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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-BAY-958
BAY-958

Chemical Structure : BAY-958

CAS No.: 1335490-39-5

BAY-958 (BAY 958;BAY958;LDC526)

货号: PC-60539Not For Human Use, Lab Use Only.

BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.
    BAY-958 displays 52/82/291/>900/>900-fold selectivity compared to CDK2/1/4/6/7.
    BAY-958 exhibits good antiproliferative activity in vitro, for example against HeLa cells (IC50=1000 nM) and MOLM-13 cells (IC50=280 nM).
    BAY-958 displays efficient cytotoxic activity against CLL cells in vitro, decreases CLL MCL-1 protein levels and triggers apoptosis rather than inhibiting proliferation.
    BAY-958 decreases splenic human CLL numbers in xenografted NSG mice, shows significant CLL cell cytotoxicity in TCL1 transgenic mice.

    物理化学性质&存储条件

    分子量 389.405
    分子式 C17H16FN5O3S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (3-((4-(4-fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)phenyl)methanesulfonamide

    参考文献

    1. Lücking U, et al. ChemMedChem. 2017 Nov 8;12(21):1776-1793.

    2. Göthert JR, et al. Oncotarget. 2018 May 29;9(41):26353-26369.

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