TP-021 (Synonyms: BCL6-IN-8c)
目录号: PL02400 纯度: ≥98%
CAS No. :2130878-25-8
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中文名称
TP-021
英文名称
TP-021
英文别名
BCL6-IN-8c;6-((2-chloro-4-nitro-5-((tetrahydro-2H-pyran-4-yl)oxy)phenyl)amino)-3,4-dihydroquinolin-2(1H)-one;GTPL9671;compound 8c [PMID: 28760529];6-{[2-chloro-4-nitro-5-(oxan-4-yloxy)phenyl]amino}-3,4-dihydro-1H-quinolin-2-one;TP-021
Cas No.
2130878-25-8
分子式
C20H20ClN3O5
分子量
417.84
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TP-021 (BCL6-IN-8c) 是一种有效的具有口服活性的 BCL6-共抑制因子相互作用抑制剂,在无细胞酶联免疫吸附试验中,其 IC50 为 0.10 µM。
生物活性
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC 50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay.
性状
Solid
IC50 & Target[1][2]
IC50: 0.10 μM (BCL6-corepressor interaction)
体外研究(In Vitro)
TP-021 (BCL6-IN-8c, Compound 8c) also exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC50 = 0.72 μM). TP-021 (BCL6-IN-8c) does not exhibit significant cytotoxicity even at 30 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
The pharmacokinetic profile of TP-021 (BCL6-IN-8c, Compound 8c) is evaluated by a mouse cassette-dosing study (0.1 mg/kg iv; 1 mg/kg po). TP-021 (BCL6-IN-8c) exhibits a good pharmacokinetic profile (C max = 233 ng/mL, T max = 2 hours, MRT = 3.3 h, AUC = 1.27 mg?h/mL, F (oral bioavailability) = 79.9%). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yasui T, et al. Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design. Bioorg Med Chem. 2017 Sep 1;25(17):4876-4886.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (119.66 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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