EGFR-IN-60 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting EGFRWT, EGFRT790M, EGFRL858R, and JAK3 with IC50 values of 83, 26, 53, and 69 nM, respectively. This compound effectively suppresses the proliferation of H1975 cells with the EGFRT790M mutation (IC50=1.32 µM) while yielding less potency against A431 cells expressing EGFRWT (IC50=4.96 µM). With favorable oral bioavailability, EGFR-IN-60 demonstrates significant antitumor activity, promoting cell death via apoptosis as indicated by an increased Bax/Bcl-2 ratio. This makes it a valuable candidate for research into targeted therapies for EGFR-related cancers.
EGFR-IN-60 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting EGFRWT, EGFRT790M, EGFRL858R, and JAK3 with IC50 values of 83, 26, 53, and 69 nM, respectively. This compound effectively suppresses the proliferation of H1975 cells with the EGFRT790M mutation (IC50=1.32 µM) while yielding less potency against A431 cells expressing EGFRWT (IC50=4.96 µM). With favorable oral bioavailability, EGFR-IN-60 demonstrates significant antitumor activity, promoting cell death via apoptosis as indicated by an increased Bax/Bcl-2 ratio. This makes it a valuable candidate for research into targeted therapies for EGFR-related cancers.
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