1373764-87-4
Chemical Structure
WB-308
- CAS No.: 1373764-87-4
- Formula:C19H17FN2O
- Molecular Weight:308.35
IUPAC Name: 1-(6-fluoro-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2-phenylethan-1-one
InChIKey: HLKIUOZYYGXOOR-UHFFFAOYSA-N
SMILES: FC1=CC2=C(C=C1)NC3=C2CCN(C3)C(CC4=CC=CC=C4)=O
Biological Activity: 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.
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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. | |||||||||||||||||||||
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