EGFR-IN-167 

EGFR-IN-1671 is a selective EGFR inhibitor with an IC₅₀ of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC₅₀ = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors^[1].

EGFR-IN-167 (Compound 26) (1 μM) 在体外表现出优异的活性 (IC₅₀ = 35/1.8 nM)^[1]。
EGFR-IN-167 (1-100000 nM, 72 h)对 A431 和 HCC827 细胞具有良好的细胞毒性作用 (GI₅₀ 分别为 260 nM 和 64 nM)，并且能显著抑制恶性细胞增殖 (对 H3255 (L858R) 和 Ba/F3 (C797S) 细胞的 GI₅₀ 分别为 458 nM和 112.7 nM)^[1]。
EGFR-IN-167 (0.01-10 μM, 4 h) 能在 A431 和 HCC827 细胞中持续抑制 EGFR 的磷酸化，即使在洗脱后也能保持抑制效果^[1]。
EGFR-IN-167 在小鼠肝脏微粒体中的半衰期为 29.6 分钟，具有较好的脂溶稳定性^[1]。
EGFR-IN-167 (10 μM) 具有良好的代谢特性，对五种主要的 CYP 同工酶 (CYP1A2、2C9、2C19、2D6 和 3A4) 的抑制率均低于 50%^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

467.47

C₂₀H₂₂FN₃O₇S

3052761-67-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tang G, et al. Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry. Eur J Med Chem. 2023 Nov 5;259:115671.  [Content Brief]