YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide
YM-155
CAS: 781661-94-7
Molecular Formula: C20H19BrN4O3
YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide - Names and Identifiers
YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide - Physico-chemical Properties
| Molecular Formula | C20H19BrN4O3 |
| Molar Mass | 443.29386 |
| Melting Point | >180°C (dec.) |
| Solubility | Soluble in DMSO (up to 25 mg/ml). |
| Appearance | solid |
| Color | Tan to yellow |
| Storage Condition | -20° |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | Sepantronium bromide (YM-155) is a survivin inhibitor with an IC50 of 0.54 nM. |
| Target | Survivin |
| In vitro study | The effect of YM155 at 30 μm on SV40 is not significant either. In p53-deficient PC-3 and PPC-1 human HRPC cells, YM155 significantly suppresses endogenous survivin expression by repressing transcription from the survivin gene promoter. In contrast, there was still no inhibitory effect on the protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at YM 155 100 nM. YM155 acts on human cancer cell lines including PC-3 and PPC-1, causing apoptosis, accompanied by an increase in caspase-3 activity. YM155 potently inhibits human cancer cell lines (mutant p53 or short p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 values of 2.3 to 11 nM. In addition, μm155 enhanced the sensitivity of NSCLC cells to γ-rays. The combination of YM155 and γ-Rays enhanced the number of apoptotic cells and caspase-3 activity. YM155 Delayed repair of double strands of radiation-induced nuclear DNA breaks. |
| In vivo study | The subcutaneous injection of YM155 at 3 and 10 mg/kg showed that YM155 completely inhibited tumor growth in PC-3, but did not reduce weight or blood cell count. Pharmacokinetic analysis showed that the effect of YM155 on tumor tissue was obvious. Moreover, the tumor inhibition rate of YM155 at 5 mg/kg in PC-3 normal transplanted tumor reached 80%. The combination of YM155 and γ-rays showed strong anticancer activity in nude mice bearing H460 or Calu6 xenografts. |
YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide - Risk and Safety
| HS Code | 29339900 |
YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.256 ml | 11.279 ml | 22.559 ml |
| 5 mM | 0.451 ml | 2.256 ml | 4.512 ml |
| 10 mM | 0.226 ml | 1.128 ml | 2.256 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.451 ml |
Last Update：2024-01-02 23:10:35
YM 155 4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide - Reference Information
| biological activity | YM155 (sepantium Bromide) is an effective survivin inhibitor, by inhibiting the activity of Survivin promoter, IC50 was 0.54 nM. The inhibitory effect on SV40 promoter activity was not significant, and the inhibitory effect on the interaction between Survivin and XIAP was weak. Phase 2. YM155 (sepantrinium Bromide) is a potent inhibitor of survivin, which acts by inhibiting the activity of Survivin promoter, with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; the inhibitory effect on SV40 promoter activity was not significant, and the interaction between Survivin and XIAP was slightly inhibited. YM155 can down-regulate survivin and XIAP, regulate autophagy and induce autophagy-dependent DNA damage in breast cancer cells. Phase 2. |
| Target | Value |
| Survivin (HeLa-SURP-luc, CHO-SV40-luc cells) | 0.54 nM |
Last Update：2024-04-09 20:52:54
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CAS: 781661-94-7
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CAS: 781661-94-7
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Product Name: YM155 (Sepantronium Bromide) Visit Supplier Webpage Request for quotationCAS: 781661-94-7
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Product Name: Sepantronium Bromide Request for quotation
CAS: 781661-94-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 781661-94-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: YM155 (Sepantronium Bromide) Visit Supplier Webpage Request for quotationCAS: 781661-94-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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