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

MitoTam bromide, hydrobromide 

Cat. No.: HY-126222
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MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces 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. MitoTam bromide, hydrobromide causes apoptosis.

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MitoTam bromide, hydrobromide Chemical Structure

MitoTam bromide, hydrobromide Chemical Structure

CAS No. : 1634624-73-9

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Description

MitoTam bromide, hydrobromide is a tamoxifen derivative[1], an electron transport chain (ETC) inhibitor, spreduces 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]. MitoTam bromide, hydrobromide causes apoptosis[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 Her2high 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]

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].

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.

1634624-73-9

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.[H]Br.[Br-]

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MitoTam bromide,ApoptosisMitochondrial MetabolismInhibitorinhibitorinhibit

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