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NSC305787 hydrochloride
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。
NSC305787 hydrochloride图片
CAS NO:53868-26-1
规格:98%
分子量:481.89
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
NSC305787hydrochloride是一种ezrin抑制剂,Kd值为5.85μM,抑制PKCΙ导致的ezrin磷酸化,IC50of8.3μM,具有抗肿瘤活性。
CAS:53868-26-1
分子式:C25H31Cl3N2O
分子量:481.89
纯度:98%
存储:Store at -20°C

Background:

NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.


NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC50s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a Kd 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[1].


NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung[1]. NSC305787 (240 μg/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mouse model of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model[2].


[1]. Bulut G, et al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81. [2]. ?elik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70.