标签归档：mtor

PI3K/mTOR Inhibitor-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-2  纯度: 98.25%

PI3K/mTOR Inhibitor-2 是一种有效的双重 pan-PI3K/mTOR 抑制剂，抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ 的 IC50 值为 3.4/34/16/1 nM，mTOR 的 IC50 值为 4.7 nM。抗肿瘤活性。

PI3K/mTOR Inhibitor-2

PI3K/mTOR Inhibitor-2 Chemical Structure

CAS No. : 1848242-58-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PI3K/mTOR Inhibitor-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR[1]. Antitumor activity[1].

IC50 & Target[1]

PI3Kα

3.4 nM (IC50)

PI3Kβ

34 nM (IC50)

PI3Kδ

16 nM (IC50)

PI3Kγ

1 nM (IC50)

mTOR

4.7 nM (IC50)

体外研究
(In Vitro)

PI3K/mTOR Inhibitor-2 (Compound 31) inhibits p-AKT and p-p70s6k in MCF-7 cells with IC50s of 11.6 and 89.2 nM, respectively[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.
分子量

478.86

Formula

C20H13ClF2N4O4S
CAS 号

1848242-58-9
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 : 8.33 mg/mL (17.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0883 mL 10.4415 mL 20.8829 mL
5 mM 0.4177 mL 2.0883 mL 4.1766 mL
10 mM 0.2088 mL 1.0441 mL 2.0883 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。
参考文献

  • [1]. Yu T, et al. Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR. ACS Med Chem Lett. 2018 Feb 27;9(3):256-261.

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mTOR inhibitor-8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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  

* Please select Quantity before adding items.

mTOR inhibitor-8 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/mTOR Inhibitor-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-3 

PI3K/mTOR Inhibitor-3 (化合物 12) 是一种咪唑并喹啉类化合物，是有效的 PI3K 和 mTOR 双重抑制剂。PI3K/mTOR Inhibitor-3 具有抗癌活性。

PI3K/mTOR Inhibitor-3

PI3K/mTOR Inhibitor-3 Chemical Structure

CAS No. : 1363338-53-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity[1].

IC50 & Target[1]

PI3K

 

mTOR

 

分子量

373.45

Formula

C22H23N5O
CAS 号

1363338-53-7
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]. Zhenhua Huang. Double inhibitors of PI3K and mTOR of imidazoline. CN102372711A.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/mTOR Inhibitor-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-3 

PI3K/mTOR Inhibitor-3 (化合物 12) 是一种咪唑并喹啉类化合物，是有效的 PI3K 和 mTOR 双重抑制剂。PI3K/mTOR Inhibitor-3 具有抗癌活性。

PI3K/mTOR Inhibitor-3

PI3K/mTOR Inhibitor-3 Chemical Structure

CAS No. : 1363338-53-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity[1].

IC50 & Target[1]

PI3K

 

mTOR

 

分子量

373.45

Formula

C22H23N5O
CAS 号

1363338-53-7
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]. Zhenhua Huang. Double inhibitors of PI3K and mTOR of imidazoline. CN102372711A.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/mTOR Inhibitor-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-3 

PI3K/mTOR Inhibitor-3 (化合物 12) 是一种咪唑并喹啉类化合物，是有效的 PI3K 和 mTOR 双重抑制剂。PI3K/mTOR Inhibitor-3 具有抗癌活性。

PI3K/mTOR Inhibitor-3

PI3K/mTOR Inhibitor-3 Chemical Structure

CAS No. : 1363338-53-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity[1].

IC50 & Target[1]

PI3K

 

mTOR

 

分子量

373.45

Formula

C22H23N5O
CAS 号

1363338-53-7
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]. Zhenhua Huang. Double inhibitors of PI3K and mTOR of imidazoline. CN102372711A.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务