HJC0152 hydrochloride
(Synonyms: 2-(2-氨基乙氧基)-5-氯-N-(2-氯-4-硝基苯基)苯甲酰胺盐酸盐) 目录号 : GC32807
An orally bioavailable inhibitor of STAT3
Cas No.:1420290-99-8
Sample solution is provided at 25 µL, 10mM.
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HJC0152 is an orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 ?M, respectively, in MDA-MB-231 cells in a luciferase reporter assay).1 It reduces total STAT3 and phosphorylated STAT3 levels in MDA-MB-231 cells and inhibits nuclear translocation of phosphorylated STAT3. HJC0152 inhibits proliferation of MCF-7 and MDA-MB-231 breast cancer and AsPC-1 and PANC-1 pancreatic cancer cells (IC50s = 0.91, 1.64, 1.9, and 1.08 ?M, respectively). It also halts the cell cycle at the G0/G1 phase, induces apoptosis, and suppresses cell proliferation in human head and neck squamous cell carcinoma cells.2 HJC0152 (7.5 mg/kg, i.p. or 25 mg/kg, p.o.) inhibits tumor growth in an MDA-MB-231 breast cancer mouse xenograft model and in an orthotopic mouse model of squamous cell carcinoma.1,2
1.Chen, H., Yang, Z., Ding, C., et al.Discovery of O-alkylamino tethered niclosamide derivatives as potent and orally bioavailable anticancer agentsACS Med. Chem. Lett.4(2)180-185(2013) 2.Wang, Y., Wang, S., Wu, Y., et al.Suppression of the growth and invasion of human head and neck squamous cell carcinomas via regulating STAT3 signaling and the miR-21/β-catenin axis with HJC0152Mol. Cancer Ther.16(4)578-590(2017)
Cell experiment: | Breast cancer MDA-MB-231 cells are incubated in 6-well plates (2.5×105/well). Cells are then treated with DMSO, or HJC0152 hydrochloride (compound 11) at different concentrations for 48 h, and then both adherent and floating cells are collected, washed once with PBS. Resuspended cells are incubated with 100 μL PBS containing 1% BSA and 100 μL Annexin V and dead cell detection reagent at room temperature for 20 min. Apoptosis is measured immediately using the Muse Cell Analyzer with the MuseTM Apoptosis Kit[1]. |
Animal experiment: | in vivo administration.--> Fifty-four female nude mice are are used for orthotopic tumor studies at 4 to 6 weeks of age. The mice are maintained in a barrier unit with 12 h light-dark switch. Freshly harvested MDA-MB-231 cells (2.5×106 cells per mouse, resuspended in 100 μL PBS) are injected into the 3rd mammary fat pad of the mice, and then randomly assigned into 8 groups (5 to10 mice per group). For the intraperitoneal treatment experiment, the mice are treated daily with 2.5 mg/kg HJC0152 hydrochloride (compound 11) (Group A) or vehicle (Group D) when the tumor volume reaches 200 mm3. A Body weights and tumors volume are measured daily and tumor volume is calculated according to the formula V=0.5×L×W2, where L=length (mm) and W=width (mm)[1]. |
References: [1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185. | |
| Cas No. | 1420290-99-8 | SDF | |
| 别名 | 2-(2-氨基乙氧基)-5-氯-N-(2-氯-4-硝基苯基)苯甲酰胺盐酸盐 | ||
| Canonical SMILES | O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl | ||
| 分子式 | C15H14Cl3N3O4 | 分子量 | 406.65 |
| 溶解度 | DMSO : 6 mg/mL (14.75 mM) | 储存条件 | Store at -20°C |
| 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 | 2.4591 mL | 12.2956 mL | 24.5912 mL |
| 5 mM | 0.4918 mL | 2.4591 mL | 4.9182 mL |
| 10 mM | 0.2459 mL | 1.2296 mL | 2.4591 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet