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5mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
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.
Targets |
Survivin (IC50 = 0.54 nM)
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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]
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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]
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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
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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.
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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 |
Molecular Formula |
C20H19BRN4O3
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Molecular Weight |
443.29
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Elemental Analysis |
C, 54.19; H, 4.32; Br, 18.03; N, 12.64; O, 10.83
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CAS # |
781661-94-7
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Related CAS # |
Sepantronium hydrochloride;355406-09-6
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Appearance |
White Solid powder
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SMILES |
CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
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InChi Key |
QBIYUDDJPRGKNJ-UHFFFAOYSA-M
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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
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Chemical Name |
1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide
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Synonyms |
YM-155; Sepantronium bromide; YM155; YM 155
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (4.51 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: Saline: 30mg/mL . Solubility in Formulation 4: 50 mg/mL (112.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
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.
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.
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 |
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