(Rac)-NSC305787 hydrochloride|53868-26-1|-陌孚医药/Medlife

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(Rac)-NSC305787 hydrochloride

目录号: PL08461 纯度: ≥99%

CAS No. :53868-26-1

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中文名称	(Rac)-NSC305787 hydrochloride
中文别名	NSC305787 (hydrochloride)
英文名称	(Rac)-NSC305787 hydrochloride
英文别名	NSC305787 (hydrochloride);NSC-305787 hydrochloride;(2-(adamantan-1-yl)-6,8-dichloroquinolin-4-yl)(piperidin-2-yl)methanol hydrochloride;(6, hydrochloride;NSC305787 hydrochloride;(Rac)-NSC305787 hydrochloride
Cas No.	53868-26-1
分子式	C₂₅H₃₁Cl₃N₂O
分子量	481.89
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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。
生物活性	NSC305787 hydrochloride is an inhibitor of ezrin with a K d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC 50 of 8.3 μM, has antitumor activity.
性状	Solid
IC50 & Target[1][2]	Kd: 5.85 μM (ezrin) IC50: 8.3 μM (ezrin)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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-Crep53pRB) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 8 mg/mL (16.60 mM; Need ultrasonic and warming)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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