Nur für die Forschung bestimmt
Kat.-Nr.: S1130
Chemische Struktur
| Verwandte Targets | Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras |
|---|---|
| Andere Survivin Inhibitors | LQZ-7I FL118 |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | 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 | |||
| Klicken Sie hier, um weitere experimentelle Zellliniendaten anzuzeigen | ||||||
| Molekulargewicht | 443.29 | Formel | C20H19BrN4O3 |
Lagerung (Ab Erhaltdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 781661-94-7 | SDF herunterladen | Lagerung von Stammlösungen |
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In vitro |
Water : 89 mg/mL
DMSO
: 55 mg/mL
(124.07 mM)
Ethanol : 6 mg/mL |
|
In vivo |
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Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.
| Targets/IC50/Ki |
Survivin
(HeLa-SURP-luc, CHO-SV40-luc cells) 0.54 nM
|
|---|---|
| In vitro |
Sepantronium Bromide (YM155) is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. It 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 this compound shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. It 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. It 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. This compound delays the repair of radiation-induced double-strand breaks in nuclear DNA. |
| Kinase-Assay |
Promoter-Luciferase-Reporter-Assay
|
|
Eine 2.767 bp lange Sequenz des menschlichen Survivin-Genpromotors wird mittels PCR aus menschlicher genomischer DNA unter Verwendung von Pyrobest-Polymerase und den folgenden Primern isoliert: 5
|
|
| In vivo |
Sepantronium Bromide (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 it is highly distributed to tumor tissue. Moreover, this compound shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice. |
Referenzen |
|
| Methoden | Biomarker | Bilder | 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 |
(Daten von https://clinicaltrials.gov, aktualisiert am 2025-01-14)
| NCT-Nummer | Rekrutierung | Bedingungen | Sponsor/Kollaboratoren | Startdatum | Phases |
|---|---|---|---|---|---|
| NCT05263583 | ACTIVE_NOT_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 |
2022-12-09 | PHASE2 |
| 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 |
2022-12-09 | Phase 2 |
| NCT01007292 | COMPLETED | Non-Hodgkin's Lymphoma |
Astellas Pharma Inc |
2009-11 | PHASE2 |
| NCT01100931 | COMPLETED | NSCLC; Solid Tumors |
National Cancer Institute (NCI) |
2010-02 | PHASE1; PHASE2 |
| NCT01038804 | COMPLETED | Breast Cancer |
Astellas Pharma Inc |
2009-12 | PHASE2 |
| NCT01009775 | COMPLETED | Melanoma |
Astellas Pharma Inc |
2009-11 | PHASE2 |