mTOR inhibitor-8

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mTOR inhibitor-8  纯度: 98.04%

mTOR inhibitor-8 是一种 mTOR 抑制剂和自噬 (autophagy) 诱导剂。mTOR inhibitor-8 通过 FKBP12 抑制 mTOR 活性，并诱导 A549 人肺癌细胞自噬。

mTOR inhibitor-8

mTOR inhibitor-8 Chemical Structure

CAS No. : 2489196-70-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
25 mg ￥9500 In-stock
50 mg ￥14500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells[1].

IC50 & Target[1]

mTOR

 

Autophagy

 

体外研究
(In Vitro)

mTOR inhibitor-8 (Compound 5e; 0.1-10 μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner[1].
mTOR inhibitor-8 induces autophagy in an mTOR-dependent manner. mTOR inhibitor-8 (10 μM; 3-24 hours) induces autophagy in a time-dependent manner. The levels of LC3B-II are enhanced[1].
mTOR inhibitor-8 (10 μM; 3-24 hours) reduces the phosphorylation of RPS6KB1 (ribosomal protein S6 kinase) and EIF4EBP1 (eukaryotic translation initiation factor 4E-binding protein 1), two essential substrates of mTOR[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.

Cell Viability Assay[1]

Cell Line: A549 cells
Concentration: 0.1, 1, 5, 10 μM
Incubation Time: 24 and 48 hours
Result: Suppressed the growth of A549 cells with an IC50 of 2.6±0.11 μM.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 10 μM
Incubation Time: 3, 6, 12 and 24 hours
Result: The levels of phosphorylation of RPS6KB1 and EIF4EBP1 were significantly decreased after treatment.

体内研究
(In Vivo)

mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis[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: Fertile chicken eggs (7-9 days old)[1]
Dosage: 25 and 50 μM
Administration: 6 days
Result: Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs.

分子量

446.95

Formula

C24H19ClN4OS
CAS 号

2489196-70-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (55.93 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2374 mL 11.1869 mL 22.3739 mL
5 mM 0.4475 mL 2.2374 mL 4.4748 mL
10 mM 0.2237 mL 1.1187 mL 2.2374 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.65 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.65 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. ZhaoMin Lin, et al. Discovery of new fluorescent thiazole-pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells. Cell Death Dis. 2020 Jul 20;11(7):551.

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