| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2469975-55-9 | [Synonyms]
Nur77 modulator 1
apoptosis,inhibit,Inhibitor,antitumor,Nur-77 modulator 1,tolerability,autophagy,stress,mitochondria,good
(E)-5-((8-Methoxy-2-methylquinolin-4-yl)amino)-N'-(4-(methylthio)benzylidene)-1H-indole-2-carbohydrazide
(E)-5-((8-Methoxy-2-methylquinolin-4-yl)amino)-N'-(4-(methylthio)benzylidene)-1H-indole-2-carbohydrazide | [Molecular Formula]
C28H25N5O2S | [MDL Number]
MFCD34167507 | [MOL File]
2469975-55-9.mol | [Molecular Weight]
495.6 |
| Hazard Information | Back Directory | [Uses]
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity[1]. | [in vivo]
Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability[1]. | Animal Model: | Nude mouse hepatoma HepG2 xenograft[1]. | | Dosage: | 10 and 20 mg/kg/day. | | Administration: | IP, once every day for 15 days. | | Result: | Lead to substantial suppression of tumor growth.
The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.
Exhibited almost no influence on the body weight of experimental mice.
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| [IC 50]
Nur77/NR4A1 | [References]
[1] Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608. DOI:10.1016/j.ejmech.2020.112608 |
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