| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C422261-1ml |
1ml |
现货  |
|
| 英文别名 | 4-Quinolinamine,6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | CM272 |
| 生化机理 | CM-272 是一种新型的 G9a (GLP) 和 DNMT 双向可逆抑制剂，对 G9a、DNMT1、DNMT3A、DNMT3B 和 GLP 的 IC50 分别为 8u2009nM、382 nM、85 nM、1200 nM 和 2u2009nM。CM-272 至少通过部分诱导免疫原性细胞死亡，延长了血液恶性肿瘤体内模型的存活时间。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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。 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 GI50 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 |
| ALogP | 4.052 |
|---|---|
| hba_count | 4 |
| HBD Count | 1 |
| Rotatable Bond | 9 |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 6-methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine |
| INCHI | InChI=1S/C28H38N4O3/c1-20-7-8-26(35-20)25-18-23(29-21-9-14-31(2)15-10-21)22-17-27(33-3)28(19-24(22)30-25)34-16-6-13-32-11-4-5-12-32/h7-8,17-19,21H,4-6,9-16H2,1-3H3,(H,29,30) |
| InChi Key | RLQLKZTYUYIWDB-UHFFFAOYSA-N |
| Canonical SMILES | CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5 |
| Isomeric SMILES | CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5 |
| 分子量 | 478.63 |
| Reaxy-Rn | 29379266 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29379266&ln= |
| DMSO(mg / mL) Max Solubility | 96 |
|---|---|
| DMSO(mM) Max Solubility | 200.572467250277 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 478.600 g/mol |
| XLogP3 | 4.800 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 9 |
| 精确质量Exact Mass | 478.294 Da |
| 单同位素质量Monoisotopic Mass | 478.294 Da |
| 拓扑极表面积Topological Polar Surface Area | 63.000 Ų |
| 重原子数Heavy Atom Count | 35 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 640.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
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 |
| 预防措施声明 |
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。 |
| Reaxy-Rn | 29379266 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29379266&ln= |
| Appearance(yellow liquid) | Pass |
|---|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
| Record the entire process by video | Conform |
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