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(Rac)-NSC305787 hydrochloride

CAS No. : 53868-26-1

MCE 国际站：(Rac)-NSC305787 hydrochloride

产品活性：NSC305787 hydrochloride 是一种 ezrin 抑制剂，K_d 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。

研究领域：Others

作用靶点：Others

In Vitro: 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 IC₅₀s 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.

In Vivo: 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/flpRB^fl/fl) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model.

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