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

生物活性靶点体外研究体内研究 3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐试剂级价格

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

3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐化学性质

储存条件 :2-8°C
溶解度 :DMSO: soluble20mg/mL, clear
形态 :powder
颜色 :white to beige

安全信息

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.