781661-94-7

Basic information

• Product Name: YM155
• Synonyms: YM155;4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide;SepantroniuM broMide;SepantroniuM broMide(YM155,YM-155);YM155 (SepantroniuM BroMide);Sepantronium Bromide (YM155);1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-, bromide (1:1);4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide YM 155
• CAS NO: 781661-94-7
• Molecular Formula: C20H19BrN4O3
• Molecular Weight: 443.29386
• EINECS: -0
• Product Categories: apis;Inhibitor;Antineoplastic;Inhibitors
• Mol File: 781661-94-7.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Storage Temp.: -20°
• Solubility: Soluble in DMSO (up to 25 mg/ml).
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• CAS DataBase Reference: YM155(CAS DataBase Reference)
• NIST Chemistry Reference: YM155(781661-94-7)
• EPA Substance Registry System: YM155(781661-94-7)

Safety Data

• Hazardous Substances Data: 781661-94-7(Hazardous Substances Data)

Usage

Description

YM155 is a novel small molecule survivin suppressant that selectively targets and inhibits the expression of survivin, a member of the inhibitor of apoptosis proteins (IAP) family. It has the ability to induce apoptosis in human tumor cell lines at low concentrations and has shown potential in overcoming drug resistance and inducing DNA damage in certain cancer types.

Uses

Used in Oncology:
YM155 is used as a potent IAP inhibitor for survivin with an IC50 of 0.54 nM. It is particularly effective in suppressing the expression of survivin and inducing apoptosis in PC-3 and PPC-1 human hormone-refractory prostate cancer (HRPC) cell lines. This makes YM155 a promising candidate for the development of anticancer therapies targeting survivin-dependent tumors.
Used in Overcoming Drug Resistance:
YM155 has demonstrated the ability to overcome erlotinib resistance in EGFR mutation-positive non-small cell lung cancer (NSCLC). This suggests that YM155 could be a valuable component in combination therapies to enhance the effectiveness of existing treatments and overcome resistance in lung cancer patients.
Used in Inducing DNA Damage and Autophagy-Dependent Cell Death:
YM155 has been shown to induce DNA damage and autophagy-dependent cell death in certain cancer cell lines, such as adenoid cystic carcinoma cells. This highlights its potential in targeting cancer cells through multiple mechanisms, increasing the chances of effective treatment and reducing the likelihood of resistance development.

References

1) Nakahara?et al. (2007),?YM155, a novel small-molecule surviving suppressant, induces regression of established human hormone-refractory prostate tumor xenografts; Cancer Res.?67?8014 2) Okamoto?et al. (2012),?Overcoming erlotinib resistance in EGFR mutation-positive non-small cell lung cancer cells by targeting survivin; Mol.Cancer Ther.?11?204 3) Glaros?et al. (2012),?The ‘survivin suppressants’ NSC 80467 and YM 155 induce a DNA damage response; Cancer Chemother. Pharmacol.?70?207 4) Wang?et al. (2014),?Induction of autophagy-dependent cell death by the survivin suppressant YM155 in salivary adenoid cystic carcinoma; Apoptosis?19?748

Upstream product

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Relevant articles and documents

BROMIDE AND ITS CRYSTAL

The 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide of the invention and its crystals, particularly α- and β-form Crystals, have no hygroscopic property, have excellent stability and therefore are useful as production materials of medicines. Particularly, the β-form Crystal is most stable and markedly useful as a bulk for medicines.