TAK-960 dihydrochloride

TAK-960 二盐酸盐

TAK-960 dihydrochloride

T658934-5mg

5mg

≥99%

2-8°C储存,干燥

冰袋运输

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1) , with an IC 50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3 , with IC 50 s of 16.9 and 50.2 nM, respectively. TA Appearance:Solid IC50& Target:PLK1 0.8 nM (IC 50 ) PLK2 16.9 nM (IC 50 ) PLK3 50.2 nM (IC 50 ) FAK/PTK2 19.6 nM (IC 50 ) MLCK/MYLK 25.6 nM (IC 50 ) FES/FPS 58.2 nM (IC 50 ) In Vitro:TAK-960 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, In Vivo:TAK-960 dihydrochloride exhibits (10mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 dihydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits th Biological Activity:TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1) , with an IC 50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3 , with IC 50 s of 16.9 and 50.2 nM, respectively. TA

C27H36Cl2F3N7O3

634.52 g/mol

[H]Cl.O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F.[H]Cl

H2O : 10 mg/mL (15.76 mM; Need ultrasonic) DMSO : 3.23 mg/mL (5.09 mM; Need ultrasonic)