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173529-10-7

中文名稱(chēng) CS-2239
英文名稱(chēng) HMN 176
CAS 173529-10-7
分子式 C20H18N2O4S
分子量 382.43
MOL 文件 173529-10-7.mol
更新日期 2024/12/15 19:35:15
173529-10-7 結(jié)構(gòu)式 173529-10-7 結(jié)構(gòu)式

基本信息

中文別名
化合物HMN176
HMN-176游離態(tài)
有絲分裂抑制劑(HMN-176)
英文別名
HMN-176
HMN 176
CS-2239
HMN 176
HMN176
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
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)632.9±65.0 °C(Predicted)
密度1.24±0.1 g/cm3(Predicted)
儲(chǔ)存條件Inert atmosphere,2-8°C
溶解度DMSO : ≥ 30 mg/mL (78.45 mM)
酸度系數(shù)(pKa)8.07±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
CS-2239價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-13647CS-2239
HMN-176
173529-10-75mg620元
2024/11/08HY-13647CS-2239
HMN-176
173529-10-710mg930元
2024/11/08HY-13647CS-2239
HMN-176
173529-10-725mg1765元

常見(jiàn)問(wèn)題列表

生物活性
HMN-176 是HMN-214的活性代謝物,HMN-214在小鼠異種移植瘤模型中具有有效的抗腫瘤活性。HMN-176 可通過(guò)干擾其在中心體和沿細(xì)胞骨架結(jié)構(gòu)的正常亞細(xì)胞空間分布,有效地抑制 PLK-1。
靶點(diǎn)

PKL1

體外研究

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.

體內(nèi)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.

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