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EGFR-IN-12

CAS No. : 879127-07-8

MCE 国际站：EGFR-IN-12

产品活性：EGFR-IN-12 是一种 4,6-二取代的嘧啶，是一种有效的，ATP 竞争性，不可逆且高度选择性的 EGFR 抑制剂，IC₅₀ 为 21 nM。EGFR-IN-12 还抑制突变型 EGFR^L858R 和 EGFR^L861Q，IC₅₀ 分别为 63 nM 和 4 nM。EGFR-IN-12 对 EGFR 的选择性高于 HER4 (IC₅₀ = 7640 nM) 和 55种其他激酶。EGFR-IN-12 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：EGFR  |  Apoptosis

In Vitro: EGFR-IN-12 (EGFR inhibitor 324674; 0-2 µM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations.
EGFR-IN-12 (EGFR inhibitor 324674; 0-3 µM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.
EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 µM and 1.04 µM, respectively.
Pretreatment of cells with EGFR-IN-12 (compound 1; 10 µM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12.

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