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OTSSP167
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
OTSSP167图片
CAS NO:1431697-89-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
OTS167
产品介绍
OTSSP167 (OTS167) 是一种高效的,ATP 竞争性的MELK抑制剂,IC50值为 0.41 nM。
生物活性

OTSSP167 (OTS167) is a highly potent and ATP-competitiveMELKinhibitor withIC50value of 0.41 nM.

IC50& Target

IC50: 0.41 nM (MELK)

体外研究
(In Vitro)

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. 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[2]. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC50of 0.41 nM[3].

体内研究
(In Vivo)

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[1].

分子量

487.42

Formula

C25H28Cl2N4O2

CAS 号

1431697-89-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vivo:
  • 1.

    OTSSP167 is prepared in vehicle (PBS)[4].