1. Apoptosis
    Metabolic Enzyme/Protease
  2. Apoptosis
    Mitochondrial Metabolism
  3. MitoTam iodide, hydriodide

MitoTam iodide, hydriodide 

Cat. No.: HY-126222A
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MitoTam iodide, hydriodide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.

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MitoTam iodide, hydriodide Chemical Structure

MitoTam iodide, hydriodide Chemical Structure

CAS No. : 1634624-74-0

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Description

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

Cell Line: MCF7 mock and 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 and decreased the antiapoptotic Bcl-2 protein in Her2high cells.

Apoptosis Analysis[2]

Cell Line: MCF-7, 4T1 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 [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[1]
Dosage: 2 μg/g
Administration: Intraperitoneal injection; 2 μg/g; once a week; 4 weeks
Result: Eliminated senescent cells also in vivo.
Animal Model: 18-month-old or 2-month-old FVB/N mice[2]
Dosage: 0.54 μmol/mouse
Administration: Intraperitoneal injection; 0.54 μmol/mouse; twice a week; 2 weeks
Result: Suppressed Her2high breast carcinomas.
Animal Model: 18-month-old or 2-month-old FVB/N mice[1]
Dosage: 0.25 μmol/mouse
Administration: Intraperitoneal injection; 0.25 μmol/mouse; 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

999.82

Formula

C₅₂H₆₀I₂NOP

CAS No.

1634624-74-0

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]I.[I-]

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MitoTam iodide, hydriodide
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