In vitro
ZM-306416 is a VEGFR antagonist and ZM-306416 can inhibit VEGFR with IC50 of 0.67 uM. Sharing the 4-anilinoquinazoline scaffold common among EGFR kinase inhibitors such as erlotinib, gefitinib and lapatinib. ZM-306416 also shows potent inhibition to EGFR. ZM-306416 can potently inhibit the EGFR kinase with an IC50 value lower than 10 nM. ZM-306416 exhibits inhibitory activity across all three kinases of the panel, yielding IC50 values of 0.33 uM for SRC, 0.33 uM for VEGFR1, and 1.3 uM for ABL kinases. ZM-306416 can also induces selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 uM and 0.072 uM, while sparing the wild type EGFR cell lines A549 and H2030..
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