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编 号:F762944
分子式:C34H41NO7
分子量:575.69
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1mg
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5mg
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生物活性:
ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

体内研究:
ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.Animal Model:Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116and Notch1/HCT116 (C4) xenografts).
Dosage:5 mg/kg
Administration:i.p., thrice a week for 4 weeks
Result:Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

体外研究:
ASR-490 (0-1.6 μM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 μM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells).ASR-490 (750 nM in HCT116 cells and 1.2 μM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells.ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants.
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