AZD4320
目录号 : GC33255AZD4320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。
Cas No.:1357576-48-7
Sample solution is provided at 25 µL, 10mM.
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]. |
References: [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. |
Cas No. | 1357576-48-7 | SDF | |
Canonical SMILES | O=C(NS(=O)(C1=CC=C(N[C@H](CCN(CCO)C)CSC2=CC=CC=C2)C(S(=O)(C(F)(F)F)=O)=C1)=O)C3=CC=C(N4CCC([C@H](C5=CC=CC=C5C6=CC=C(Cl)C=C6)O)CC4)C=C3 | ||
分子式 | C45H48ClF3N4O7S3 | 分子量 | 945.53 |
溶解度 | DMSO: 125 mg/mL (132.20 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.0576 mL | 5.288 mL | 10.5761 mL |
5 mM | 0.2115 mL | 1.0576 mL | 2.1152 mL |
10 mM | 0.1058 mL | 0.5288 mL | 1.0576 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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