化合物PLX51107 TQ0253

Product Introduction
Bioactivity


英文名: PLX51107

描述: PLX51107 是一种选择性 BET 抑制剂，与 CBP 和 EP300 的结构域相互作用。它对 BRD2、BRD3、BRD4 和 BRDT 的 BD1 结构域的亲和力Kd 值分别为 1.6、2.1、1.7 和 5 nM，BD2 结构域亲和力Kd 值分别为 5.9、6.2、6.1 和 120 nM。

动物实验: For engraftment studies, C57BL/6 WT mice are engrafted with 1E7 cells by tail-vein injection of splenocytes derived from Eμ-TCL1 or Eμ-Myc/TCL1 mice with active disease. At the onset of leukemia (Eμ-TCL1: ≥ 10% CD19/CD5/CD45-positive circulating cells; Eμ-Myc/TCL1: WBC count ≥ 8 and/or ≥ 5% CD19/CD5/CD45-positive circulating cells), mice are randomized to receive treatments as indicated. PLX51107 20 mg/kg, qd (once daily), oral gavage. Vehicle = 10% N-methyl-2-pyrrolidone plus diluent (40% PEG400, 5% TPGS, 5% Poloxamer 407, and 50% water). Mice are sacrificed when meeting early removal criteria (>20% weight loss, impaired motility, splenomegaly, and evident tumor masses), and tissues are collected for further analysis.

体外活性: PLX51107是一种BET抑制剂，对BRD2、BRD3、BRD4和BRDT的BD1的Kds分别为1.6、2.1、1.7和5 nM，对BD2的Kds分别为5.9、6.2、6.1和120 nM。PLX51107还与CBP和EP300的溴结构域相互作用(Kd约在100 nM范围内)。PLX51107（0.156-10 μM）抑制初级慢性淋巴细胞性白血病（CLL）细胞的CpG诱导增殖。此外，PLX51107还导致p21和IκBα的积累，降低c-MYC水平，并调控促凋亡和抗凋亡蛋白。

体内活性: PLX51107（2 mg/kg，p.o.）在Ba/F3（小鼠IL3依赖的前B细胞系）脾肿大模型中通过口服抑制脾肿大75%，效果与25 mg/kg OTX015相似。PLX51107（20 mg/kg，每日一次，p.o.）通过每日一次口服，在侵袭性CLL和Richter转化（RT）疾病模型中展现出强大的抗白血病效果。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 70 mg/mL (159.65 mM)


关键字: Epigenetic Reader Domain | PLX 51107 | PLX-51107 | PLX51107 | inhibit | Inhibitor

相关产品: BAZ1A-IN-1 | TP-472 | AW68 | GNE-064 | M‑89 | GNE-207 | Trotabresib | GSK9311 hydrochloride | DDO-8926 | WWL0245

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | PPI Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途