Chemical Structure : BAY-958
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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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.
分子量 | 389.405 | |
分子式 | C17H16FN5O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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