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[CAS NO. 781661-94-7] Sepantronium bromide
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-10194 |
| Brand: | MCE |
| CAS: | 781661-94-7 |
Overview
| MDL | MFCD11983133 |
|---|---|
| Molecular Weight | 443.29 |
| Molecular Formula | C20H19BrN4O3 |
| SMILES | O=C1C2=C(C(C3=CC=CC=C31)=O)[N+](CC4=NC=CN=C4)=C(C)N2CCOC.[Br-] |
13 Publications Citing Use of MCE
- [1]Cancer Lett. 2018 Jul 1;425:54-64.
- [2]Cell Death Dis. 2020 Nov 15;11(11):982.
- [3]Cancers. 2019 Oct 14;11(10):1550.
- [4]Cancers. 2019 Jul 5;11(7):947.
- [5]Stem Cell Res Ther. 2020 Jun 10;11(1):229.
- [6]Nutrients. 2018 Mar 15;10(3). pii: E353.
- [7]Sci Rep. 2019 Aug 21;9(1):12149.
- [8]Toxicol Appl Pharmacol. 2020 Apr 17;397:115013.
- [9]Anticancer Res. 2019 Sep;39(9):4817-4828.
- [10]Anticancer Res. 2019 Feb;39(2):609-617.
- [11]Anticancer Res. 2018 Dec;38(12):6699-6706.
- [12]Research Square Preprint. 2021 Jul.
- [13]BMC Complement Med Ther. 2020 Sep 3;20(1):269.
IC50 & Target
IC50: 0.54 nM (Survivin) [1]
In Vitro
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 IC
50
s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00281541 | Astellas Pharma Inc|Astellas Pharma US, Inc. |
Melanoma
|
November 2005 | Phase 2 |
| NCT01007292 | Astellas Pharma Inc |
Non-Hodgkin´s Lymphoma
|
November 2009 | Phase 2 |
| NCT00498914 | Astellas Pharma Inc |
Lymphoma, Large-Cell, Diffuse|Lymphoma, B-Cell Refractory
|
June 2007 | Phase 2 |
| NCT00818480 | Astellas Pharma Inc |
Prostate Cancer|Melanoma|Non-Hodgkin´s Lymphoma
|
February 2006 | Phase 2 |
| NCT01038804 | Astellas Pharma Inc |
Breast Cancer
|
December 2009 | Phase 2 |
| NCT01009775 | Astellas Pharma Inc |
Melanoma
|
November 2009 | Phase 2 |
| NCT01100931 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
NSCLC|Solid Tumors
|
February 2010 | Phase 1|Phase 2 |
| NCT00514267 | Astellas Pharma Inc |
Prostate Cancer|Tumors
|
May 2007 | Phase 1|Phase 2 |
| NCT00257478 | Astellas Pharma Inc|Astellas Pharma US, Inc. |
Prostate Cancer|Cancer of Prostate|Prostatic Cancer|Cancer of the Prostate
|
Phase 2 | |
| NCT00328588 | Astellas Pharma Inc |
Lung Cancer|Cancer of Lung|Cancer of the Lung|Non-Small Cell Lung Carcinoma|Carcinoma, Non-Small Cell Lung
|
December 2006 | Phase 2 |
| NCT01023386 | Astellas Pharma Inc |
Cancer
|
November 2009 | Phase 1 |
| NCT05263583 | Cothera Bioscience, Inc |
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
|
March 1, 2022 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 112.79 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 112.79 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (112.79 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 2 mg/mL (4.51 mM); Clear solution; Need ultrasonic
References
- [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.
- [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.
- [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.
Synonyms
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