规格

价格

库存

数量

1 mg

¥ 172

现货

5 mg

¥ 378

现货

10 mg

¥ 619

现货

25 mg

¥ 987

现货

50 mg

¥ 1,550

现货

100 mg

¥ 2,470

现货

200 mg

¥ 3,930

现货

1 mL x 10 mM (in DMSO)

¥ 389

现货

生物活性

产品描述	AZD-8055 is an orally bioavailable, highly selective, ATP-competitive mTOR kinase inhibitor that directly binds to the ATP-binding pocket of the mTOR kinase domain, while potently inhibiting both mTORC1 and mTORC2 complexes (IC₅₀ values of 0.8 nM and 0.1 nM, respectively). AZD-8055 is suitable for research in oncology, metabolic diseases, and fibrotic disorders.
靶点活性	mTOR:0.8 nM (MDA-MB-468 cells)
体外活性	方法：Huh7 人肝癌细胞转染 HPCAL1 敲低（shRNA），转染后加入梯度浓度 AZD-8055 （0， 10， 50， 100， 500 nM），药物处理 72 小时，CCK-8 法检测细胞活力。结果：HPCAL1 敲低细胞对 AZD-8055 的敏感性增加（细胞活力更低）。[1] 方法：葡萄膜黑色素瘤细胞系：92.1， Mel202， MP38， MP41，加入 AZD-8055 （1 μM）和罗米地辛（25 ng/mL），罗米地辛处理 6 小时后更换新鲜培养基，继续培养至 48 小时，流式细胞术（Annexin V/SYTOX Green 染色）检测细胞凋亡。结果：AZD-8055 与罗米地辛联合在所有四种细胞系中均诱导了最高水平的凋亡，效果优于其他组合。[2]
体内活性	方法：通过 hydrodynamic tail-vein injection 构建的 MYC/Trp53⁻/⁻ 肝癌模型，同时使用 CRISPR/Cas9 敲除 Hpcal1(sgHpcal1)或对照(sgCON)，构建成功后腹腔注射 AZD-8055 (10 mg/kg/天，每日一次)，持续给药 30 天。结果：AZD-8055 治疗使 sgHpcal1 小鼠的肿瘤负荷显著降低，效果优于 sgCON 组。[1]
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].

化学信息

分子量	465.54
分子式	C₂₅H₃₁N₅O₄
CAS No.	1009298-09-2
Smiles	C[C@@H]1N(C=2C3=C(N=C(N2)N4[C@@H](C)COCC4)N=C(C=C3)C5=CC(CO)=C(OC)C=C5)CCOC1
密度	1.248

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

Ethanol: 3 mg/mL (6.44 mM), Sonication is recommended.

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

DMSO: 91 mg/mL (195.47 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.5 mg/mL (9.67 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1480 mL	10.7402 mL	21.4804 mL	107.4022 mL
5 mM	0.4296 mL	2.1480 mL	4.2961 mL	21.4804 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2148 mL	1.0740 mL	2.1480 mL	10.7402 mL
20 mM	0.1074 mL	0.5370 mL	1.0740 mL	5.3701 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1480 mL
100 mM	0.0215 mL	0.1074 mL	0.2148 mL	1.0740 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

AZD-8055

AZD-8055

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

AZD-8055

AZD-8055

AZD-8055 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词