1. Apoptosis Metabolic Enzyme/Protease
  2. Apoptosis Mitochondrial Metabolism
  3. MitoTam bromide, hydrobromide

MitoTam bromide, hydrobromide, a Tamoxifen derivative, is an electron transport chain (ETC) inhibitor. MitoTam bromide, hydrobromide reduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells.

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MitoTam bromide, hydrobromide Chemical Structure

MitoTam bromide, hydrobromide Chemical Structure

CAS No. : 1634624-73-9

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Based on 1 publication(s) in Google Scholar

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Description

MitoTam bromide, hydrobromide, a Tamoxifen derivative[1], is an electron transport chain (ETC) inhibitor. MitoTam bromide, hydrobromide reduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology[2]. MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells[1][2].

In Vitro

MitoTam (0.5 μM-56 μM; 24 hours) kills breast cancer cell Lines and nonmalignant cells with an IC50 range from 0.65 μM to 55.9 μM[1].
MitoTam (2.5 μM; 2-24 hours) results in stronger activation of the apoptotic pathway in MCF7 Her2 high cells compared with mock MCF7 cells[1].
MitoTam (0.05 μM-1 μM; 3 days) causes a concentration-dependent induction of apoptosis in breast cancer cells, while there was no effect for non-malignant breast epithelial cells[2]

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

Cell Viability Assay[1]

Cell Line: Breast Cancer Cell Lines: BT474, MCF7, MCF7 Her2high, MCF7 Her2low, MDA-MB-231, MDA-MB-436, MDA-MB-453, SK-BR-3, T47D; NeuTL cells; Nonmalignant Cells: A014578, H9c2 cells
Concentration: 0.5 μM-56 μM
Incubation Time: 24 hours
Result: Killed breast cancer cells MCF7, MCF7 Her2high, MCF7 Her2low with IC50 values of 1.25 μM, 0.65 μM and 1.45 μM respectively.

Western Blot Analysis[1]

Cell Line: MCF7 mock cells, MCF7 Her2high cells
Concentration: 2.5 μM
Incubation Time: 2 hours, 4 hours, 8 hours, 16 hours, 24 hours
Result: Revealed accelerated cleavage of procaspase-9, Parp1/2 and proapoptotic Bax, decreased the antiapoptotic Bcl-2 protein in Her2high cells.

Apoptosis Analysis[2]

Cell Line: MCF-7 cells, 4T1 cells and MCF-10a cells
Concentration: 0.05 μM-1 μM
Incubation Time: 3 days
Result: Resulted in apoptosis in MCF7 and 4T1 cells.
In Vivo

MitoTam (intraperitoneal injection; 2 μg/g; once a week; 4 weeks) decreases β-gal staining of lungs from MitoTam-treated mice, accompaning by a inhibition in the expression of senescence markers p16Ink4a, p21waf1 and PAI comparing control mice sup>[2].
MitoTam (intraperitoneal injection; 0.54 μmol/mouse; twice a week; 2 weeks) inhibits growth of syngeneic tumors by 80%[1].
MitoTam (intraperitoneal injection; 0.25 μmol/mouse; twice a week; 2 weeks) slows down the growth of MCF7 mock tumors and stops tumor progression after two doses; suppresses Her2high carcinomas decreased threefold from the original size with complete disappearance[1].

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

Animal Model: 18-month-old or 2-month-old FVB/N mice[2]
Dosage: 2 μg/g
Administration: Intraperitoneal injection; 2 μg/g; once a week; 4 weeks
Result: Eliminated senescent cells also in vivo.
Animal Model: FVB/N c-neu mouse[1]
Dosage: 0.54 μmol/mouse
Administration: Intraperitoneal injection; 0.54 μmol/mouse; twice a week; 2 weeks
Result: Suppressed Her2high breast carcinomas.
Animal Model: Balb/c nude mice with MCF7 mock or MCF7 Her2high cells[1]
Dosage: 0.25 μmol/mouse/dose
Administration: Intraperitoneal injection; 0.25 μmol/mouse/dose; twice a week; 2 weeks
Result: Prevented reaching the ethical endpoint in all situations, slowed down the growth of MCF7 mock tumors and suppressed Her2high carcinomas decreased.
Molecular Weight

905.82

Formula

C52H60Br2NOP

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(CCOC1=CC=C(/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)/CCCCCCCCCC[P+](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)C=C1)C.Br[H].[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 240 mg/mL (264.95 mM; Need ultrasonic; 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 1.1040 mL 5.5199 mL 11.0397 mL
5 mM 0.2208 mL 1.1040 mL 2.2079 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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1040 mL 5.5199 mL 11.0397 mL 27.5993 mL
5 mM 0.2208 mL 1.1040 mL 2.2079 mL 5.5199 mL
10 mM 0.1104 mL 0.5520 mL 1.1040 mL 2.7599 mL
15 mM 0.0736 mL 0.3680 mL 0.7360 mL 1.8400 mL
20 mM 0.0552 mL 0.2760 mL 0.5520 mL 1.3800 mL
25 mM 0.0442 mL 0.2208 mL 0.4416 mL 1.1040 mL
30 mM 0.0368 mL 0.1840 mL 0.3680 mL 0.9200 mL
40 mM 0.0276 mL 0.1380 mL 0.2760 mL 0.6900 mL
50 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5520 mL
60 mM 0.0184 mL 0.0920 mL 0.1840 mL 0.4600 mL
80 mM 0.0138 mL 0.0690 mL 0.1380 mL 0.3450 mL
100 mM 0.0110 mL 0.0552 mL 0.1104 mL 0.2760 mL
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  • Do most proteins show cross-species activity?

    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.

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MitoTam bromide, hydrobromide
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