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Sepantronium Bromide (YM155) Survivin Remmer

Name: Sepantronium Bromide (YM155)
Brand: Selleck Chemicals
SKU: S1130
Rating: 5 (182 reviews)

Cat.Nr.: S1130

Sepantronium Bromide (YM155) is een krachtige survivin onderdrukker door de Survivin-promotoractiviteit te remmen met een IC50 van 0,54 nM in HeLa-SURP-luc en CHO-SV40-luc cellen. Het remt de SV40-promotoractiviteit niet significant, maar er wordt waargenomen dat het de interactie van Survivin met XIAP lichtjes remt. Deze verbinding reguleert survivin en XIAP naar beneden, moduleert autophagy en induceert autophagy-afhankelijke DNA-schade in borstkankercellen. Fase 2.

Sepantronium Bromide (YM155) Survivin Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 443.29

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.45%

99.45

Gerelateerde doelwitten	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Overige Survivin Inhibitoren	LQZ-7I FL118

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	443.29	Formule	C₂₀H₁₉BrN₄O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	781661-94-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid (Solubility)

In vitro
Batch:

Water : 89 mg/mL

DMSO : 55 mg/mL (124.07 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 6 mg/mL

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

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-reporteranalyse
Kinase Assay	Een 2.767 bp sequentie van de menselijke survivin-genpromotor wordt geïsoleerd uit menselijk genomisch DNA door PCR met Pyrobest polymerase en de volgende primers: 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.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/17804712/ [2] https://pubmed.ncbi.nlm.nih.gov/18927289/

Toepassingen (Applications)

Methoden	Biomarkers	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

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2025-01-14)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

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