MitoTam bromide, hydrobromide

MitoTam bromide, hydrobromide, a Tamoxifen derivative, is an electron transport chain ( ETC ) inhibitor. MitoTam bromide, hydrobromide reduces 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. In Vitro MitoTam (0.5 μM-56 μM; 24 hours) kills breast cancer cell Lines and nonmalignant cells with an IC 50 range from 0.65 μM to 55.9 μM. MitoTam (2.5 μM; 2-24 hours) results in stronger activation of the apoptotic pathway in MCF7 Her2 high cells compared with mock MCF7 cells. 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 cellsMCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Breast Cancer Cell Lines: BT474, MCF7, MCF7 Her2 high , MCF7 Her2 low , 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 Her2 high , MCF7 Her2 low with IC 50 values of 1.25 μM, 0.65 μM and 1.45 μM respectively. Western Blot AnalysisCell Line: MCF7 mock cells, MCF7 Her2 high 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 AnalysisCell 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>. MitoTam (intraperitoneal injection; 0.54 μmol/mouse; twice a week; 2 weeks) inhibits growth of syngeneic tumors by 80% . 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 Her2 high carcinomas decreased threefold from the original size with complete disappearance . 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 miceDosage: 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 Dosage: 0.54 μmol/mouse Administration: Intraperitoneal injection; 0.54 μmol/mouse; twice a week; 2 weeks Result: Suppressed Her2 high breast carcinomas. Animal Model: Balb/c nude mice with MCF7 mock or MCF7 Her2 high cells 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 Her2 high carcinomas decreased. Form:Solid

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