AES-350|cas:847249-57-4|西域试剂

AES-350,98.02%

产品编号：Bellancom-138831| CAS NO：847249-57-4| 分子式：C₁₈H₂₀N₂O₃| 分子量：312.36

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货号	价格	库存与货期
Bellancom-138831	￥3500.00	杭州北京（现货）
Bellancom-138831	￥5800.00	杭州北京（现货）
Bellancom-138831	￥11000.00	杭州北京（现货）
Bellancom-138831	￥0.00	杭州北京（现货）
Bellancom-138831	￥0.00	杭州北京（现货）

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AES-350

产品介绍

AES-350 是一种有效的口服活性 HDAC6 抑制剂，IC₅₀ 和 K_i 分别为 0.0244 μM 和 0.035 μM。AES-350 对 HDAC-3、-8 和 -11 的 IC₅₀ 值分别为 0.187 μM、0.245 μM。AES-350 通过抑制 HDAC 诱导 AML 细胞凋亡，可用于急性髓系白血病 (AML) 研究。

生物活性

AES-350 is a potent and orally active HDAC6 inhibitor with an IC₅₀ and a K_i of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

体外研究

In contrast, AES-350 has submicromolar activity (IC₅₀=0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC₅₀=0.31±0.061 μM). AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC₅₀>30 μM in noncancerous MRC-9 cells). AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC₅₀=0.73 ± 0.12 μM).
AES-350 (0.25-4 μM; 18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner. The late apoptosis ratios are 8.74%, 11.7%,16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM.
An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350. Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC₅₀=0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	MV4-11 cells
Concentration:	0.25 μM; 0.5 μM; 1.00 μM; 2.00 μM; 4.00 μM
Incubation Time:	18 hours
Result:	Revealed a clear dosedependent increase in the percentage of cells entering late-stage apoptosis, similar to SAHA.

体内研究
(In Vivo)

AES-350 (oral gavage; 20 mg/kg; single dose) exhibits a relative good pharmacokinetic (PK) properties in CD-1 mice. The single dose oral bioavailability (F%) of 51 is 19.8%. In comparison, the reported F% for SAHA in mice is significantly lower (8%).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (320.14 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2014 mL	16.0072 mL	32.0143 mL
5 mM	0.6403 mL	3.2014 mL	6.4029 mL
10 mM	0.3201 mL	1.6007 mL	3.2014 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 (protect from light)。-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: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。