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AZD-8055

产品编号 T1859 CAS 1009298-09-2

AZD-8055 是一种选择性、具有口服活性和 ATP 竞争性的 mTOR 抑制剂，IC50为 0.8 nM。AZD-8055 抑制 mTORC1和 mTORC2。

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AZD-8055, CAS 1009298-09-2

规格	价格/CNY	货期
1 mg	￥ 172	现货
5 mg	￥ 378	现货
10 mg	￥ 622	现货
25 mg	￥ 987	现货
50 mg	￥ 1,560	现货
100 mg	￥ 2,470	现货
200 mg	￥ 3,950	现货
500 mg	￥ 6,350	现货
1 mL * 10 mM (in DMSO)	￥ 418	现货

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其他形式的 AZD-8055:

AZD-8055 fumarate
询价

选择批次

纯度: 99.69%

纯度: 98.69%

纯度: 98%

纯度: 97.45%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
靶点活性	mTOR:0.8 nM (MDA-MB-468 cells)
体外活性	AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells [1]. In vitro, the median relative IC50 for AZD8055 against the PPTP cell lines was 24.7?nM. Relative I/O values >0% were observed in 8 cell lines and 15 cell lines showed Relative I/O values ranging from -4.7 to -92.2% [2].
体内活性	In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition [1]. AZD8055 administration could significantly decrease the IL-1β and TNF-α concentrations. Rats subjected to SAH + vehicle group demonstrated histological evidence of apoptosis compared with the sham group. The group treated with AZD8055 demonstrated a significant decrease in apoptosis ratio in the rat brain sample. In addition, in SAH group, the number of fluoro-jade B-positive cells clearly increased compared with the sham group. And the number of fluoro-jade B-positive cells decreased significantly in the SAH + rapamycin group and SAH + AZD8055 group [3].
激酶实验	The activity of mTOR was assayed using the recombinant mTOR technique described above. For inhibition experiments, AZD8055 was added to the reaction mixture and preincubated for 10 min before addition of ATP. Inhibition was performed at 1 to 3,000 nmol/L of AZD8055 in varying concentrations of ATP (40–200 μmol/L) [1].
细胞实验	For growth inhibition and acridine staining, cells were exposed to increasing concentrations of AZD8055 for 72 to 96 h and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images were captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells were quantified. For LC3 assessment, cells were exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells were lysed on ice and analyzed by immunoblotting [1].
动物实验	Tumor cells (10^6 for U87-MG, 5 × 10^6 for A549) were injected s.c. in a volume of 0.1 mL, and mice were randomized into control and treatment groups when tumor size reached 0.2 cm^3. AZD8055 was formulated in 30% (w/v) captisol (pH 3.0). The control group received the vehicle only. Tumor volumes (measured by caliper), animal body weight, and tumor condition were recorded twice weekly for the duration of the study. The tumor volume was calculated (taking length to be the longest diameter across the tumor and width to be the corresponding perpendicular diameter) using the following formula: (length × width) × √(length × width) × (π/6) [1].

分子量	465.54
分子式	C25H31N5O4
CAS No.	1009298-09-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 3 mg/mL (6.44 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 47 mg/mL (101 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.148 mL	10.7402 mL	21.4804 mL	53.7011 mL
Ethanol / DMSO	5 mM	0.4296 mL	2.148 mL	4.2961 mL	10.7402 mL
DMSO	10 mM	0.2148 mL	1.074 mL	2.148 mL	5.3701 mL
	20 mM	0.1074 mL	0.537 mL	1.074 mL	2.6851 mL
	50 mM	0.043 mL	0.2148 mL	0.4296 mL	1.074 mL
	100 mM	0.0215 mL	0.1074 mL	0.2148 mL	0.537 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Chresta CM, et al. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res, 2010, 70(1), 288-298. 2. Houghton PJ, et al. Initial testing (stage 1) of the mTOR kinase inhibitor AZD8055 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Feb;58(2):191-9. 3. You W, et al. Inhibition of mammalian target of rapamycin attenuates early brain injury through modulating microglial polarization after experimental subarachnoid hemorrhage in rats. J Neurol Sci. 2016 Aug 15;367:224-31. 4. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1–RIPK3–MLKL signal transduction in response to TNF receptor 1 ligation[J]. Journal of cell science. 2019 May 20;132(10). pii: jcs227777. 5. Xia Y, Chen J, Yu Y, et al. Compensatory combination of mTOR and TrxR inhibitors to cause oxidative stress and regression of tumors[J]. Theranostics. 2021, 11(9): 4335.

文献引用

1. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. Journal of Cell Science. 2019, 132(10): jcs227777 2. Xia Y, Chen J, Yu Y, et al. Compensatory combination of mTOR and TrxR inhibitors to cause oxidative stress and regression of tumors. Theranostics. 2021, 11(9): 4335. 3. Zhang W, Li X, Jiang M, et al.SOCS3 deficiency-dependent autophagy repression promote the survival of early-stage myeloid-derived suppressor cells in breast cancer by activating the Wnt/mTOR pathway.Journal of Leukocyte Biology.2023: qiad020.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AZD-8055 1009298-09-2 Apoptosis Autophagy PI3K/Akt/mTOR signaling mTOR AZD8055 inhibit Mammalian target of Rapamycin Inhibitor AZD 8055 inhibitor

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AZD-8055

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords