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编 号:F626431
分子式:C18H14N4O
分子量:302.33
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.

体内研究:
MKI-1 (50 mg/kg, ip, twice a week) reduces tumor growth and enhances the radiosensitivity of BT549 xenograft model in response to 6 Gy irradiation compared with the control group, with no notable changes in body weight, suggesting the absence of gross toxicity in the treated mice.Animal Model:Five-week-old female BALB/c nude mice (BT549 cells).
Dosage:50 mg/kg.
Administration:Twice per week by intraperitoneal (i.p.) injection.
Result:Reduced tumor growth.

体外研究:
MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells.MKI-1 (100 μM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells.MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation.MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells.
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