Sepantronium (bromide) (Synonyms: YM-155)

Name: Sepantronium bromide
Brand: MedChemExpress
SKU: HY-10194
Rating: 5.0 (22 reviews)

製品番号: HY-10194 純度: 99.36%: Data Sheet SDS COA 取扱説明書
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Sepantronium bromide (YM-155) is a survivin inhibitor with an IC₅₀ of 0.54 nM.

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CAS 番号 : 781661-94-7

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$66	在庫あり	Estimated Time of Arrival: December 31
10 mg	$92	在庫あり	Estimated Time of Arrival: December 31
25 mg	$205	在庫あり	Estimated Time of Arrival: December 31
50 mg	$340	在庫あり	Estimated Time of Arrival: December 31
100 mg	$541	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 22 publication(s) in Google Scholar

Other Forms of Sepantronium bromide:

Sepantronium hydrochloride お問い合わせ
Sepantronium bromide (Standard) お問い合わせ

顧客検証

Cell Imaging/Staining

In Vivo Efficacy Study

IHC

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617. [Abstract]; A2780 CSLCs are treated in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Jul 1:425:54-64. [Abstract]; The cell model HepG2-Sur5P-EGFP-Sur3U was treated with Sepantronium bromide (YM155) at a final concentration of 100 nmol/ml. After 24 h later, the fluorescence strength of EGFP was recorded and the expression of Survivin was examined.

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Jul 1:425:54-64. [Abstract]; Huh-7 cell xenograft models were established by subcutaneously injection of 1 × 10⁶ cells per mouse in 4 groups of nude mice (n = 5/group). After five intratumoral injections of Sepantronium bromide (YM155) at 3 mg/ml, the tumor volume was counted weekly.

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Jul 1:425:54-64. [Abstract]; Huh-7 cell xenograft models were established by subcutaneously injection of 1 × 10⁶. cells per mouse in 4 groups of nude mice (n = 5/group). After five intratumoral injections of Sepantronium bromide (YM155) at 3 mg/ml. The xenografted tumors were weighed and compared.

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Jul 1:425:54-64. [Abstract]; Sepantronium bromide (YM-155, 3mg/mL)The xenograft tumor sections were examined by immunohistochemistry and TUNEL labeling. The expression levels of Survivin and the percentages of apoptotic cells in xenografted tumors were quantified within 5 high-power fields under microscope and showed in histograms.

: Sepantronium bromide purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353. [Abstract]; Influences of YM155, a chemical inhibitor of survivin on ABT-737-induced apoptosis are analyzed by western blot.

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製品説明

Sepantronium bromide (YM-155) is a survivin inhibitor with an IC₅₀ of 0.54 nM^[1].

IC₅₀ & Target

IC50: 0.54 nM (Survivin)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
143B	IC₅₀	0.32 μM Compound: YM155	Antiproliferative activity against human 143B cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human 143B cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
5637	IC₅₀	0.11 μM Compound: YM155	Antiproliferative activity against human 5637 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human 5637 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
A-375	IC₅₀	0.006 μM Compound: 1; YM155	Anticancer activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Anticancer activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38092421]
A549	IC₅₀	0.01 μM Compound: YM155	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
A549	IC₅₀	0.0134 μM Compound: YM155	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 28814374]
ASPC1	IC₅₀	0.51 μM Compound: YM155	Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
BXPC-3	IC₅₀	0.09 μM Compound: YM155	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
CWR22R	IC₅₀	0.011 μM Compound: 1; YM155	Cytotoxicity against human 22Rv1 cells assessed as cell growth inhibition Cytotoxicity against human 22Rv1 cells assessed as cell growth inhibition	[PMID: 38092421]
DU-145	EC₅₀	13.8 nM Compound: YM155	Cytotoxicity against human DU145 cells by MTT assay Cytotoxicity against human DU145 cells by MTT assay	[PMID: 28774426]
DU-145	IC₅₀	0.004 μM Compound: 1; YM155	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability by SRB assay	[PMID: 38092421]
HeLa	IC₅₀	1.8 μM Compound: YM155	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
HepG2	IC₅₀	3.72 μM Compound: YM155	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
HUVEC	IC₅₀	0.5 nM Compound: YM155	Antiangiogenic activity in HUVEC Antiangiogenic activity in HUVEC	[PMID: 28814374]
HUVEC	IC₅₀	0.5 nmol Compound: YM155	Antiangiogenic activity in HUVEC Antiangiogenic activity in HUVEC	[PMID: 28814374]
HUVEC	IC₅₀	0.92 μM Compound: YM155	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
MCF7	IC₅₀	0.01 μM Compound: YM155	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
MDA-MB-435	IC₅₀	>1 μM Compound: YM-155	Antiproliferative activity against human MDA-MB-435/LCC6MDR cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-435/LCC6MDR cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 34371464]
MDA-MB-435	IC₅₀	2.4 μM Compound: YM-155	Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 34371464]
MRC5	IC₅₀	1.94 μM Compound: YM155	Antiproliferative activity against human MRC5 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MRC5 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
NCI-H1299	IC₅₀	0.12 μM Compound: YM155	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
NCI-H460	IC₅₀	0.1 μM Compound: YM155	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
NIH3T3	IC₅₀	13.6 μM Compound: YM155	Antiproliferative activity against mouse NIH3T3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against mouse NIH3T3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
PANC-1	IC₅₀	0.01 μM Compound: YM155	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
PC-3	EC₅₀	92 nM Compound: YM155	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 28774426]
SK-MEL-5	IC₅₀	0.004 μM Compound: 1; YM155	Antiproliferative activity against human SK-MEL-5 cells assessed as reduction in cell viability Antiproliferative activity against human SK-MEL-5 cells assessed as reduction in cell viability	[PMID: 38092421]
TE-1	IC₅₀	0.008 μM Compound: YM155	Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 38079530]
Vero C1008	CC₅₀	400 μM Compound: 27; YM155	Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay	[PMID: 35620927]

体外実験

Sepantronium bromide (YM155; 30 μM) is not sensitive to survivn gene promoter-driven luciferase reporter activity. Sepantronium bromide shows significant supression on endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 via transcriptional inhibition of the survivin gene promoter. Sepantronium bromide (100 nM) does not affect protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin. Sepantronium bromide potently inhibits human cancer cell lines (mutated or truncated p53) such as PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC₅₀s ranging from 2.3 to 11 nM, respectively^[1].
Sepantronium bromide (YM155) resultin in an increase in sensitivity of NSCLC cells to γ-radiation. Sepantronium bromide combined with γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. In addition, Sepantronium bromide delays the repair of radiation-induced double-strand breaks in nuclear DNA^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Sepantronium bromide (YM155; 3 and 10 mg/kg) inhibits the tumor growth in PC-3 xenografts, without obvious body weight loss and blood cell count decrease. Sepantronium bromide is highly distributed to tumor tissue in vivo. Sepantronium bromide shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts^[1].
Sepantronium bromide (YM155) in combination with γ-radiation shows potent antitumor activity against H460 or Calu6 xenografts in nude mice^[2].
In this orthotopic renal and metastatic lung tumors models, Sepantronium bromide (YM-155) and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

443.29

分子式

C₂₀H₁₉BrN₄O₃

CAS 番号

781661-94-7

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C2=C(C(C3=CC=CC=C31)=O)[N+](CC4=NC=CN=C4)=C(C)N2CCOC.[Br-]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

H₂O : 50 mg/mL (112.79 mM; Need ultrasonic)

DMSO : 11.67 mg/mL (26.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2559 mL	11.2793 mL	22.5586 mL
5 mM	0.4512 mL	2.2559 mL	4.5117 mL
10 mM	0.2256 mL	1.1279 mL	2.2559 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2 mg/mL (4.51 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (112.79 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.36%

Select Batch:

データシート (286 KB) SDS (393 KB)

COA (257 KB) HNMR (265 KB) RP-HPLC (245 KB) LCMS (87 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Nakahara T, et al. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer Res. 2007 Sep 1;67(17):8014-21. [Content Brief]

[2]. Iisa T, et al. Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. [Content Brief]

[3]. Guo K, et al. A combination of YM-155, a small molecule survivin inhibitor, and IL-2 potently suppresses renal cell carcinoma in murine model. Oncotarget. 2015 Aug 28;6(25):21137-47. [Content Brief]

細胞実験 ^[1]	The antiproliferative activity of Sepantronium bromide is measured. After treatment with Sepantronium bromide for 48 h, the cell count is determined by sulforhodamine B assay. The GI₅₀ value is calculated by logistic analysis, which is the drug concentration resulting in a 50% reduction in the net protein increase (as measured by sulforhodamine B staining) in control cells during the drug incubation. The assay is done in triplicate, and the mean GI₅₀ value is obtained from the results of four independent assays. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Five-week-old male nude mice (BALB/c nu/nu) are used for the assay. PC-3 cells (2×10⁶-3×10⁶) are injected into the flanks of the mice and allowed to reach a tumor volume of > 100 mm³ in tumor volume (length×width²×0.5). Sepantronium bromide is s.c. administered as a 3-day continuous infusion per week for 2 weeks using an implanted micro-osmotic pump or i.v. administered five times a week for 2 weeks. The percentage of tumor growth inhibition 14 days after initial Sepantronium bromide administration is calculated for each group using the following formula: MTV=100×{1-[(MTV of the treated group on day 14)-(MTV of the treated group on day 0)]/[(MTV of the control group on day 14)-(MTV of the control group on day 0)]}, where MTV is mean tumor volume. For both the frozen tumors and plasma samples, survivin expression levels are analyzed by Western blotting and Sepantronium bromide concentration by high-performance liquid chromatography/triple quadrupole mass spectrometry (LC/MS/MS) using validated methods. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Nakahara T, et al. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer Res. 2007 Sep 1;67(17):8014-21. [Content Brief] [2]. Iisa T, et al. Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. [Content Brief] [3]. Guo K, et al. A combination of YM-155, a small molecule survivin inhibitor, and IL-2 potently suppresses renal cell carcinoma in murine model. Oncotarget. 2015 Aug 28;6(25):21137-47. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.2559 mL	11.2793 mL	22.5586 mL	56.3965 mL
	5 mM	0.4512 mL	2.2559 mL	4.5117 mL	11.2793 mL
	10 mM	0.2256 mL	1.1279 mL	2.2559 mL	5.6396 mL
	15 mM	0.1504 mL	0.7520 mL	1.5039 mL	3.7598 mL
	20 mM	0.1128 mL	0.5640 mL	1.1279 mL	2.8198 mL
	25 mM	0.0902 mL	0.4512 mL	0.9023 mL	2.2559 mL
H₂O	30 mM	0.0752 mL	0.3760 mL	0.7520 mL	1.8799 mL
	40 mM	0.0564 mL	0.2820 mL	0.5640 mL	1.4099 mL
	50 mM	0.0451 mL	0.2256 mL	0.4512 mL	1.1279 mL
	60 mM	0.0376 mL	0.1880 mL	0.3760 mL	0.9399 mL
	80 mM	0.0282 mL	0.1410 mL	0.2820 mL	0.7050 mL
	100 mM	0.0226 mL	0.1128 mL	0.2256 mL	0.5640 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Sepantronium bromide Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sepantronium781661-94-7YM-155YM155YM 155SurvivinAutophagyInhibitorinhibitorinhibit

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Sepantronium (bromide) (Synonyms: YM-155)

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Sepantronium (bromide) 関連抗体

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•関連小分子:

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Sepantronium (bromide) 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Sepantronium bromide Related Classifications

Molarity Calculator

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The molarity calculator equation

The dilution calculator equation

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