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编 号:F124782
分子式:C18H19NO7
分子量:361.35
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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:
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29?μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52?μM and unstresses RPMI 8226 cells with an IC50 of 0.14?μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.

体内研究:
MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal.Animal Model:Female athymic nude mice with MDA-MB-231 tumor
Dosage:300 mg/kg
Administration:Oral; for 28 days
Result:Reduced tumor regrowth post-NSC 125973 withdrawal.

体外研究:
MKC8866 (20?μM; 6 days) decreases proliferation of all breast cancer cell lines.?MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase.?MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells.?MKC8866 (20 μM; 72?hours) is sufficient to completely block NSC 125973-induced expression of XBP1s .
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