Sepantronium Bromide (YM155)

製品コードS1130 バッチS113005

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H19BrN4O3
分子量 443.29 CAS No. 781661-94-7
Solubility (25°C)* 体外 Water 89 mg/mL (200.77 mM)
DMSO 55 mg/mL (124.07 mM)
Ethanol 6 mg/mL (13.53 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
in vitro

Sepantronium Bromide (YM155) is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. It significantly inhibits endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 through transcriptional inhibition of the survivin gene promoter. On the contrary this compound shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. YM155 indicates great apoptosis in human cancer cell lines including PC-3 and PPC-1 with a concomitant increase in caspase-3 activity. It potently inhibits human cancer cell lines (mutated or truncated p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 from 2.3 to 11 nM, respectively. [1] This compound increases the sensitivity of NSCLC cells to γ-radiation. The combination of YM155 and γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. It delays the repair of radiation-induced double-strand breaks in nuclear DNA. [2]
in vivo

Sepantronium Bromide (YM155) completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that it is highly distributed to tumor tissue. Moreover, this compound shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. [1] The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Promoter-luciferase reporter assay
A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5
細胞アッセイ 細胞株 Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375)
濃度 ~ 100 nM
反応時間 48 hours
実験の流れ

Sepantronium Bromide (YM155) is dissolved in DMSO and added to cells for 48 hours. Cells are seeded in 96-well plates at a density of 5-40 × 103. Then the cell count is determined by sulforhodamine B assay.
動物実験 動物モデル PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
投薬量 5 mg/kg
投与方法 Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump

参考

  • https://pubmed.ncbi.nlm.nih.gov/17804712/
  • https://pubmed.ncbi.nlm.nih.gov/18927289/

カスタマーフィードバック

Data from [Clin Cancer Res, 2013, 19, 5591-601]

Data from [Leukemia, 2012, 26, 623-632]

Data from [Leukemia, 2012, 26, 623-632]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
Single-cell RNA sequencing and machine learning provide candidate drugs against drug-tolerant persister cells in colorectal cancer [ Biochim Biophys Acta Mol Basis Dis, 2025, 1871(3):167693] PubMed: 39870146
High-Throughput Drug Screening of Clear Cell Ovarian Cancer Organoids Reveals Vulnerability to Proteasome Inhibitors and Dinaciclib and Identifies AGR2 as a Therapeutic Target [ Cancer Res Commun, 2025, 5(6):1018-1033] PubMed: 40459063
Bivalent chromatin accommodates survivin and BRG1/SWI complex to activate DNA damage response in CD4+ cells [ Cell Commun Signal, 2024, 22(1):440] PubMed: 39261837
A high-throughput approach to identify BRCA1-downregulating compounds to enhance PARP inhibitor sensitivity [ iScience, 2024, 27(7):110180] PubMed: 38993666
Exploring effective biomarkers and potential immune related gene in small cell lung cancer [ Sci Rep, 2024, 14(1):7604] PubMed: 38556560
TP53RK Drives the Progression of Chronic Kidney Disease by Phosphorylating Birc5 [ Adv Sci (Weinh), 2023, 10(25):e2301753] PubMed: 37382161
Fusion-negative rhabdomyosarcoma 3D organoids to predict effective drug combinations: A proof-of-concept on cell death inducers [ Cell Rep Med, 2023, 4(12):101339] PubMed: 38118405
CBX5 loss drives EGFR inhibitor resistance and results in therapeutically actionable vulnerabilities in lung cancer [ Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120] PubMed: 36652476
FAP is critical for ovarian cancer cell survival by sustaining NF-κB activation through recruitment of PRKDC in lipid rafts [ Cancer Gene Ther, 2023, 30(4):608-621] PubMed: 36494579

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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