中文名 | HMN-176 |
英文名 | HMN-176 |
别名 | 化合物HMN176 HMN-176游离态 有丝分裂抑制剂(HMN-176) |
英文别名 | HMN-176 HMN 176 HMN176 CS-2239 Benzenesulfonamide, 4-methoxy-N-[2-[(1E)-2-(1-oxido-4-pyridinyl)ethenyl]phenyl]- (NE)-N-[(6E)-6-[2-(1-hydroxypyridin-4-ylidene)ethylidene]cyclohexa-2,4-dien-1-ylidene]-4-methoxybenzenesulfonamide |
CAS | 173529-10-7 |
化学式 | C20H18N2O4S |
分子量 | 382.43 |
密度 | 1.24±0.1 g/cm3(Predicted) |
沸点 | 632.9±65.0 °C(Predicted) |
溶解度 | DMSO: ≥ 30 mg/mL |
酸度系数 | 8.07±0.10(Predicted) |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.615 ml | 13.074 ml | 26.148 ml |
5 mM | 0.523 ml | 2.615 ml | 5.23 ml |
10 mM | 0.261 ml | 1.307 ml | 2.615 ml |
5 mM | 0.052 ml | 0.261 ml | 0.523 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!