48, 72 and 96h
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CM272
Dangerous GoodsCAS number：1846570-31-7 molecular formula：C28H38N4O3
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 4-Quinolinamine,6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]- | ||
| CAS number | 1846570-31-7 | molecular formula | C28H38N4O3 |
| molecular weight | 478.63 g/mol | Exact mass | 10mM in DMSO |
| PSA | 63.000 Ų | logp | 4.052 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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MSDS
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