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Sepantronium Bromide (YM155) of Selleck (Japan)

Sepantronium Bromide (YM155)

Name: Sepantronium Bromide (YM155)
Brand: Selleck Chemicals
SKU: S1130
Rating: 5 (180 reviews)

Catalog No.S1130 Purity:99.45%

For research use only.

Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.

Sepantronium Bromide (YM155) Chemical Structure

CAS No. 781661-94-7

Purity & Quality Control

Batch: Purity: 99.45%

99.45

Sepantronium Bromide (YM155) Related Products

Related Compound Libraries	Autophagy Compound Library Apoptosis Compound Library Ferroptosis Compound Library Pyroptosis Compound Library Mitochondria-Targeted Compound Library	Click to Expand

Signaling Pathway

Survivin Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Kasumi-1	Growth Inhibition Assay		72 h	DMSO	IC50=0.009 ± 0.0009 μM	25659731
M-07e	Growth Inhibition Assay		72 h	DMSO	IC50=0.040 ± 0.013 μM	25659731
THP-1	Growth Inhibition Assay		72 h	DMSO	IC50=0.051 ± 0.013 μM	25659731
CMK	Growth Inhibition Assay		72 h	DMSO	IC50=0.053 ± 0.009 μM	25659731
MV4-11	Growth Inhibition Assay		72 h	DMSO	IC50=0.055 ± 0.028 μM	25659731
AML-193	Growth Inhibition Assay		72 h	DMSO	IC50=0.462 ± 0.060 μM	25659731
HL-60	Growth Inhibition Assay		72 h	DMSO	IC50=0.001 ± 0.0002 μM	25659731
ML-2	Growth Inhibition Assay		72 h	DMSO	IC50=0.009 ± 0.002 μM	25659731
OCI/AML3	Growth Inhibition Assay		72 h	DMSO	IC50=0.011 ± 0.002 μM	25659731
HEL	Growth Inhibition Assay		72 h	DMSO	IC50=0.559 ± 0.038 μM	25659731
ME-1	Growth Inhibition Assay		72 h	DMSO	IC50=0.684 ± 0.179 μM	25659731
THP-1	Apoptosis Assay	1 μM	72 h	DMSO	induces apoptosis	25659731
M-07e	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
THP-1	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
CMK	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
AML-193	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
Kasumi-1	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
MV4-11	Function Assay	0–1 μM	72 h	DMSO	induces downregulation of Survivin	25659731
MUG-Chor	Growth Inhibition Assay	0-5 μM	24/48 h		IC50=7.05 nM for 48h	25640185
U-CH1	Growth Inhibition Assay	0-5 μM	24/48 h		IC50=9.03 nM for 48h	25640185
KATOIII	Growth Inhibition Assay	10/20 nM	48 h		inhibits cell growth in a dose-dependent manner	25635055
AGS	Growth Inhibition Assay	10/20 nM	48 h		inhibits cell growth in a dose-dependent manner	25635055
SACC-83	Function Assay	5 nM	48 h		decreases nuclear expression of HIF-1α	25485635
INA-6	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
U-266	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
MOLP-8	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
HG-1	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
NCI-H929	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
OPM-2	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
L-363	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
MOLP-2	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
KMS-12-BM	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
SK-MM-2	Growth Inhibition Assay	0-500 nM	48 h		inhibits cell growth in a dose-dependent manner	25296978
U-266	Apoptosis Assay	0-50 nM	24 h		induces apoptosis	25296978
INA-6	Apoptosis Assay	0-50 nM	24 h		induces apoptosis	25296978
MCF7	Growth Inhibition Assay		72 h		IC50=13 ± 6 nM	25220225
MCF7-TamR6	Growth Inhibition Assay		72 h		IC50=8 ± 6 nM	25220225
MCF7-TamR7	Growth Inhibition Assay		72 h		IC50=8 ± 3 nM	25220225
MCF7-TamR8	Growth Inhibition Assay		72 h		IC50=15 ± 6 nM	25220225
MCF7-TamC3	Growth Inhibition Assay		72 h		IC50=6 ± 3 nM	25220225
MCF7-TamC6	Growth Inhibition Assay		72 h		IC50=6 ± 0.1 nM	25220225
MDA-MB-231	Growth Inhibition Assay		72 h		IC50=5 ± 1 nM	25220225
SK-BR-3	Growth Inhibition Assay		72 h		IC50=7 ± 0.3 nM	25220225
Eca109	Function Assay	1-50 nM	48 h	DMSO	suppresses survivin expression in a dose dependent manner	25139395
TE13	Function Assay	1-50 nM	48 h	DMSO	suppresses survivin expression in a dose dependent manner	25139395
Eca109	Growth Inhibition Assay	0-100 nM	24/48 h	DMSO	decreases cell viability in a dose-dependent manner	25139395
TE13	Growth Inhibition Assay	0-100 nM	24/48 h	DMSO	decreases cell viability in a dose-dependent manner	25139395
MT-3	Kinase Assay		72 h	DMSO	IC50=2.86 ± 0.54 nM for DR4 expression	24866585
MDA-MB-468	Kinase Assay		72 h	DMSO	IC50=0.11 ± 0.01 nM for DR4 expression	24866585
SUM-159	Kinase Assay		72 h	DMSO	IC50=1.72 ± 0.33 nM for DR4 expression	24866585
MT-3	Kinase Assay		72 h	DMSO	IC50=54.11 ± 4.32 nM for DR5 expression	24866585
MDA-MB-468	Kinase Assay		72 h	DMSO	IC50=0.07 ± 0.02 nM for DR5 expression	24866585
SUM-159	Kinase Assay		72 h	DMSO	IC50=69.4 ± 4.23 nM for DR5 expression	24866585
MT-3 + NAC	Kinase Assay		72 h	DMSO	IC50=56.2 ± 2.07 nM for DR5 expression	24866585
MT-3 + SB203580	Kinase Assay		72 h	DMSO	IC50=38.41 ± 5.02 nM for DR5 expression	24866585
DB	Growth Inhibition Assay	10 nM	24 h	DMSO	inhibits cell proliferation	24486595
SU-DHL-8	Growth Inhibition Assay	10 nM	24 h	DMSO	inhibits cell proliferation	24486595
WSU-DLCL2	Growth Inhibition Assay	10 nM	24 h	DMSO	inhibits cell proliferation	24486595
ACC-2	Growth Inhibition Assay	0-100 nM	24 h		inhibits cell growth in a dose-dependent manner	24370995
ACC-2	Apoptosis Assay	0-20 nM	24 h		induces apoptosis in a dose-dependent manner	24370995
ACC-2	Function Assay	0-20 nM	24 h		increases the conversion of LC3I to LC3II	24370995
BFTC905	Growth Inhibition Assay	0-1000 nM	48 h	DMSO	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
T24	Growth Inhibition Assay	0-1000 nM	48 h	DMSO	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
TSGH8301	Growth Inhibition Assay	0-1000 nM	48 h	DMSO	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
BFTC909	Growth Inhibition Assay	0-1000 nM	48 h	DMSO	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
BFTC905	Apoptosis Assay	20 nM	48 h	DMSO	induces apoptosis	24297644
BFTC905	Function Assay	20 nM	48 h	DMSO	decreases the expression of LC3B-II	24297644
A2780p	Function Assay	0-100 nM	24 h	DMSO	induces Survivin downregulation	24262875
A2780cis	Function Assay	0-100 nM	24 h	DMSO	induces Survivin downregulation	24262875
A2780p	Apoptosis Assay	5-100 nM	24/48 h	DMSO	increases apoptosis in a concentration-dependent manner	24262875
A2780cis	Apoptosis Assay	5-100 nM	24/48 h	DMSO	increases apoptosis in a concentration-dependent manner	24262875
SH-SY5Y	Apoptosis Assay	1/10/100 µM	72 h	DMSO	induces apoptosis in a dose-dependent manner	24254560
HL-60	Growth Inhibition Assay		72 h	DMSO	IC50=0.3 nM	23618862
U937	Growth Inhibition Assay		72 h	DMSO	IC50=0.8 nM	23618862
HL-60	Function Assay	1 μM	6/12/24 h	DMSO	inhibits the expression of survivin	23618862
U937	Function Assay	1 μM	6/12/24 h	DMSO	inhibits the expression of survivin	23618862
HL-60	Apoptosis Assay	0.1/1 μM	8 h	DMSO	induces apoptosis	23618862
Sk-NEP-1	Growth Inhibition Assay	1-10000 nM	24 h	DMSO	IC50=100 nM	23267699
SK-NEP-1	Apoptosis Assay	50/100 nM	12/24 h	DMSO	induces apoptosis	23267699
TC-32	Growth Inhibition Assay	0.1-1000 nM			EC50=3.0 nM, inhibits cell growth in a dose-dependent manner	22961763
TC-71	Growth Inhibition Assay	0.1-1000 nM			EC50=5.7 nM, inhibits cell growth in a dose-dependent manner	22961763
SK-ES-1	Growth Inhibition Assay	0.1-1000 nM			EC50=2.8 nM, inhibits cell growth in a dose-dependent manner	22961763
RD-ES	Growth Inhibition Assay	0.1-1000 nM			EC50=6.2 nM, inhibits cell growth in a dose-dependent manner	22961763
HEK293	Growth Inhibition Assay	0.1-1000 nM			EC50=23.0 nM, inhibits cell growth in a dose-dependent manner	22961763
M059J	Growth Inhibition Assay	0-50 nM	48 h		inhibits cell growth in a dose-dependent manner	22770110
M059K	Growth Inhibition Assay	0-50 nM	48 h		inhibits cell growth in a dose-dependent manner	22770110
M059J	Apoptosis Assay	30 nM	24 h		induces apoptosis	22770110
M059K	Apoptosis Assay	30 nM	24 h		induces apoptosis	22770110
PANC-1	Growth Inhibition Assay	0.01-1000 nM	48 h		IC50=3.69 nM	22723871
MIAPaCa-2	Growth Inhibition Assay	0.01-1000 nM	48 h		IC50=29.36 nM	22723871
BxPC-3	Growth Inhibition Assay	0.01-1000 nM	48 h		IC50=30.26 nM	22723871
PANC-1	Function Assay	0-1000 nM	24 h		induces downregulation of XIAP and survivin expression	22723871
MIAPaCa-2	Function Assay	0-1000 nM	24 h		induces downregulation of XIAP and survivin expression	22723871
BxPC-3	Function Assay	0-1000 nM	24 h		induces downregulation of XIAP and survivin expression	22723871
RPMI-7951	Growth Inhibition Assay				GI50=3.2 nM	21737502
SK-MEL-5	Growth Inhibition Assay				GI50=4.2 nM	21737502
A375	Growth Inhibition Assay				GI50=6.3 nM	21737502
SK-MEL-28	Growth Inhibition Assay				GI50=7.6 nM	21737502
SK-MEL-2	Growth Inhibition Assay				GI50=11 nM	21737502
DB	Growth Inhibition Assay		48 h		GI50=3.5 nM	21237508
Pfeiffer	Growth Inhibition Assay		48 h		GI50=3.9 nM	21237508
SU-DHL-5	Growth Inhibition Assay		48 h		GI50=0.23 nM	21237508
SU-DHL-8	Growth Inhibition Assay		48 h		GI50=1.4 nM	21237508
WSU-DLCL-2	Growth Inhibition Assay		48 h		GI50=1.4 nM	21237508
A549	Growth inhibition assay				Growth inhibition of human A549 cells, IC50=0.0134μM	28814374
DU145	Cytotoxicity assay				Cytotoxicity against human DU145 cells by MTT assay, EC50=0.0138μM	28774426
PC3	Cytotoxicity assay				Cytotoxicity against human PC3 cells by MTT assay, EC50=0.092μM	28774426
A549	Function assay				Inhibition of PAK1 in human A549 cells, IC50=0.5μM	28814374
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

Survivin ^[1]
(HeLa-SURP-luc, CHO-SV40-luc cells)

0.54 nM

In vitro
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]
Kinase Assay	Promoter-luciferase reporter assay
Kinase 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 Research	Cell lines	Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375)
	Concentrations	~ 100 nM
	Incubation Time	48 hours
	Method	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	Survivin / XIAP / Caspase-7 / Caspase-9 / Caspase-3 / Cleaved Caspase-8 / PARP β-catenin / c-Myc / Cyclin D1 / CD44 p-STAT3 / STAT3		26771139
	Immunofluorescence	EGFR PARP-1 / PAR		22723871
	Growth inhibition assay	Cell viability		29636860

In Vivo
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]
Animal Research	Animal Models	PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
	Dosages	5 mg/kg
	Administration	Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05263583	Recruiting	High-grade B-cell Lymphoma\|Burkitt Lymphoma\|Lymphoma B-Cell\|Lymphoma Large B-Cell Diffuse\|Lymphatic Diseases\|Lymphoma High-Grade\|C-MYC/BCL2 Double-Hit High-Grade B-Cell Lymphoma\|C-MYC/BCL6 Double-Hit High-Grade B-Cell Lymphoma\|C-Myc Gene Rearrangement	Cothera Bioscience Inc	December 9 2022	Phase 2
NCT01023386	Completed	Cancer	Astellas Pharma Inc	November 2009	Phase 1

References

https://pubmed.ncbi.nlm.nih.gov/17804712/
https://pubmed.ncbi.nlm.nih.gov/18927289/

Chemical Information & Solubility

Molecular Weight	443.29	Formula	C₂₀H₁₉BrN₄O₃
CAS No.	781661-94-7	SDF	Download Sepantronium Bromide (YM155) SDF
Smiles	CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 89 mg/mL

DMSO : 55 mg/mL ( (124.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (67.68mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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