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编 号:F183362
分子式:C35H28N4O5
分子量:584.62
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1mg
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5mg
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生物活性:
Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription.

体内研究:
Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor.Animal Model:Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:50 mg/kg
Administration:Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.

体外研究:
Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC50 range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC50 of 780 nM in RXF 393 cells. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation. Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines.
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