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Apoptosis
Survivin inhibitor
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IAP inhibitor
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Autophagy activator
Sepantronium Bromide (YM155)
僅限科研使用
Sepantronium Bromide (YM155)
Sepantronium Bromide(YM155)是一種有效的survivin抑制藥，通過抑制Survivin啟動子活性而發(fā)揮作用，在HeLa-SURP-luc 和 CHO-SV40-luc細(xì)胞中IC50為0.54 nM；對SV40啟動子活性抑制作用不顯著，能夠輕微抑制Survivin與XIAP相互作用。YM155 在乳腺癌細(xì)胞中可下調(diào) survivin 和 XIAP、調(diào)節(jié)自噬并誘導(dǎo)自噬依賴的DNA損傷。Phase 2。
Sepantronium Bromide (YM155) Chemical Structure
CAS: 781661-94-7
產(chǎn)品質(zhì)控
批次：
純度：
99.45%
99.45
Sepantronium Bromide (YM155)相關(guān)產(chǎn)品
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相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(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 | ||
| 點擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Sepantronium Bromide(YM155)是一種有效的survivin抑制藥，通過抑制Survivin啟動子活性而發(fā)揮作用，在HeLa-SURP-luc 和 CHO-SV40-luc細(xì)胞中IC50為0.54 nM；對SV40啟動子活性抑制作用不顯著，能夠輕微抑制Survivin與XIAP相互作用。YM155 在乳腺癌細(xì)胞中可下調(diào) survivin 和 XIAP、調(diào)節(jié)自噬并誘導(dǎo)自噬依賴的DNA損傷。Phase 2。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | YM155 30 μM時對SV40作用效果也不大。在p53缺陷的PC-3和PPC-1 人類HRPC細(xì)胞中，通過抑制 survivin基因啟動子的轉(zhuǎn)錄，YM155顯著抑制內(nèi)源性survivin的表達(dá)。相反，YM155 100 nM時對c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin,及β-tubulin的蛋白表達(dá)仍沒抑制效果。YM155作用于人類癌細(xì)胞系包括PC-3和PPC-1，使細(xì)胞發(fā)生凋亡，伴隨著caspase-3活性上升。YM155有效抑制人類癌細(xì)胞系(突變p53或短小p53) 包括PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5及A375 ，IC50值為2.3到11 nM。[1]另外，YM155增強(qiáng)NSCLC細(xì)胞對γ-射線的敏感性。YM155和γ-射線聯(lián)用，增強(qiáng)凋亡細(xì)胞數(shù)和caspase-3活性。 YM155推遲修復(fù)放射誘導(dǎo)核DNA斷裂的雙鏈。[2] |
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|---|---|---|---|---|
| 激酶實驗 | 啟動子-熒光酶素報告實驗 | |||
| 使用Pyrobest聚合酶和引物5’-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3’和5’-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3’， 從人類基因組DNA中分離2767個堿基對序列的人類survivin基因啟動子。在pGL3-Basic質(zhì)粒的XhoI/HindIII切除位點，內(nèi)切酶XhoI/HindIII切除產(chǎn)生的PCR片段。產(chǎn)生的質(zhì)粒稱為pSUR-luc。通過DNA測序儀在所有增強(qiáng)序列處測定DNA序列。通過熒光酶素實驗，使用短暫轉(zhuǎn)染的HeLa-S3細(xì)胞，測定pSUR-luc的活力。使用的pGL3質(zhì)粒含有SV40啟動子和增強(qiáng)子序列。 pSUR-luc和pSV2bsr 質(zhì)粒通過Lipofectamin2000穩(wěn)定轉(zhuǎn)染到HeLa細(xì)胞中。加入10 μg/mL滅瘟素，根據(jù)適當(dāng)?shù)臒晒饷杆匦盘柡突蚍€(wěn)定性，篩選HeLa-SURP-luc單一群落。pGL3和pSV2bsr質(zhì)粒穩(wěn)定轉(zhuǎn)染到CHO細(xì)胞中。加入10 μg/mL滅瘟素，根據(jù)適當(dāng)?shù)臒晒饷杆匦盘柡突蚍€(wěn)定性，篩選CHO-SV40-luc單一群落。從HeLa-SURP-luc和CHO-SV40-luc群落中獲得細(xì)胞用于化學(xué)篩選。細(xì)胞按每孔5×103接種在96孔板上，加入YM155（溶于DMSO中）。24小時后測定熒光酶素活性。通過回歸分析計算IC50值。 | ||||
| 細(xì)胞實驗 | 細(xì)胞系 | PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5，和A375細(xì)胞 | ||
| 濃度 | ~ 100 nM | |||
| 孵育時間 | 48小時 | |||
| 方法 | PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5，及A375細(xì)胞系按5到40×103密度接種在96孔板上。YM155溶解在DMSO中，持續(xù)處理細(xì)胞48小時。通過sulforhodamine B試劑測定細(xì)胞數(shù)。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | YM155按3和10 mg/kg皮下注射前列腺移植瘤，結(jié)果顯示YM155完全抑制PC-3的腫瘤生長，但是重量沒有降低，血細(xì)胞數(shù)也沒有下降。藥物動力學(xué)分析顯示YM155作用于腫瘤組織效果很明顯。而且，YM155按5 mg/kg作用于PC-3常位移植瘤時腫瘤抑制率達(dá)80% 。[1]YM155和γ-射線聯(lián)用作用于攜帶H460或Calu6 移植瘤的裸鼠，顯示出強(qiáng)抗癌活性。[2] |
|
|---|---|---|
| 動物實驗 | 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，每周持續(xù)處理3天，處理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 |
|
化學(xué)信息&溶解度
| 分子量 | 443.29 | 分子式 | C20H19BrN4O3 |
| CAS號 | 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-] | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
Water : 89 mg/mL (200.77 mM) DMSO : 55 mg/mL ( (124.07 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 6 mg/mL (13.53 mM) |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
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