WB-308 

WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.

308.35

C₁₉H₁₇FN₂O

1373764-87-4

FC1=CC2=C(C=C1)NC3=C2CCN(C3)C(CC4=CC=CC=C4)=O

Room temperature in continental US; may vary elsewhere.

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• [1]. Inhibition of non-small cell lung cancer (NSCLC) growth by a novel small molecular inhibitor of EGFR