CS-2239
| 中文名称 | CS-2239 |
|---|---|
| 中文同义词 | 有丝分裂抑制剂(HMN-176);HMN-176游离态;化合物HMN176;(E)-4-(2-((4-甲氧基苯基)磺酰胺)苯乙烯基)吡啶 1-氧化物 |
| 英文名称 | HMN 176 |
| 英文同义词 | HMN 176;HMN-176;(NE)-N-[(6E)-6-[2-(1-hydroxypyridin-4-ylidene)ethylidene]cyclohexa-2,4-dien-1-ylidene]-4-methoxybenzenesulfonamide;CS-2239;HMN 176; HMN176;Benzenesulfonamide, 4-methoxy-N-[2-[(1E)-2-(1-oxido-4-pyridinyl)ethenyl]phenyl]-;Polo-like Kinase (PLK),HMN-176,HMN176,HMN 176,Inhibitor,inhibit;(E)-4-(2-((4-Methoxyphenyl)sulfonamido)styryl)pyridine 1-oxide |
| CAS号 | 173529-10-7 |
| 分子式 | C20H18N2O4S |
| 分子量 | 382.43 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;API |
| Mol文件 | 173529-10-7.mol |
| 结构式 |  |
CS-2239 性质
| 沸点 | 632.9±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.24±0.1 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 溶解度 | 二甲基亚砜：≥30mg/mL（78.45 mM） |
| 酸度系数(pKa) | 8.07±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
PKL1
HMN-176 (2.5 μM) greatly increases the duration of mitosis in hTERT-RPE1 and CFPAC-1 Cell lines. The effect of HMN-176 on spindle morphology does not appear to be related to effects on microtubule polymerization. HMN-176 (2.5, 0.25, and 0.025 μM) inhibits aster formation in a concentration dependent manner. HMN-176 (0.1, 1.0, or 10.0 µg/mL) demonstrates inhibitory effects in multiple tumors, with notable activity seen in breast, nonsmall-cell lung, and ovarian cancer specimens. HMN-176 demonstrates activity towards 63% of the breast (5/8), 67% of the non-small cell lung (4/6), and 57% of the ovarian (4/7) tumor specimens treated with 10.0 µg/mL. HMN-176 shows potent cytotoxicity, with a mean IC 50 value of 118 nM. HMN-176 displays similar cytotoxicity against tumors with various characteristics from different organs. Treatment with 3 μM HMN-176 suppresses the expression of MDR1 mRNA by 56%. HMN-176 has no significant effect on the residual promoter activity.
HMN-176 prevents spindle assembly and meiosis in Spisula oocytes by inhibiting centrosome-dependent MT nucleation, i.e., aster formation. Oocytes treated with 0.25 μM HMN-176 undergoes GVBD, but asters or spindles fails to form, even after prolonged periods. After p.o. of HMN-214 to male rats, the prodrug is not detected in the plasma, while plasma levels of HMN-176 peaks at 2 h and gradually decreases thereafter.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-13647 | HMN-176 | 1 mg | 380元 | |
| 2024/04/30 | HY-13647 | CS-2239 HMN-176 | 173529-10-7 | 5mg | 1000元 |