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编 号:F217705
分子式:C27H27F2N7O5S2
分子量:631.67
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10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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生物活性:
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.

体外研究:
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Centrinone-B slightly binds to Aurora A and Aurora B, with Kis of 1239 nM and 5597.14 nM. Centrinone-B (LCR-323) exhibits >1000-fold selectivity for Plk4 over Aurora A/B in vitro and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone-B (LCR-323) (0-200 nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Inhibition of PLK4 by Centrinone-B (LCR-323) also induces apoptosis in human melanoma cell lines.
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