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MedChemexpress LLC
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Product Name:NSC305787 (hydrochloride)
CAS:53868-26-1
Purity:>98% Package:3500RMB/5mg
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NSC305787 (hydrochloride) manufacturers
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| | NSC305787 (hydrochloride) Basic information |
| Product Name: | NSC305787 (hydrochloride) | | Synonyms: | NSC305787 (hydrochloride);NSC-305787 HCl;NSC305787 hydrochloride,NSC-305787 hydrochloride;(2-(Adamantan-1-yl)-6,8-dichloroquinolin-4-yl)(piperidin-2-yl)methanol hydrochloride | | CAS: | 53868-26-1 | | MF: | C25H31Cl3N2O | | MW: | 481.89 | | EINECS: | | | Product Categories: | | | Mol File: | 53868-26-1.mol |  |
| | NSC305787 (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 8 mg/mL (16.60 mM) | | form | Solid | | color | White to off-white |
| | NSC305787 (hydrochloride) Usage And Synthesis |
| Biological Activity | NSC305787 (hydrochloride) is an ezrin inhibitor with Kd value of 5.85 μM, inhibits PKCI-induced ezrin phosphorylation, IC50 of 8.3 μM, and has antitumor activity. | | in vitro | NSC305787 hydrochloride is an inhibitor of ezrin with a K d of 5.85 μM, and has antitumor activity. It inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC 50 s of 8.3, 9.4, 55, 58.9 μM, respectively. It 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 PKCI kinase activity. It (1, 10 μM) shows inhibitory activity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, it reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture. | | in vivo | NSC305787 (hydrochloride) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung. It 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. | | target | Kd: 5.85 μM (ezrin)
IC50: 8.3 μM (ezrin) |
| | NSC305787 (hydrochloride) Preparation Products And Raw materials |
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