| Identification | Back Directory | [Name]
MitoTam bromide, hydrobromide | [CAS]
1634624-73-9 | [Synonyms]
MitoTam bromide, hydrobromide | [Molecular Formula]
C52H59BrNOP | [MDL Number]
MFCD32197221 | [MOL File]
1634624-73-9.mol | [Molecular Weight]
824.93 |
| Hazard Information | Back Directory | [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].
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 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] | [Uses]
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 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. |
| [References]
[1]. Rohlenova K, et al. Selective Disruption of Respiratory Supercomplexes as a New Strategy to Suppress Her2highBreast Cancer. Antioxid Redox Signal. 2017 Jan 10;26(2):84-103.
[2]. Hubackova S, et al. Selective elimination of senescent cells by mitochondrial targeting is regulated by ANT2. Cell Death Differ. 2019 Jan;26(2):276-290. |
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