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53868-26-1

中文名稱 NSC305787 HYDROCHLORIDE
英文名稱 NSC305787 (hydrochloride)
CAS 53868-26-1
分子式 C25H31Cl3N2O
分子量 481.89
MOL 文件 53868-26-1.mol
53868-26-1 結(jié)構(gòu)式 53868-26-1 結(jié)構(gòu)式

基本信息

中文別名
PKC抑制劑(NSC305787 HYDROCHLORIDE)
英文別名
NSC-305787 HCl
NSC305787 (hydrochloride)

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : 8 mg/mL (16.60 mM)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
NSC305787 hydrochloride 是一種 ezrin 抑制劑,Kd 值為 5.85 μM,抑制 PKCΙ 導(dǎo)致的 ezrin 磷酸化,IC50 of 8.3 μM,具有抗腫瘤活性。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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.

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