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1449240-68-9

中文名稱 3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽
英文名稱 K145 (hydrochloride)
CAS 1449240-68-9
分子式 C18H25ClN2O3S
分子量 384.921
MOL 文件 1449240-68-9.mol
更新日期 2023/03/20 15:41:25
1449240-68-9 結(jié)構(gòu)式 1449240-68-9 結(jié)構(gòu)式

基本信息

中文別名
SPHK2抑制劑(K145鹽酸鹽)
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽
英文別名
K145(HCl)
SphK2 inhibitor
K14 (hydrochloride)
K145 (hydrochloride)
K145 hydrochloride >=98% (HPLC)
SPHK2 INHIBITOR
K 145 HYDROCHLORIDE
K-145 HYDROCHLORIDE
3-(2-Amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione hydrochloride
3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione hydrochloride (1:1)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

WGK Germany3
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽價格(試劑級)
報(bào)價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-15779A3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽
K145 hydrochloride
1449240-68-95mg418元
2024/11/08HY-15779A3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽
K145 hydrochloride
1449240-68-910mM * 1mLin DMSO459元
2024/11/08HY-15779A3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亞丙基]-2,4-噻唑烷二酮鹽酸鹽
K145 hydrochloride
1449240-68-910mg585元

常見問題列表

生物活性
K145 hydrochloride 是一種選擇性的,具有底物競爭性和口服活性的 SphK2 抑制劑,IC50 為 4.3 μM,Ki 為 6.4 μM。K145 hydrochloride 對 SphK1 和其他蛋白激酶沒有活性。K145 hydrochloride 可誘導(dǎo)細(xì)胞凋亡,并具有強(qiáng)大的抗腫瘤活性。
靶點(diǎn)

IC50: 4.3 μM (SphK2)
Ki: 6.4 μM (SphK2)

體外研究

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.
體內(nèi)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.
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