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1431698-10-0

中文名稱 OTSSP 167 鹽酸鹽
英文名稱 OTSSP167HCL
CAS 1431698-10-0
分子式 C25H29Cl3N4O2
分子量 523.882
MOL 文件 1431698-10-0.mol
更新日期 2024/12/24 22:28:11
1431698-10-0 結構式 1431698-10-0 結構式

基本信息

中文別名
OTSSP 167 鹽酸鹽
英文別名
OTSSP167HCL
OTS-167 hydrochloride
OTSSP167 HCl (OTS167 HCl)
MELK INHIBITOR
OTSSP-167
OTSSP 167
OTSSP167hydrochloride/OTSSP-167hydrochloride
1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone hydrochloride
Ethanone,1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-,hydrochloride(1:1)
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)結晶固體
顏色Light yellow to gray

常見問題列表

生物活性
OTSSP167 hydrochloride 是一種高效的,ATP 競爭性的 MELK 抑制劑,IC50 值為 0.41 nM。
靶點

IC50: 0.41 nM (MELK)

體外研究

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC 50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively. OTSSP167 can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells. OTSSP167 causes GFP-MELK localization to cell cortex in prometaphase cells. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC 50 of 0.41 nM.

體內(nèi)研究

OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts.

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