Powder: -20°C for 3 years | In solvent: -80°C for 1 year
THZ1 is a covalent inhibitor of CDK7 (IC50: 3.2nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 753 | 待询 | ||
10 mg | ¥ 1,383 | 待询 | ||
25 mg | ¥ 2,733 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 978 | 待询 |
产品描述 | THZ1 is a covalent inhibitor of CDK7 (IC50: 3.2nM). |
体外活性 | THZ1 covalently modifies CDK7 by targeting C312 residue outside of the kinase domain, providing an unanticipated means of achieving covalent selectivity. THZ1 potently inhibits the proliferation of Jurkat and Loucy T-ALL cell lines (IC50: 50nM and 0.55nM, respectively). In the kinase binding assay, THZ1 shows a good binding affinity (IC50: 3.2nM [1]. |
体内活性 | As an inhibitor of CDK7, THZ1 inhibits the phosphorylation of the C-terminal domain of RNAP polymerase II, effecting the regulation of transcription. THZ1 also inhibits the activation of the CDK proteins. It is reported to disrupt the CDK7 signaling pathways both in Jurkat cells and Loucy cells. THZ1 shows a broad-based activity with IC50 values less than 200nM in a variety of cancer cell lines. Among these cell lines, T-ALL is exceptional sensitivity to THZ1 due to the transcription effect of RUNX1 caused by THZ1 [1]. |
别名 | THZ1 Hydrochloride |
分子量 | 602.51 |
分子式 | C31H29Cl2N7O2 |
CAS No. | T23458 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: ≥30.1255mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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