| Identification | Back Directory | [Name]
NSC668394 | [CAS]
382605-72-3 | [Synonyms]
NSC668394
5,8-Quinolinedione, 7-[[2-(3,5-dibromo-4-hydroxyphenyl)ethyl]amino]- | [Molecular Formula]
C17H12Br2N2O3 | [MDL Number]
MFCD28160708 | [MOL File]
382605-72-3.mol | [Molecular Weight]
452.1 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 3.85 mg/mL (8.52 mM; ultrasonic and warming and heat to 80°C) | [form ]
Solid | [color ]
Orange to red | [InChIKey]
OHPHDPYJEHZGDE-UHFFFAOYSA-N | [SMILES]
O=C1C=C(NCCC2=CC(Br)=C(O)C(Br)=C2)C(C3=C1C=CC=N3)=O |
| Hazard Information | Back Directory | [Uses]
NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis[1][2][3]. | [Biological Activity]
NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis[1][2][3].
NSC668394 (10 μM; pretreated for 15 min) inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and actin binding in vitro[1].NSC668394 (1-10 μM; 2-6 h) inhibits ezrin-mediated invasion by K7M2 osteosarcoma (OS) cells on the HUVEC monolayer[1].NSC668394 (20 μM) causes significant decrease in growth in JM1 and JM2 rat hepatoma cell lines[2].NSC668394 (10 μM) reduces cell motility phenotypes in zebrafish[1].
NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung[1]. | [in vivo]
NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung[1].
| Animal Model: | Female BALB/c and SCID/Beige mice were injected with K7M2 or MNNG-HOS tumor cells[1] | | Dosage: | 0.226 mg/kg/day | | Administration: | I.p. 5-days a week for 66 days | | Result: | Showed an increase in survival.
Decreased the number of the green fluorescent protein (GFP)-expressing metastatic foci in the lung tissues.
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| [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. [2]. Xue Y, et, al. Phosphorylated Ezrin (Thr567) Regulates Hippo Pathway and Yes-Associated Protein (Yap) in Liver. Am J Pathol. 2020 Jul;190(7):1427-1437. [3]. ?elik H, et, al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70. |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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