AES-350
目录号 : GC48775
An inhibitor of class I and class IIb HDACs
Cas No.:847249-57-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AES-350 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.605, 0.187, and 0.245 µM for HDAC1, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.0244 and 0.899 µM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb HDACs over HDAC2, -4, -5, -7, -9, and -11 (IC50s = >1 µM for all). AES-350 is cytotoxic to MV4-11, MOLM-13, and MRC-9 cells (IC50s = 0.576, 6, and 33.2 µM, respectively). It induces apoptosis in MV4-11 cells in a concentration-dependent manner.
1.Shouksmith, A.E., Gawel, J.M., Nawar, N., et al.Class I/IIb-selective HDAC inhibitor exhibits oral bioavailability and therapeutic efficacy in acute myeloid leukemiaACS Med. Chem. Lett.11(1)56-64(2019)
| Cas No. | 847249-57-4 | SDF | |
| Canonical SMILES | CC(C)(C)C1=CC=C(C(NC2=CC=C(C(NO)=O)C=C2)=O)C=C1 | ||
| 分子式 | C18H20N2O3 | 分子量 | 312.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 1 mg/ml | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.201 mL | 16.0051 mL | 32.0102 mL |
| 5 mM | 0.6402 mL | 3.201 mL | 6.402 mL |
| 10 mM | 0.3201 mL | 1.6005 mL | 3.201 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia
ACS Med Chem Lett 2019 Dec 13;11(1):56-64.PMID:31938464DOI:PMC6956385
The HDAC inhibitor 4-tert-butyl-N-(4-(hydroxycarbamoyl)phenyl)benzamide (AES-350, 51) was identified as a promising preclinical candidate for the treatment of acute myeloid leukemia (AML), an aggressive malignancy with a meagre 24% 5-year survival rate. Through screening of low-molecular-weight analogues derived from the previously discovered novel HDAC inhibitor, AES-135, compound 51 demonstrated greater HDAC isoform selectivity, higher cytotoxicity in MV4-11 cells, an improved therapeutic window, and more efficient absorption through cellular and lipid membranes. Compound 51 also demonstrated improved oral bioavailability compared to SAHA in mouse models. A broad spectrum of experiments, including FACS, ELISA, and Western blotting, were performed to support our hypothesis that 51 dose-dependently triggers apoptosis in AML cells through HDAC inhibition.