(Rac)-NSC305787 hydrochloride

CAS: 53868-26-1 F: C25H31Cl3N2O W: 481.89

NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by

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Bioactivity	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.
Target	Kd: 5.85 μM (ezrin)IC50: 8.3 μM (ezrin)
Invitro	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].
In Vivo	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].
Name	(Rac)-NSC305787 hydrochloride
CAS	53868-26-1
Formula	C25H31Cl3N2O
Molar Mass	481.89
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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]. Çelik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70.