BAY-299是一种有效的抑制剂,能抑制bromodomain和PHD指家族成员BRPF2以及TATA盒结合蛋白相关因子TAF1和TAF1L,其IC50分别为67 nM、8 nM和106 nM。
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BAY-299 is an effecitve inhibitor of the bromodomain and PHD finger family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L with IC50s of 67 nM, 8 nM, and 106 nM, respectively.
体外活性
BAY-299 inhibits the cells proliferation of NCI-H526, CHL-1, MOLM-13, MV4-11, 769-P, Jurkat, and 5637 with GI50s of 6860, 7400, 1060, 2630, 3210, 3900, and 7980 nM, respectively. BAY-299 blocks the interaction of BRPF2 BD with H4 and H3.3 with IC50s of 575 and 825 nM, respectively[1].
体内活性
The in vivo pharmacokinetic properties of BAY-299 in rats show are blood clearance is low (17% of hepatic blood flow), terminal half-life long to very long with t1/2 of 10 h, volume of distribution in steady-state high, and bioavailability high with F of 73%[1].
Cas No.
2080306-23-4
分子式
C25H23N3O4
分子量
429.47
别名
BAY-299
储存和溶解度
DMSO:25 mg/mL (58.21 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years