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编 号:F311697
分子式:C14H14F3N5
分子量:309.29
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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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50mg
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生物活性:
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.

体内研究:
ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model.Animal Model:Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)
Dosage:25 mg/kg body weight
Administration:I.p; daily for 21 days
Result:Significantly reduced by about 60% the formation of total metastatic lung colonies.

体外研究:
ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM.ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner.ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells.ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest.ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells.
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