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Chemical Structure| 781661-94-7 Chemical Structure| 781661-94-7
Chemical Structure| 781661-94-7

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CAS No.: 781661-94-7

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YM155 is an inhibitor of survivin with IC50 of 0.54 nM.

Synonyms: YM-155

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Product Details of Sepantronium bromide

CAS No. :781661-94-7
Formula : C20H19BrN4O3
M.W : 443.29
SMILES Code : [Br-].O=C1C=2C=CC=CC2C(=O)C3=C1N(C(=[N+]3CC4=NC=CN=C4)C)CCOC
Synonyms :
YM-155
MDL No. :MFCD11983133
InChI Key :QBIYUDDJPRGKNJ-UHFFFAOYSA-M
Pubchem ID :11178236

Safety of Sepantronium bromide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target

  • Survivin

    Survivin, IC50:0.54 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
UKF-NB-3 0.49 nM 120 h YM155 affects the viability of drug-resistant neuroblastoma cells through survivin depletion and p53 activation. PMC5133961
UKF-NB-6 0.65 nM 120 h YM155 affects the viability of drug-resistant neuroblastoma cells through survivin depletion and p53 activation. PMC5133961
CAL27 cells 12.7 nM 24 h YM155 induced apoptosis in CAL27 cells in a mitochondria and death receptor-dependent manner, and significantly enhanced autophagy, leading to cell death PMC4669714
HSC3 cells 19.1 nM 24 h YM155 induced apoptosis in HSC3 cells in a mitochondria and death receptor-dependent manner, and significantly enhanced autophagy, leading to cell death PMC4669714
U251 cells 5 nM 48 h To evaluate the effects of YM155 on the proliferation and radiosensitivity of U251 cells, the results showed that YM155 reduced cell viability and enhanced radiosensitivity. PMC5865331
U87 cells 5 nM 48 h To evaluate the effects of YM155 on the proliferation and radiosensitivity of U87 cells, the results showed that YM155 reduced cell viability and enhanced radiosensitivity. PMC5865331
KBM7 cells 100 nM 3 days To validate the dependency of YM155 on SLC35F2, results showed that cells lacking SLC35F2 were significantly less sensitive to YM155. PMC4913867
Healthy human peripheral blood mononuclear cells (PBMCs) 100 nM 24 h To evaluate the effect of YM155 on T cell apoptosis, results showed that YM155 increased T cell apoptosis. PMC8377163
HeLa cells 25 nM 24 h The cell viability assay was used to screen the sensitivity of USP32 knockout to YM155, and it was found that USP32 knockout increased sensitivity to YM155. PMC8581437
PC3 cells 10 nM 16 h To investigate the effect of Sepantronium on oxygen consumption in PC3 cells, the results showed that Sepantronium significantly inhibited oxygen consumption. PMC4539531
PC3 cells 10 nM 16 h To investigate the effect of Sepantronium on ATP production in PC3 cells, the results showed that Sepantronium significantly reduced ATP production. PMC4539531
PC3 cells 10 nM 16 h To investigate the effect of Sepantronium on Complex II activity in PC3 cells, the results showed that Sepantronium significantly inhibited Complex II activity. PMC4539531

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
mice CAL27 xenograft and transgenic HNSCC mouse models intraperitoneal injection 5 mg/kg twice per week for 2 weeks YM155 displayed potent antitumor activities in both CAL27 xenograft and transgenic HNSCC mouse models by delaying tumor onset and suppressing tumor growth PMC4669714
Nude mice Orthotopic glioblastoma model Intratumoral injection 5 mg/kg Twice a week, total of five injections To evaluate the effects of YM155 combined with radiotherapy on the survival and tumor growth in a glioblastoma mouse model, the results showed that combination therapy significantly prolonged survival and inhibited tumor growth. PMC5865331
Mice SW480 cell xenograft model Subcutaneous injection 10 mg/kg Once daily for 7 days To validate the impact of SLC35F2 expression levels on YM155 efficacy in vivo, results showed that tumors with high SLC35F2 expression were more sensitive to YM155. PMC4913867
Mice Acute heart transplant rejection model Intraperitoneal injection 5 mg/kg Administered on days -1, 1, 3, 5 To evaluate the effect of YM155 on acute heart transplant rejection, results showed that YM155 prolonged graft survival and reduced inflammatory cell infiltration. PMC8377163
NOD scid γ (NSG) mice Breast cancer xenograft model Intraperitoneal injection 7.5 mg/kg Twice a week until the end of the experiment The xenograft model was used to validate the effect of USP32 knockout on the anti-tumor efficacy of YM155, and it was found that USP32 knockout significantly reduced tumor volume and weight. PMC8581437

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.28mL

2.26mL

1.13mL

22.56mL

4.51mL

2.26mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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