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Sepantronium Bromide (YM155) Survivin Inhibidor

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

Cat. No.: S1130

Sepantronium Bromide (YM155) es un potente supresor de survivin al inhibir la actividad del promotor de Survivin con una IC50 de 0,54 nM en células HeLa-SURP-luc y CHO-SV40-luc. No inhibe significativamente la actividad del promotor SV40, pero se observa que inhibe ligeramente la interacción de Survivin con XIAP. Este compuesto regula a la baja la survivin y la XIAP, modula la autophagy e induce daño en el ADN dependiente de la autofagia en células de cáncer de mama. Fase 2.

Sepantronium Bromide (YM155) Survivin Inhibidor Chemical Structure

Estructura química

Peso molecular: 443.29

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.45%

99.45

Dianas relacionadas	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Otros Survivin Inhibidores	LQZ-7I FL118

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	443.29	Fórmula	C₂₀H₁₉BrN₄O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	781661-94-7	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente

Solubilidad (Solubility)

In vitro
Lote:

Water : 89 mg/mL

DMSO : 55 mg/mL (124.07 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 6 mg/mL

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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.
Ensayo de quinasa	Ensayo de reportero de promotor-luciferasa
Ensayo de quinasa	Una secuencia de 2.767 pb del promotor del gen survivin humano se aísla del ADN genómico humano mediante PCR utilizando la polimerasa Pyrobest y los siguientes cebadores: 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.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/17804712/ [2] https://pubmed.ncbi.nlm.nih.gov/18927289/

Aplicaciones (Applications)

Métodos	Biomarcadores	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

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2025-01-14)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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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