(E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide
HMN-214
CAS: 173529-46-9
Molecular Formula: C22H20N2O5S
(E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide - Names and Identifiers
(E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide - Physico-chemical Properties
| Molecular Formula | C22H20N2O5S |
| Molar Mass | 424.47 |
| Density | 1.24 |
| Boling Point | 663.1±65.0 °C(Predicted) |
| pKa | 0.86±0.10(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| In vitro study | HMN-214 is an oral prodrug that can be rapidly converted to HMN-176. And HMN-214 in vitro experimental data are very few. However, HMN-176 is the active metabolic form of HMN-214, has a broad spectrum of anticancer activity, and effectively acts on a variety of cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, the mean IC50 was 118 nM. HMN-176 toxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with an IC50 of 143 nM-265 nM. 3 M HMN-176 in HeLa cells, the cell cycle was stopped at G2/M phase. HMN-176 inhibited cell growth with an IC50 of 2 μm in anti-adrenamycin K2/ARS cells. 3 M HMN-176 down-regulates the expression of the multidrug resistance gene (MDR1) because NF-Y transcription factor binding to the MDR1 promoter is disturbed. 2.5 M HMN-176 acts on human RPE1 and CFPAC-1 cells to delay the formation of the appropriate spindle assembly checkpoint. 250 nM-2.5 μm HMN-176 inhibited meiotic spindle assembly. 2.5 μm HMN-176 also inhibited human centrosome microtubule formation. These results indicate that HMN-176 exerts anticancer activity by interfering with centrosome-regulated MT assembly during mitosis. |
| In vivo study | HMN-214 is HMN-176 of the oral drug precursor, with high oral absorption. Therefore, for in vivo experiments, HMN-214 was used instead of HMN-176. HMN-214 at a dose of 30 mg/kg treatment of mice, will not cause significant neurotoxicity. HMN-214 inhibits tumor growth in mice bearing PC-3, A549, and WiDr xenografts at doses ranging from 10 mg/kg to 20 mg/kg. HMN-214 at the dose of 10 mg/kg-20 mg/kg, the expression of MDR1 mRNA was significantly inhibited in the nude mouse model carrying multiple drug resistant KB-A.1 cells. |
(E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.356 ml | 11.779 ml | 23.558 ml |
| 5 mM | 0.471 ml | 2.356 ml | 4.712 ml |
| 10 mM | 0.236 ml | 1.178 ml | 2.356 ml |
| 5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
Last Update：2024-01-02 23:10:35
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Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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