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编 号:F741766
分子式:C23H18FN3O2
分子量:387.41
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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:
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.

体内研究:
TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner.Animal Model:Six-week-old female NOD-SCID mice were injected with HCT116 cells
Dosage:100, 150 mg/kg
Administration:P.o. twice daily for 18 days
Result:Significantly inhibited tumor growth at a dose of 150 mg/kg.No obvious weight loss and no other side effects were observed.

体外研究:
TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively.TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively.TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells.TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells.TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells.TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells.
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