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编 号:F315875
分子式:C18H16N2OS
分子量:308.4
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo.

体内研究:
INH1 (50 or 100 mg/kg, i.p., every other day/25 cycles) inhibits tumor outgrowth in a xenografted breast cancer model in nude mice.Animal Model:Xenografted nude mice breast cancer model.
Dosage:50 or 100 mg/kg.
Administration:I.P., every other day/25 cycles.
Result:Inhibited tumor growth.

体外研究:
INH1 (25 μM, 24 h) treatment resulted in reduced association of Hec1 with kinetochore and decrease of global Nek2 protein level.INH1 exhibits GI50 values of 10.5 μM (in MDA-MB-468 cells), 15 μM (in SKBR3 cells), 10.5 μM (in T47D cells), 20.5 μM (in MDA-MB-361 cells), 15 μM (in ZR-75-1 cells), 15 μM (in HBL 100 cells), 15.5 μM (in MDA-MB-435 cells), 11 μM (in HS578T cells) and 41 μM (in MCF10A cells), respectively.INH1 (5k) has an IC50 value of 176 nM in the dose-dependent transwell migration assays in MDA-MB-231 cells. INH1 (5k) substantially reduces cellular f-actin and prevented localization of fascin to actin-rich membrane protrusions.INH1 induces abnormal mitotic processes, as well as cell apoptosis.
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