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pan-TEAD-IN-1 (Compound 3) 是一种可口服的TEAD泛抑制剂,通过靶向TEAD的棕榈酰化位点,干扰其与共激活因子YAP/TAZ的相互作用,从而抑制Hippo信号通路中癌基因(如Ctgf和Cyr61)的转录上调。pan-TEAD-IN-1 展现出优异的活性,对luciferase的IC50为0.36 nM,对H226细胞的IC50为1.52 nM,并拥有良好的药代动力学特性 (AUC0–∞= 228.7 μg/mL·min,T1/2= 183.9 min)。在TEAD依赖型癌症的异种移植小鼠模型中,该化合物显著抑制肿瘤生长,具有研究TEAD依赖型癌症的潜力。
pan-TEAD-IN-1 (Compound 3) 是一种可口服的TEAD泛抑制剂,通过靶向TEAD的棕榈酰化位点,干扰其与共激活因子YAP/TAZ的相互作用,从而抑制Hippo信号通路中癌基因(如Ctgf和Cyr61)的转录上调。pan-TEAD-IN-1 展现出优异的活性,对luciferase的IC50为0.36 nM,对H226细胞的IC50为1.52 nM,并拥有良好的药代动力学特性 (AUC0–∞= 228.7 μg/mL·min,T1/2= 183.9 min)。在TEAD依赖型癌症的异种移植小鼠模型中,该化合物显著抑制肿瘤生长,具有研究TEAD依赖型癌症的潜力。
产品描述 | pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP/TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC50 of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg/mL·min, T1/2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types. |
分子量 | 331.33 |
分子式 | C19H16F3NO |
CAS No. | 3027484-09-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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