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

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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Based on 1 publication(s) in Google Scholar

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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].

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[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].

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[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.
Appearance

Solid

Color

White to light yellow

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-]

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 : 100 mg/mL (100.02 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 1.0002 mL 5.0009 mL 10.0018 mL
5 mM 0.2000 mL 1.0002 mL 2.0004 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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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.83%

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 1.0002 mL 5.0009 mL 10.0018 mL 25.0045 mL
5 mM 0.2000 mL 1.0002 mL 2.0004 mL 5.0009 mL
10 mM 0.1000 mL 0.5001 mL 1.0002 mL 2.5005 mL
15 mM 0.0667 mL 0.3334 mL 0.6668 mL 1.6670 mL
20 mM 0.0500 mL 0.2500 mL 0.5001 mL 1.2502 mL
25 mM 0.0400 mL 0.2000 mL 0.4001 mL 1.0002 mL
30 mM 0.0333 mL 0.1667 mL 0.3334 mL 0.8335 mL
40 mM 0.0250 mL 0.1250 mL 0.2500 mL 0.6251 mL
50 mM 0.0200 mL 0.1000 mL 0.2000 mL 0.5001 mL
60 mM 0.0167 mL 0.0833 mL 0.1667 mL 0.4167 mL
80 mM 0.0125 mL 0.0625 mL 0.1250 mL 0.3126 mL
100 mM 0.0100 mL 0.0500 mL 0.1000 mL 0.2500 mL
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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.

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MitoTam iodide, hydriodide
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