NSC305787 HYDROCHLORIDE

中文名称:

NSC305787 HYDROCHLORIDE

中文同义词:

PKC抑制剂(NSC305787 HYDROCHLORIDE)

英文名称:

NSC305787 (hydrochloride)

英文同义词:

NSC305787 (hydrochloride);NSC-305787 HCl

CAS号:

53868-26-1

分子式:

分子量:

0

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

Mol File

生物活性

NSC305787 hydrochloride 是一种 ezrin 抑制剂，Kd 值为 5.85 μM，抑制 PKCΙ 导致的 ezrin 磷酸化，IC50 of 8.3 μM，具有抗肿瘤活性。

靶点

Kd: 5.85 μM (ezrin) IC50: 8.3 μM (ezrin)

体外研究

NSC305787 hydrochloride is an inhibitor of ezrin with a K d of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC 50 s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a K d value of 172.4 μM, and inhibits ezrin T567 phosphorylation primarily via its binding to ezrin and not through inhibition of PKCΙ kinase activity. NSC305787 (1, 10 μM) shows inhibitory activity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, NSC305787 (10 μM) reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture.

体内研究

NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung. NSC305787 (240 μg/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mouse model of osteosarcoma (Osx-Cre + p53 fl/fl pRB fl/fl ) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model.