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MitoTam bromide, hydrobromide is a tamoxifen analogue acting as an electron transport chain (ETC) inhibitor with anticancer activity. It reduces mitochondrial membrane potential in senescent cells, causes apoptosis and affects mitochondrial morphology.MitoTam iodide suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells.
| ln Vitro |
With an IC50 range of 0.65 μM to 55.9 μM, MitoTam (0.5 μM-56 μM; 24 hours) kills nonmalignant cells and breast cancer cell lines[1]. When compared to mock MCF7 cells, MitoTam (2.5 μM; 2-24 hours) causes a greater activation of the apoptotic pathway in MCF7 Her2 high cells[1]. Breast cancer cells undergo a concentration-dependent activation of apoptosis upon exposure to MitoTam (0.05 μM-1 μM; 3 days); non-malignant breast epithelial cells were unaffected[2].
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| ln Vivo |
When compared to control mice, MitoTam (intraperitoneal injection; 2 μg/g; once a week; 4 weeks) reduces the amount of β-gal staining in the lungs of the mice treated with it. This is accompanied by a suppression of the expression of senescence markers p16Ink4a, p21waf1, and PAI [2]. MitoTam, an intraperitoneal injection administered twice a week for two weeks at a dose of 0.54 μmol/mouse, reduces syngeneic tumor growth by 80%[1]. MitoTam, an intraperitoneal injection administered twice a week for two weeks at a concentration of 0.25 μmol/mouse, suppresses Her2high carcinomas, causing them to shrink three times their initial size and eventually disappear[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Breast Cancer Cell Types: 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 Tested Concentrations: 0.5 μM-56 μM Incubation Duration: 24 hrs (hours) Experimental Results: 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 Types: MCF7 mock cells, MCF7 Her2high cells Tested Concentrations: 2.5 μM Incubation Duration: 2 hrs (hours), 4 hrs (hours), 8 hrs (hours), 16 hrs (hours), 24 hrs (hours) Experimental Results: Revealed accelerated cleavage of procaspase-9, Parp1/2 and proapoptotic Bax, diminished the antiapoptotic Bcl-2 protein in Her2high cells. Apoptosis Analysis[2] Cell Types: MCF-7 cells, 4T1 cells and MCF-10a cells Tested Concentrations: 0.05 μM-1 μM Incubation Duration: 3 days Experimental Results: Resulted in apoptosis in MCF7 and 4T1 cells. |
| Animal Protocol |
Animal/Disease Models: 18-month-old or 2-month-old FVB/N mice [2]
Doses: 2 μg/g Route of Administration: intraperitoneal (ip)injection; 2 μg/g; once a week; 4 weeks Experimental Results: Eliminated senescent cells also in vivo. Animal/Disease Models: FVB/N c-neu mouse[1] Doses: 0.54 μmol/mouse Route of Administration: intraperitoneal (ip)injection; 0.54 μmol/mouse; twice a week; 2 weeks Experimental Results: Suppressed Her2high breast carcinomas. Animal/Disease Models: Balb/c nude mice with MCF7 mock or MCF7 Her2high cells[1] Doses: 0.25 μmol/mouse /dose Route of Administration: intraperitoneal (ip)injection; 0.25 μmol/mouse/dose; twice a week; 2 weeks Experimental Results: Prevented reaching the ethical endpoint in all situations, slowed down the growth of MCF7 mock tumors and suppressed Her2high carcinomas diminished. |
| References |
| Molecular Formula |
C52H59BRNOP
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|---|---|
| Molecular Weight |
824.908734560013
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| Exact Mass |
905.275
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| CAS # |
1634624-73-9
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| Related CAS # |
MitoTam iodide, hydriodide;1634624-74-0
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| PubChem CID |
86304737
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
57
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| Complexity |
984
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[P+](C1C=CC=CC=1)(C1C=CC=CC=1)(C1C=CC=CC=1)CCCCCCCCCC/C(/C1C=CC=CC=1)=C(\C1C=CC=CC=1)/C1C=CC(OCCN(C)C)=CC=1.[Br-]
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| InChi Key |
LKYHAJFFVLTBRB-DRFCFMONSA-M
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| InChi Code |
InChI=1S/C52H59NOP.2BrH/c1-53(2)41-42-54-47-39-37-46(38-40-47)52(45-28-16-10-17-29-45)51(44-26-14-9-15-27-44)36-24-7-5-3-4-6-8-25-43-55(48-30-18-11-19-31-48,49-32-20-12-21-33-49)50-34-22-13-23-35-50;;/h9-23,26-35,37-40H,3-8,24-25,36,41-43H2,1-2H3;2*1H/q+1;;/p-1/b52-51-;;
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| Chemical Name |
[(Z)-12-[4-[2-(dimethylamino)ethoxy]phenyl]-11,12-diphenyldodec-11-enyl]-triphenylphosphanium;bromide;hydrobromide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~240 mg/mL (~264.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2123 mL | 6.0613 mL | 12.1225 mL | |
| 5 mM | 0.2425 mL | 1.2123 mL | 2.4245 mL | |
| 10 mM | 0.1212 mL | 0.6061 mL | 1.2123 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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