产品
编 号:F643522
分子式:C52H60Br2NOP
分子量:905.82
产品类型
结构图
CAS No: 1634624-73-9
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产品详情
生物活性:
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.
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 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 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:FVB/N c-neu mouse
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
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.
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 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 cells