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Novel Potent EGFR-JAK3 Dual-Target Inhibitor that Overcomes KRAS Mutation Resistance in Colorectal Cancer.
Anti-cancer Agents in Medicinal Chemistry 2022 June 10
BACKGROUND: In-depth and clear mechanistic study is a prerequisite for new drugs to enter clinical research.
METHOD: New chemical entity BY4008 was identified by our lab as novel and highly potent EGFR and JAK3 dual-target inhibitor. In a cell-based test, it exhibited strong antiproliferative activities against SW620 and HCT116 colon cancer cells harboring KRAS mutation with IC50 of nanomolar potency. Furthermore, acridine orange/ethidium bromide (AO/EB), Hematoxylin-Eosin (H&E) and DAPI staining assays as well as flow cytometry analyses indicated that BY4008 has the function of pro-apoptosis and arresting the cell cycle. In addition, BY4008 inhibited the autophosphorylation of EGFR and blocked the activation of downstream signaling as well as JAK-STAT3 pathway.
RESULT: Meanwhile, a decreased level of reactive oxygen species (ROS) and an increased level of malondialdehyde (MDA) in SW620 and HCT116 cells were observed after exposure to BY4008.
CONCLUSION: In summary, this study provides an important structural basis and mechanistic study for future effective treatment of colorectal cancer.
METHOD: New chemical entity BY4008 was identified by our lab as novel and highly potent EGFR and JAK3 dual-target inhibitor. In a cell-based test, it exhibited strong antiproliferative activities against SW620 and HCT116 colon cancer cells harboring KRAS mutation with IC50 of nanomolar potency. Furthermore, acridine orange/ethidium bromide (AO/EB), Hematoxylin-Eosin (H&E) and DAPI staining assays as well as flow cytometry analyses indicated that BY4008 has the function of pro-apoptosis and arresting the cell cycle. In addition, BY4008 inhibited the autophosphorylation of EGFR and blocked the activation of downstream signaling as well as JAK-STAT3 pathway.
RESULT: Meanwhile, a decreased level of reactive oxygen species (ROS) and an increased level of malondialdehyde (MDA) in SW620 and HCT116 cells were observed after exposure to BY4008.
CONCLUSION: In summary, this study provides an important structural basis and mechanistic study for future effective treatment of colorectal cancer.
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