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编 号:F754907
分子式:C57H67N7O9
分子量:994.18
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生物活性:
Anticancer agent 84 is an anticancer agent. Anticancer agent 84 represses the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure. Anticancer agent 84 can be used for the research of cancer.

体内研究:
Anticancer agent 84 (i.p.; 2.5 mg/kg; daily; for 24 days) significantly inhibits tumor growth in the MDAMB-231 mouse xenograft model accompanied by c-MYC downregulation.Animal Model:BALB/C-nu/nu mice(female, five-week-aged, 10?12 g)
Dosage:2.5 mg/kg
Administration:intraperitoneally, daily, for 24 days
Result:Exhibited potent antitumor activity and could act as a c-MYC repressor in vivo.

体外研究:
Anticancer agent 84 has cytotoxicity in cancer cells (HepG2, MDA-MB-231) and normal cells (HBL-100) with IC50 values of 5.0 μM, 3.9 μM and >100 μM, respectively.Anticancer agent 84 displays good c-MYC G4 binding and stabilization abilities. Anticancer agent 84 blocks c-MYC transcription by targeting the promoter G4, leading to c-MYC-dependent cancer cell death in triple-negative breast cancer cell MDA-MB-23.Anticancer agent 84 (2 μM) significantly disrupts the binding of the three proteins (NM23-H2, BLM and DHX36) to c-MYC G4 with IC50 values of 0.16 μM, 2.3 μM and 7.0 μM, respectively.Anticancer agent 84 (0-5 μM) impacts c-MYC-related events in TNBC, including proliferation, invasion, cell cycle, and apoptosis.
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