AZD4320是BH-3的新型类似物，有效的BCL2/BCLxL的双重抑制剂。AZD4320对于KPUM-MS3，KPUM-UH1，和STR-428细胞系的IC50分别为26nM，17nM，和170nM。
AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
AZD4320 potently augments the antitumor effect of AZD5153 in double expressing lymphoma (DEL)- and double hit lymphoma (DHL)-derived cell lines in a dose-dependent manner. AZD4320 shows mostly synergistic, and at least additive, growth inhibitory effects on DEL- and DHL derived cell lines, and profoundly increases cells undergoing apoptosis in all three cell lines[1].
[1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.
Cell experiment: | Two DEL-derived cell lines, KPUM-MS3 and KPUM-UH1, and a DHL-derived cell line, STR-428 are used. To examine the combinatory growth inhibitory effects of AZD4320, cells are treated with five concentrations (0.25, 0.5, 1.0, 2.0, 4.0×IC50) for 72 h, and subjected to a modified MTT assay[1]. |
参考文献: [1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21. | |
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