MitoTam iodide, hydriodide

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MitoTam iodide, hydriodide 

MitoTam iodide, hydriodide 他莫昔芬衍生物，它是一种电子传递链 (ETC) 抑制剂，抑制衰老细胞中的线粒体膜电位变化并影响线粒体形态。 MitoTam iodide, hydriodide 是一种有效的抗癌剂。MitoTam iodide, hydriodide 抑制乳腺癌细胞中呼吸复合物 (CI- respiration) 和超复合物 (SCs) 的形成。 MitoTam iodide, hydriodide 可以诱导细胞凋亡 (apoptosis)。

MitoTam iodide, hydriodide

MitoTam iodide, hydriodide Chemical Structure

CAS No. : 1634624-74-0

规格 价格 是否有货
5 mg ￥5000 询问价格 & 货期
10 mg ￥8500 询问价格 & 货期
25 mg ￥18000 询问价格 & 货期
50 mg ￥30000 询问价格 & 货期
100 mg ￥46000 询问价格 & 货期

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生物活性

MitoTam iodide, hydriodide is a Tamoxifen derivative[1], an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology[2]. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells[1][2]. MitoTam iodide, hydriodide causes apoptosis[2].

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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
Concentration: 0.5 μM-56 μM
Incubation Time: 24 hours
Result: 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[2]

Cell Line: MCF7 mock and MCF7 Her2high 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 and decreased the antiapoptotic Bcl-2 protein in Her2high cells.

Apoptosis Analysis[2]

Cell Line: MCF-7, 4T1 and MCF-10a cells
Concentration: 0.05 μM-1 μM
Incubation Time: 3 days
Result: Resulted in apoptosis in MCF7 and 4T1 cells.

体内研究
(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 [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].

上海金畔生物科技有限公司 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 mice[1]
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[2]
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[1]
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.

分子量

999.82

Formula

C52H60I2NOP
CAS 号

1634624-74-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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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