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ChemicalBook--->CAS DataBase List--->2378780-25-5

2378780-25-5

2378780-25-5 Structure

2378780-25-5 Structure
IdentificationBack Directory
[Name]

Nur77 antagonist 1
[CAS]

2378780-25-5
[Synonyms]

Nur77 antagonist 1
Hazard InformationBack Directory
[Uses]

Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells[1].
[in vivo]

Nur77 antagonist 1(Compound ja) (10 mg/kg, i.p) has excellent antitumor efficiency and good in vivo tolerance in the breast cancer MDA-MB-231 xenograft nude mice model[1].
Nur77 antagonist 1 (1.25-5 μM) has good in vivo safety in zebrafish embryo model[1].

Animal Model:the breast cancer MDA-MB-231 xenograft nude mice model[1]
Dosage:10 mg/kg
Administration:i.p
Result:Reduced tumor weight and volume with tumor growth inhibition (TGI) of 99.95%.
Increased cleaved caspase 3 and decreased the proliferation marker Ki67 expression in tumor tissues.
[IC 50]

Nur77/NR4A1
[References]

[1] Qin J, et al. Discovery of 5-(Pyrimidin-2-ylamino)-1H-indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer. J Med Chem. 2023 Nov 20. DOI:10.1021/acs.jmedchem.3c01336
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