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CAS No. : 934541-31-8
MCE 国际站:TAK-901
产品活性:TAK-901是多靶点的的极光激酶 (aurora)抑制剂,对极光激酶A和B的IC50 值分别为21 和15 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:Aurora Kinase
In Vitro: TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistent with Aurora B inhibition, TAK-901 suppresses cellular histone H3 phosphorylation and induces polyploidy. In various human cancer cell lines, TAK-901inhibits cell proliferation with effective concentration values from 40 to 500 nM. Examination of a broad panel of kinases in biochemical assays reveals inhibition of multiple kinases. However, TAK-901 potently inhibits only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2.
In Vivo: In rodent xenografts, TAK-901 exhibits potent activity against multiple human solid tumor types, and complete regression is observed in the ovarian cancer A2780 model. TAK-901 also displayed potent activity against several leukemia models. TAK-901 induces pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Anti-Blood Cancer Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | AAPK-25 | AT9283 | Aurora kinase inhibitor-3 | Aurora Kinases-IN-2 | ENMD-2076 Tartrate | Barasertib-HQPA | dAURK-4 | AMG 900 | SCH-1473759 | Aurora A inhibitor 1 | BI-847325 | CCT129202 | Tripolin A | ZM-447439 | LY3295668 | TAK-632 | Aurora inhibitor 1 | MK-8745 | Ilorasertib | JB170 | PHA-680632 | Aurora kinase inhibitor-8 | SNS-314 | Hesperadin | Tozasertib | Alisertib | Aurora A/PKC-IN-1 | Derrone | KW-2449
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