Bioactivity | EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma[1]. |
Invitro | EP26 (0-4 µM; 48 h) 以剂量依赖性方式降低 p-EGFR 的蛋白表达[1]。EP26 (0.5, 1, 2µM; 48 h) 诱导细胞周期停滞在 G0/G1 期[1]。EP26 以剂量依赖性方式与人 PD-L1 和鼠 PD-L1 结合,KD 值分别为 0.58、0.52 µM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> EP26 相关抗体: Cell Proliferation Assay[1] Cell Line: |
In Vivo | EP26 (50, 100 mg/kg; p.o.; once a day for 21 days) 在小鼠中显示出抗肿瘤活性[1]。药代动力学分析[1].PK parameters |
Formula | C42H42ClFN4O5 |
Molar Mass | 737.26 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Yang Z, et al. Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy. J Med Chem. 2024 May 23;67(10):7995-8019. |