YM155 (Sepantronium Bromide)

Alias: YM-155; Sepantronium bromide; YM155; YM 155
Cat No.:V0771 Purity: ≥98%
YM155 (also called Sepantronium Bromide; YM-155; YM 155) is a novel and potent survivin inhibitor with potential anticancer activity.
YM155 (Sepantronium Bromide) Chemical Structure CAS No.: 781661-94-7
Product category: Survivin
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of YM155 (Sepantronium Bromide):

  • YM-155 hydrochloride
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

YM155 (also called Sepantronium Bromide; YM-155; YM 155) is a novel and potent survivin inhibitor with potential anticancer activity. YM155 (also called Sepantronium Bromide; YM-155; YM 155) is a novel and potent survivin inhibitor with potential anticancer activity. It is a small-molecule proapoptotic agent that does not significantly inhibit SV40 promoter activity but is observed to slightly inhibit the interaction of Survivin with XIAP. In HeLa-SURP-luc and CHO-SV40-luc cells, it inhibits survivin promoter activity with an IC50 of 0.54 nM. The IAP family members and B-cell lymphoma 2 (BCL-2) related proteins are not significantly affected by YM155, despite the fact that it has a strong suppressive effect on survivin.

Biological Activity I Assay Protocols (From Reference)
Targets
Survivin (IC50 = 0.54 nM)
ln Vitro
YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. Through transcriptional inhibition of the survivin gene promoter, YM155 significantly reduces endogenous survivin expression in human HRPC cell lines PC-3 and PPC-1 that lack p53. The protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin is not sufficiently affected by YM155 at 100 nM, on the other hand. With a corresponding rise in caspase-3 activity, YM155 shows significant apoptosis in human cancer cell lines such as PC-3 and PPC-1. The human cancer cell lines PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5, and A375 are all potently inhibited by YM155 (with IC50 values ranging from 2.3 to 11 nM, respectively).[1] YM155 increases the sensitivity of NSCLC cells to γ-radiation. Caspase-3 activity and the number of apoptotic cells are both boosted by the combination of YM155 and beta-radiation. Double-strand breaks in nuclear DNA caused by radiation are postponed by YM155.[2]
ln Vivo
At doses of 3 and 10 mg/kg, YM155 completely inhibits the growth of PC-3 s.c. xenografted prostate tumors without causing weight loss or a drop in blood cell count. YM155 is widely distributed throughout tumor tissue, according to pharmacokinetic analysis. Furthermore, in PC-3 orthotopic xenografts, YM155 exhibits 80% TGI at a dose of 5 mg/kg. [1] In nude mice, the combination therapy of YM155 and -radiation exhibits strong antitumor activity against H460 or Calu6 xenografts. [2]
Enzyme 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
Cells are seeded in 96-well plates at a density of 5-40 × 103. For 48 hours, cells are given DMSO with YM155 dissolved in it. Then, using a sulforhodamine B assay, the cell count is calculated.
Animal Protocol
PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
5 mg/kg
Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump
References

[1]. Cancer Res . 2007 Sep 1;67(17):8014-21.

[2]. Clin Cancer Res . 2008 Oct 15;14(20):6496-504.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H19BRN4O3
Molecular Weight
443.29
Elemental Analysis
C, 54.19; H, 4.32; Br, 18.03; N, 12.64; O, 10.83
CAS #
781661-94-7
Appearance
White Solid powder
SMILES
CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
InChi Key
QBIYUDDJPRGKNJ-UHFFFAOYSA-M
InChi Code
InChI=1S/C20H19N4O3.BrH/c1-13-23(9-10-27-2)17-18(24(13)12-14-11-21-7-8-22-14)20(26)16-6-4-3-5-15(16)19(17)25;/h3-8,11H,9-10,12H2,1-2H3;1H/q+1;/p-1
Chemical Name
1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide
Synonyms
YM-155; Sepantronium bromide; YM155; YM 155
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~55 mg/mL (~124.1 mM)
Water: ~89 mg/mL (~200.8 mM)
Ethanol: ~6 mg/mL (~13.5 mM)
Solubility (In Vivo)
Saline: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2559 mL 11.2793 mL 22.5586 mL
5 mM 0.4512 mL 2.2559 mL 4.5117 mL
10 mM 0.2256 mL 1.1279 mL 2.2559 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05263583 Recruiting Drug: Sepantronium Bromide Burkitt Lymphoma
Lymphoma, B-Cell
Cothera Bioscience, Inc December 9, 2022 Phase 2
NCT01023386 Completed Drug: YM155 Cancer Astellas Pharma Inc November 2009 Phase 1
NCT01007292 Completed Drug: YM155
Biological: Rituximab
Non-Hodgkin's Lymphoma Novartis Pharmaceuticals November 2009 Phase 2
NCT01009775 Completed Drug: YM155
Drug: Docetaxel
Melanoma Astellas Pharma Inc November 2009 Phase 2
NCT01038804 Completed Drug: YM155
Drug: Docetaxel
Breast Cancer Astellas Pharma Inc December 2009 Phase 2
Biological Data
  • YM155 (Sepantronium Bromide)

  • YM155 (Sepantronium Bromide)

  • YM155 (Sepantronium Bromide)

Contact Us