3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐
![3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐,1449240-68-9,结构式](https://www.chemicalbook.com/CAS/20180713/GIF/1449240-68-9.gif)
- CAS号:1449240-68-9
- 英文名:K145 (hydrochloride)
- 中文名:3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐
- CBNumber:CB72677063
- 分子式:C18H25ClN2O3S
- 分子量:384.9207
- MOL File:1449240-68-9.mol
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble20mg/mL, clear
- 形态 :powder
- 颜色 :white to beige
- WGK Germany :3
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐性质、用途与生产工艺
- 生物活性 K145 hydrochloride 是一种选择性的，具有底物竞争性和口服活性的 SphK2 抑制剂，IC50 为 4.3 µM，Ki 为 6.4 µM。K145 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡，并具有强大的抗肿瘤活性。
-
靶点
IC50: 4.3 µM (SphK2)
Ki: 6.4 µM (SphK2) -
体外研究
K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells.
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels.Cell Viability Assay
Cell Line: U937 cells Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM Incubation Time: 24 hours, 48 hours, 72 hours Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Apoptosis Analysis
Cell Line: U937 cells Concentration: 10 µM Incubation Time: 24 hours Result: Significantly induced apoptosis in U937 cells. Western Blot Analysis
Cell Line: U937 cells Concentration: 4 µM, 8 µM Incubation Time: 3 hours Result: Phosphorylated ERK and Akt were decreased. -
体内研究
K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice.
Animal Model: BALB/c-nu mice injected with U937 cells Dosage: 50 mg/kg Administration: Oral gavage; daily; for 15 days Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
- 更新日期：2024/11/08
- 产品编号：HY-15779A
- 产品名称：3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐 K145 hydrochloride
- CAS编号：1449240-68-9
- 包装：5mg
- 价格：418元
- 更新日期：2024/11/08
- 产品编号：HY-15779A
- 产品名称：3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐 K145 hydrochloride
- CAS编号：1449240-68-9
- 包装：10mM * 1mLin DMSO
- 价格：459元
- 公司名称：A.J Chemicals
- 联系电话：--
- 电子邮件：sales@ajchem.in
- 国家：印度
- 产品数：6100
- 优势度：58
