CS-2239

生物活性靶点体外研究体内研究 CS-2239 试剂级价格

CS-2239

CAS号:173529-10-7
英文名:HMN 176
中文名:CS-2239
CBNumber:CB42667261
分子式:C20H18N2O4S
分子量:382.43
MOL File:173529-10-7.mol

CS-2239化学性质

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 :DMSO : ≥ 30 mg/mL (78.45 mM)
酸度系数(pKa) :8.07±0.10(Predicted)
形态 :Solid
颜色 :White to off-white

CS-2239性质、用途与生产工艺

生物活性 HMN-176 是HMN-214的活性代谢物，HMN-214在小鼠异种移植瘤模型中具有有效的抗肿瘤活性。HMN-176 可通过干扰其在中心体和沿细胞骨架结构的正常亚细胞空间分布，有效地抑制 PLK-1。
靶点

PKL1
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.