EGFR Inhibitor

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EGFR 抑制剂是一种细胞渗透性、选择性的 EGFR 激酶抑制剂 (IC50: 21 nM)，可阻断细胞中受体的自身磷酸化。

EGFR inhibitor is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

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. Apoptosis Analysis Cell Line:HT29 and SW480 cells Concentration:0 μM, 1 μM, 2 μM Incubation Time:48 hours Result:Induced apoptosis in HT29 cells and SW480 cells.Western Blot Analysis Cell Line:HT29 and SW480 cells Concentration:0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Time:3 hours Result:Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.

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Angiogenesis

EGFR

EGFR| EGFR (L858R)| EGFR (L861Q)

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879127-07-8

413.4

C21H18F3N5O

>98% (HPLC)

DMSO: 25 mg/mL;Ethanol: 10 mg/mL

FC(F)(F)c1cccc(Nc2cc(Nc3cccc(NC(=O)C4CC4)c3)ncn2)c1

N-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide

(-20℃)

With Ice Pack

≥ 2 years