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编 号:F643521
分子式:C52H60I2NOP
分子量:999.82
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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 .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 Her2high carcinomas decreased threefold from the original size with complete disappearance.Animal Model:18-month-old or 2-month-old FVB/N mice
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
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
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.

体外研究:
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.MitoTam (2.5 μM; 2-24 hours) results in stronger activation of the apoptotic pathway in MCF7 Her2high 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 cells.
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