4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮
| 中文名称 | 4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮 |
|---|---|
| 中文同义词 | (2E,6E)-4-乙基-2,6-二(3-吡啶基亚甲基)环己酮;4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮;MCB-613游离态 |
| 英文名称 | MCB-613 |
| 英文同义词 | 4-ethyl-2,6-bis(pyridin-3-ylmethylene)cyclohexanone;(2E,6E)-4-Ethyl-2,6-bis(3-pyridinylmethylene)cyclohexanone;MCB-613;CS-2522;(2E,6E)-4-ethyl-2,6-bis(pyridin-3-ylmethylidene)cyclohexan-1-one;Cyclohexanone, 4-ethyl-2,6-bis(3-pyridinylmethylene)-, (2E,6E)- |
| CAS号 | 1162656-22-5 |
| 分子式 | C20H20N2O |
| 分子量 | 304.39 |
| EINECS号 | |
| 相关类别 | 合成材料中间体;标准品;API |
| Mol文件 | 1162656-22-5.mol |
| 结构式 |  |
4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮 性质
| 沸点 | 510.4±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.159±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | 不溶于水； ≥13.2 mg/mL，溶于 DMSO，温和加热； ≥9.26 mg/mL，乙醇溶液，超声波 |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.36±0.12(Predicted) |
MCB-613 是一种有效的类固醇受体共激活因子 (SRC) 小分子“刺激物” (SMS)，超刺激 SRCs 的转录活性。
MCB-613 增加了 SRC 与其他共激活因子的相互作用，并显着诱导 ER 应激与活性氧 (ROS) 的产生相结合。
MCB-613 是一种 SMS，通过过度刺激 SRC 致癌程序，靶向癌基因用作抗癌药物。MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells. MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression. MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells.
RT-PCR
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 6 μM; 8 μM |
| Incubation Time: | 24 hours |
| Result: | Increased MMP13 mRNA expression. |
Western Blot Analysis
| Cell Line: | HeLa cells |
| Concentration: | 2 μM; 4 μM; 6 μM; 8 μM; 10 μM |
| Incubation Time: | 24 hours |
| Result: | Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression. |
Cell Viability Assay
| Cell Line: | SRC-3 KO and WT HeLa cells |
| Concentration: | 3 μM; 4 μM; 5 μM; 6 μM; 7 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased SRC-3 KO and WT HeLa cell viability. |
MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity
| Animal Model: | MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads) |
| Dosage: | 20 mg/kg |
| Administration: | Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks |
| Result: | Inhibited tumor growth in vivo. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19625 | MCB-613 | 1 mg | 500元 | |
| 2024/01/25 | HY-19625 | 4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮 MCB-613 | 1162656-22-5 | 5mg | 1100元 |