Sepantronium bromide

Sepantronium bromide (YM-155) is a novel, highly selective Survivin inhibitor with good water solubility, exhibiting pro-apoptotic effects and antitumor activity. Sepantronium bromide is a Survivin inhibitor with an IC50 of 0.54 nM.

Survivin:0.54 nM

Methods: MM cell line RPMI8226 cells and NK cells were treated with gradient concentrations of Sepantronium bromide (0.1, 1, 2.5, 5, 10, 25, 50 nM) for 18 hours, followed by flow cytometric analysis for cytotoxicity.
Results: For MM cells, 2.5 nM and 5 nM Sepantronium bromide exhibited strong cytotoxicity, while these concentrations were non-toxic to NK cells. [1]
Methods: H9C2 rat cardiomyocytes were cultured with normal glucose (5.5 mM) (control group), high glucose (33 mM) (model group), and YAP1 overexpression ± HG ± Sepantronium bromide (1 μM) (intervention group) for 48 hours. Apoptosis rates were assessed via Hoechst 33342 staining.
Results: High glucose (HG) induced increased cardiomyocyte apoptosis. YAP1 overexpression significantly reduced HG-induced apoptosis. Co-treatment with Sepantronium bromide partially inhibited the anti-apoptotic effect of YAP1 overexpression, leading to a rebound in apoptosis rates. [2]

Methods: RAG2⁻/⁻γc⁻/⁻ mice received subcutaneous implantation of ceramic scaffolds loaded with human BMSCs, followed by loading with luciferase-labeled UM9 MM cells to establish a humanized bone marrow microenvironment. After successful establishment, continuous subcutaneous infusion of Sepantronium bromide (1 mg/kg/day for 10 days) via a subcutaneous osmotic pump, intraperitoneal injection of Daratumumab (8 mg/kg, twice weekly for 5 weeks), or combined administration of both drugs. Monitoring continued until day 63 post-treatment initiation.
Results: The combination therapy group effectively controlled tumor growth throughout the entire experimental period (63 days), exhibiting significantly smaller tumor volumes compared to both the Sepantronium bromide monotherapy and Daratumumab monotherapy groups. [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

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. (Only for Reference)

H2O: 82 mg/mL (184.99 mM), Sonication is recommended.

Ethanol: 6 mg/mL (13.54 mM), Sonication is recommended.

DMSO: 48 mg/mL (108.29 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.26 mM), Sonication is recommended.

10% DMSO+90% Saline: 4.8 mg/mL (10.83 mM), Solution.