| Identification | Back Directory | [Name]
NSC305787 (hydrochloride) | [CAS]
53868-26-1 | [Synonyms]
NSC-305787 HCl
NSC305787 (hydrochloride) | [Molecular Formula]
C25H31Cl3N2O | [MDL Number]
MFCD29924224 | [MOL File]
53868-26-1.mol | [Molecular Weight]
481.89 |
| Hazard Information | Back Directory | [Uses]
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. | [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) | [storage]
Store at -20°C | [References]
[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. DOI:10.1038/onc.2011.245
[2] ?elik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70. DOI:10.1074/jbc.M116.718189 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
www.biorbyt.com |
|