| 产品描述： | 表观遗传阅读器域抑制剂;Epigenetic Reader Domain Inhibitors;;InformationPLX51107 PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).TargetsBRD2 BD1 (Cell-free assay); BRD4 BD1 (Cell-free assay); BRD3 BD1 (Cell-free assay); BRDT BD1 (Cell-free assay); BRD2 BD2 (Cell-free assay) 31640,1.6 nM(Kd); 1.7 nM(Kd); 2.1 nM(Kd) ;5 nM(Kd); 5.9 nM(Kd)In vitroIn a set of cell cultures, short-term (4h) treatment of PLX51107 result in robust change in PD markers but do not induce an immediate apoptotic response. Induction of apoptosis occurrs after prolonged treatment (16 hours or more of continuous exposure). PLX51107 induces accumulation of p21 and IκBα, reduced levels of cMYC, and modulation of pro- and anti-apoptotic proteins.In vivoPLX51107 is well tolerated in mice. The half-life of PLX51107 is relative short in rodents and dogs (<3 h). PLX51107 demonstrates in vivo antitumor effects in preclinical models of CLL and aggressive lymphoma. |
| 靶点： |
Kd: 1.6 nM (BRD2-BD1), 2.1 nM (BRD3-BD1), 1.7 nM (BRD4-BD1), 5 nM (BRDT-BD1), 5.9 nM (BRD2-BD2), 6.2 nM (BRD3-BD2), 6.1 nM (BRD4-BD2), 120 nM (BRDT-BD2), ∼100 nM (CBP), ∼100 nM (EP300) |
| 体内研究： |
PLX51107 (2 mg/kg，口服) 在 Ba/F3 (小鼠 IL3 依赖性前 B 细胞系) 脾肿大小鼠模型中抑制 75% 的脾肿大，其效果与 25 mg/kg OTX015 相似。PLX51107 (20 mg/kg，qd，po) 通过每天一次口服给药在侵袭性慢性淋巴细胞白血病 (CLL) 和里氏转化 (RT) 疾病模型中表现出有效的抗白血病作用。 |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.281 ml |
11.403 ml |
22.806 ml |
| 5 mM |
0.456 ml |
2.281 ml |
4.561 ml |
| 10 mM |
0.228 ml |
1.14 ml |
2.281 ml |
| 50 mM |
0.046 ml |
0.228 ml |
0.456 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京