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
- 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。
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靶点
PKL1
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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.
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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.
- 更新日期:2024/08/19
- 产品编号:HY-13647
- 产品名称:HMN-176
- CAS编号:
- 包装:1 mg
- 价格:380元
- 更新日期:2024/08/19
- 产品编号:HY-13647
- 产品名称:CS-2239 HMN-176
- CAS编号:173529-10-7
- 包装:5mg
- 价格:1000元
- 公司名称:MedChemexpress LLC
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- 公司名称:Cckinase, Inc.
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- 电子邮件:sales@cckinase.com
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- 公司名称:Aladdin Scientific
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- 公司名称:TargetMol Chemicals Inc.
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