Sepantronium Bromide (YM155)

Catalog No.S1130 Batch:S113002

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Technical Data

Formula

C20H19BrN4O3
Molecular Weight 443.29 CAS No. 781661-94-7
Solubility (25°C)* In vitro Water 89 mg/mL (200.77 mM)
DMSO 60 mg/mL (135.35 mM)
Ethanol 9 mg/mL (20.3 mM)
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
Survivin [1]
(HeLa-SURP-luc, CHO-SV40-luc cells)
0.54 nM
In vitro

YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. YM155 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 YM155 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. YM155 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] YM155 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. YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA. [2]
In vivo

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 YM155 is highly distributed to tumor tissue. Moreover, YM155 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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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
Cell Assay:

[1]
  • Cell lines

    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)

  • Concentrations

    ~ 100 nM

  • Incubation Time

    48 hours

  • Method

    Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay.
Animal Study:

[1]
  • Animal Models

    PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)

  • Dosages

    5 mg/kg

  • Administration

    Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump

Customer Product Validation

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

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

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

Data from [Proc Natl Acad Sci U S A, 2012, 109, 600-5]

Selleck's Sepantronium Bromide (YM155) has been cited by 181 publications

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
Survivin prevents the polycomb repressor complex 2 from methylating histone 3 lysine 27 [ iScience, 2023, 26(7):106976] PubMed: 37534134
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] PubMed: 35704690
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
Effects of YM155 on the proliferation and apoptosis of pulmonary artery smooth muscle cells in a rat model of high pulmonary blood flow-induced pulmonary arterial hypertension [ Clin Exp Hypertens, 2022, 44(5):470-479] PubMed: 35507763

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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