53868-26-1

中文名称 NSC305787 HYDROCHLORIDE

英文名称 NSC305787 (hydrochloride)

CAS 53868-26-1

分子式 C25H31Cl3N2O

分子量 481.89

MOL 文件 53868-26-1.mol

更新日期 2024/11/15 18:20:30

53868-26-1 结构式

基本信息物理化学性质 NSC305787 HYDROCHLORIDE价格(试剂级) 常见问题列表

基本信息

中文别名

PKC抑制剂(NSC305787 HYDROCHLORIDE)

英文别名

NSC-305787 HCl
NSC305787 (hydrochloride)

物理化学性质

储存条件-20°C储存

溶解度DMSO : 8 mg/mL (16.60 mM)

形态Solid

颜色White to off-white

NSC305787 HYDROCHLORIDE价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2025/02/08	HY-18931A	(Rac)-NSC305787 hydrochloride	53868-26-1	1 mg	1300元
2025/02/08	HY-18931A	NSC305787 HYDROCHLORIDE NSC305787 hydrochloride	53868-26-1	5mg	2900元
2025/02/08	HY-18931A	NSC305787 HYDROCHLORIDE NSC305787 hydrochloride	53868-26-1	10mM * 1mLin DMSO	3074元

常见问题列表

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.