1. Apoptosis
    Autophagy
  2. Survivin
    Autophagy

YM-155 (Synonyms: Sepantronium bromide)

Cat. No.: HY-10194 Purity: >98.0%
Data Sheet SDS Handling Instructions

YM-155 is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

For research use only. We do not sell to patients.
YM-155 Chemical Structure

YM-155 Chemical Structure

CAS No. : 781661-94-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 348 In-stock
100 mg USD 492 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

YM-155 is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

IC50 & Target

IC50: 0.54 nM (survivin)

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]. In this orthotopic renal and metastatic lung tumors models, YM155 and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images[3].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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'-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3' and 5'-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3'. The resulting PCR fragment is digested with XhoI/HindIII and ligated into the XhoI/HindIII cleavage site of the pGL3-Basic vector. The resulting plasmid is named pSUR-luc. DNA sequencing is done on all amplified sequences by a DNA sequencer. The activity of pSUR-luc is confirmed by luciferase assay with transiently transfected HeLa-S3 cells. Luciferase assay is done. The pGL3 control vector, which contains the SV40 promoter and enhancer sequences, is used. HeLa cells are stably transfected with pSUR-luc and pSV2bsr by Lipofect-AMINE 2000. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named HeLa-SURP-luc. CHO cells are stably transfected with pGL3-control and pSV2bsr. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named CHO-SV40-luc. Stocked cells from the HeLa-SURP-luc and CHO-SV40-luc clones are used for chemical screening and characterization of YM155. YM155 in DMSO are added to the cells, which had been seeded the previous day on 96-well plastic plates at 5×103 per well. Luciferase activity is measured 24 hours later. IC50 is calculated by logistic analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

YM-155 is dissolved in DMSO and diluted in saline to a final DMSO concentration of ≤0.1%.

The antiproliferative activity of YM-155 is measured. After treatment with YM-155 for 48 h, the cell count is determined by sulforhodamine B assay. The GI50 value is calculated by logistic analysis, which is the drug concentration resulting in a 50% reduction in the net protein increase (as measured by sulforhodamine B staining) in control cells during the drug incubation. The assay is done in triplicate, and the mean GI50 value is obtained from the results of four independent assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

YM-155 is dissolved and diluted in saline immediately before administration.

Five-week-old male nude mice (BALB/c nu/nu) are used for the assay. PC-3 cells (2×106-3×106) are injected into the flanks of the mice and allowed to reach a tumor volume of > 100 mm3 in tumor volume (length×width2×0.5). YM-155 is s.c. administered as a 3-day continuous infusion per week for 2 weeks using an implanted micro-osmotic pump or i.v. administered five times a week for 2 weeks. The percentage of tumor growth inhibition 14 days after initial YM-155 administration is calculated for each group using the following formula: MTV=100×{1-[(MTV of the treated group on day 14)-(MTV of the treated group on day 0)]/[(MTV of the control group on day 14)-(MTV of the control group on day 0)]}, where MTV is mean tumor volume. For both the frozen tumors and plasma samples, survivin expression levels are analyzed by Western blotting and YM-155 drug concentration by high-performance liquid chromatography/triple quadrupole mass spectrometry (LC/MS/MS) using validated methods. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

443.29

Formula

C₂₀H₁₉BrN₄O₃

CAS No.

781661-94-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10.66 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
YM-155
Cat. No.:
HY-10194
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