Sepantronium Bromide (YM155)

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.

CAS No. 781661-94-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
100mg	JPY 115500	国内在庫あり
1g	JPY 418500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（173）

製品安全説明書

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Sepantronium Bromide (YM155)関連製品

関連化合物ライブラリー	Autophagy Compound Library Apoptosis Compound Library Ferroptosis Compound Library Pyroptosis Compound Library Mitochondria-Targeted Compound Library	もっと見る

シグナル伝達経路

Survivinシグナル伝達経路

Survivin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
WSU-DLCL2	Growth Inhibition Assay	10 nM	24 h	inhibits cell proliferation	24486595
SU-DHL-8	Growth Inhibition Assay	10 nM	24 h	inhibits cell proliferation	24486595
DB	Growth Inhibition Assay	10 nM	24 h	inhibits cell proliferation	24486595
TE13	Growth Inhibition Assay	0-100 nM	24/48 h	decreases cell viability in a dose-dependent manner	25139395
Eca109	Growth Inhibition Assay	0-100 nM	24/48 h	decreases cell viability in a dose-dependent manner	25139395
TE13	Function Assay	1-50 nM	48 h	suppresses survivin expression in a dose dependent manner	25139395
Eca109	Function Assay	1-50 nM	48 h	suppresses survivin expression in a dose dependent manner	25139395
INA-6	Apoptosis Assay	0-50 nM	24 h	induces apoptosis	25296978
U-266	Apoptosis Assay	0-50 nM	24 h	induces apoptosis	25296978
SK-MM-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
MOLP-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
OPM-2	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
HG-1	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
U-266	Growth Inhibition Assay	0-500 nM	48 h	inhibits cell growth in a dose-dependent manner	25296978
INA-6	Growth Inhibition Assay	0-500 nM	48 h	inhibits cell growth in a dose-dependent manner	25296978
SACC-83	Function Assay	5 nM	48 h	decreases nuclear expression of HIF-1α	25485635
AGS	Growth Inhibition Assay	10/20 nM	48 h	inhibits cell growth in a dose-dependent manner	25635055
KATOIII	Growth Inhibition Assay	10/20 nM	48 h	inhibits cell growth in a dose-dependent manner	25635055
U-CH1	Growth Inhibition Assay	0-5 μM	24/48 h	IC50=9.03 nM for 48h	25640185
MUG-Chor	Growth Inhibition Assay	0-5 μM	24/48 h	IC50=7.05 nM for 48h	25640185
MV4-11	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
Kasumi-1	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
AML-193	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
CMK	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
THP-1	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
M-07e	Function Assay	0–1 μM	72 h	induces downregulation of Survivin	25659731
THP-1	Apoptosis Assay	1 μM	72 h	induces apoptosis	25659731
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	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
T24	Growth Inhibition Assay	0-1000 nM	48 h	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
TSGH8301	Growth Inhibition Assay	0-1000 nM	48 h	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
BFTC909	Growth Inhibition Assay	0-1000 nM	48 h	IC50=20 nM, inhibits cell growth in a dose-dependent manner	24297644
BFTC905	Apoptosis Assay	20 nM	48 h	induces apoptosis	24297644
BFTC905	Function Assay	20 nM	48 h	decreases the expression of LC3B-II	24297644
A2780p	Function Assay	0-100 nM	24 h	induces Survivin downregulation	24262875
A2780cis	Function Assay	0-100 nM	24 h	induces Survivin downregulation	24262875
A2780p	Apoptosis Assay	5-100 nM	24/48 h	increases apoptosis in a concentration-dependent manner	24262875
A2780cis	Apoptosis Assay	5-100 nM	24/48 h	increases apoptosis in a concentration-dependent manner	24262875
SH-SY5Y	Apoptosis Assay	1/10/100 µM	72 h	induces apoptosis in a dose-dependent manner	24254560
HL-60	Function Assay	1 μM	6/12/24 h	inhibits the expression of survivin	23618862
U937	Function Assay	1 μM	6/12/24 h	inhibits the expression of survivin	23618862
HL-60	Apoptosis Assay	0.1/1 μM	8 h	induces apoptosis	23618862
Sk-NEP-1	Growth Inhibition Assay	1-10000 nM	24 h	IC50=100 nM	23267699
SK-NEP-1	Apoptosis Assay	50/100 nM	12/24 h	induces apoptosis	23267699
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
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
MT-3 + SB203580	Kinase Assay		72 h	IC50=38.41 ± 5.02 nM for DR5 expression	24866585
MT-3 + NAC	Kinase Assay		72 h	IC50=56.2 ± 2.07 nM for DR5 expression	24866585
SUM-159	Kinase Assay		72 h	IC50=69.4 ± 4.23 nM for DR5 expression	24866585
MDA-MB-468	Kinase Assay		72 h	IC50=0.07 ± 0.02 nM for DR5 expression	24866585
MT-3	Kinase Assay		72 h	IC50=54.11 ± 4.32 nM for DR5 expression	24866585
SUM-159	Kinase Assay		72 h	IC50=1.72 ± 0.33 nM for DR4 expression	24866585
MDA-MB-468	Kinase Assay		72 h	IC50=0.11 ± 0.01 nM for DR4 expression	24866585
MT-3	Kinase Assay		72 h	IC50=2.86 ± 0.54 nM for DR4 expression	24866585
SK-BR-3	Growth Inhibition Assay		72 h	IC50=7 ± 0.3 nM	25220225
MDA-MB-231	Growth Inhibition Assay		72 h	IC50=5 ± 1 nM	25220225
MCF7-TamC6	Growth Inhibition Assay		72 h	IC50=6 ± 0.1 nM	25220225
MCF7-TamC3	Growth Inhibition Assay		72 h	IC50=6 ± 3 nM	25220225
MCF7-TamR8	Growth Inhibition Assay		72 h	IC50=15 ± 6 nM	25220225
MCF7-TamR7	Growth Inhibition Assay		72 h	IC50=8 ± 3 nM	25220225
MCF7-TamR6	Growth Inhibition Assay		72 h	IC50=8 ± 6 nM	25220225
MCF7	Growth Inhibition Assay		72 h	IC50=13 ± 6 nM	25220225
ME-1	Growth Inhibition Assay		72 h	IC50=0.684 ± 0.179 μM	25659731
HEL	Growth Inhibition Assay		72 h	IC50=0.559 ± 0.038 μM	25659731
OCI/AML3	Growth Inhibition Assay		72 h	IC50=0.011 ± 0.002 μM	25659731
ML-2	Growth Inhibition Assay		72 h	IC50=0.009 ± 0.002 μM	25659731
HL-60	Growth Inhibition Assay		72 h	IC50=0.001 ± 0.0002 μM	25659731
AML-193	Growth Inhibition Assay		72 h	IC50=0.462 ± 0.060 μM	25659731
MV4-11	Growth Inhibition Assay		72 h	IC50=0.055 ± 0.028 μM	25659731
CMK	Growth Inhibition Assay		72 h	IC50=0.053 ± 0.009 μM	25659731
THP-1	Growth Inhibition Assay		72 h	IC50=0.051 ± 0.013 μM	25659731
M-07e	Growth Inhibition Assay		72 h	IC50=0.040 ± 0.013 μM	25659731
Kasumi-1	Growth Inhibition Assay		72 h	IC50=0.009 ± 0.0009 μM	25659731
HL-60	Growth Inhibition Assay		72 h	IC50=0.3 nM	23618862
U937	Growth Inhibition Assay		72 h	IC50=0.8 nM	23618862
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
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
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
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生物活性

製品説明

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.

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
細胞実験	細胞株	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)
	濃度	~ 100 nM
	反応時間	48 hours
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	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]
動物実験	動物モデル	PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
	投与量	5 mg/kg
	投与経路	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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Nakahara T, et al. Cancer Res, 2007, 67(17), 8014-8021. [2] Iwasa T, et al. Clin Cancer Res, 2008, 14(20), 6496-6504.

参考

化学情報

分子量	443.29	化学式	C₂₀H₁₉BrN₄O₃
CAS No.	781661-94-7	SDF	Download Sepantronium Bromide (YM155) SDFをダウンロードする
Smiles	CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

Water : 89 mg/mL

DMSO : 55 mg/mL ( (124.07 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 6 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):