Sepantronium Bromide (YM155)
Sepantronium Bromide(YM155)是一种有效的survivin抑制药，通过抑制Survivin启动子活性而发挥作用，在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM；对SV40启动子活性抑制作用不显著，能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivin 和 XIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。
Sepantronium Bromide (YM155) Chemical Structure
CAS: 781661-94-7
产品质控
批次：
纯度：
99.45%
99.45
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Sepantronium Bromide(YM155)是一种有效的survivin抑制药，通过抑制Survivin启动子活性而发挥作用，在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM；对SV40启动子活性抑制作用不显著，能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivin 和 XIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | YM155 30 μM时对SV40作用效果也不大。在p53缺陷的PC-3和PPC-1 人类HRPC细胞中，通过抑制 survivin基因启动子的转录，YM155显著抑制内源性survivin的表达。相反，YM155 100 nM时对c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin,及β-tubulin的蛋白表达仍没抑制效果。YM155作用于人类癌细胞系包括PC-3和PPC-1，使细胞发生凋亡，伴随着caspase-3活性上升。YM155有效抑制人类癌细胞系(突变p53或短小p53) 包括PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5及A375 ，IC50值为2.3到11 nM。[1]另外，YM155增强NSCLC细胞对γ-射线的敏感性。YM155和γ-射线联用，增强凋亡细胞数和caspase-3活性。 YM155推迟修复放射诱导核DNA断裂的双链。[2] |
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|---|---|---|---|---|
| 激酶实验 | 启动子-荧光酶素报告实验 | |||
| 使用Pyrobest聚合酶和引物5’-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3’和5’-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3’， 从人类基因组DNA中分离2767个碱基对序列的人类survivin基因启动子。在pGL3-Basic质粒的XhoI/HindIII切除位点，内切酶XhoI/HindIII切除产生的PCR片段。产生的质粒称为pSUR-luc。通过DNA测序仪在所有增强序列处测定DNA序列。通过荧光酶素实验，使用短暂转染的HeLa-S3细胞，测定pSUR-luc的活力。使用的pGL3质粒含有SV40启动子和增强子序列。 pSUR-luc和pSV2bsr 质粒通过Lipofectamin2000稳定转染到HeLa细胞中。加入10 μg/mL灭瘟素，根据适当的荧光酶素信号和基因稳定性，筛选HeLa-SURP-luc单一群落。pGL3和pSV2bsr质粒稳定转染到CHO细胞中。加入10 μg/mL灭瘟素，根据适当的荧光酶素信号和基因稳定性，筛选CHO-SV40-luc单一群落。从HeLa-SURP-luc和CHO-SV40-luc群落中获得细胞用于化学筛选。细胞按每孔5×103接种在96孔板上，加入YM155（溶于DMSO中）。24小时后测定荧光酶素活性。通过回归分析计算IC50值。 | ||||
| 细胞实验 | 细胞系 | PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5，和A375细胞 | ||
| 浓度 | ~ 100 nM | |||
| 孵育时间 | 48小时 | |||
| 方法 | PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5，及A375细胞系按5到40×103密度接种在96孔板上。YM155溶解在DMSO中，持续处理细胞48小时。通过sulforhodamine B试剂测定细胞数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT3 / STAT3 β-catenin / c-Myc / Cyclin D1 / CD44 Survivin / XIAP / Caspase-7 / Caspase-9 / Caspase-3 / Cleaved Caspase-8 / PARP |
|
22723871 | |
| Immunofluorescence | PARP-1 / PAR EGFR |
|
26090615 | |
| Growth inhibition assay | Cell viability |
|
29636860 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | YM155按3和10 mg/kg皮下注射前列腺移植瘤，结果显示YM155完全抑制PC-3的肿瘤生长，但是重量没有降低，血细胞数也没有下降。药物动力学分析显示YM155作用于肿瘤组织效果很明显。而且，YM155按5 mg/kg作用于PC-3常位移植瘤时肿瘤抑制率达80% 。[1]YM155和γ-射线联用作用于携带H460或Calu6 移植瘤的裸鼠，显示出强抗癌活性。[2] |
|
|---|---|---|
| 动物实验 | Animal Models | 皮下注射PC-3移植瘤的雄性裸鼠(BALB/c nu/nu) |
| Dosages | 5 mg/kg | |
| Administration | 皮下注射，每周持续处理3天，处理3周。 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
化学信息&溶解度
| 分子量 | 443.29 | 分子式 | C20H19BrN4O3 |
| CAS号 | 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-] | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Water : 89 mg/mL (200.77 mM) DMSO : 55 mg/mL ( (124.07 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 6 mg/mL (13.53 mM) |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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