Found it - we of course don't know if the particular lead they have selected has anywhere near that potency (which would be unprecedented among TKI's I think).
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In some embodiments, one or more compounds described herein bind to EGFR. In some embodiments, one or more compounds described herein bind to EGFR having one or more mutations (e.g., bind selectively). In some embodiments, the IC50 of a subject compound for mutant EGFR inhibition can be less than about 100 nM, less than about 50 nM, less than about 10 nM, less than about 1 nM,less than about 0.5 nM, or less than about 1 pM.
[238] In some embodiments, the IC50 of a subject compound for mutant EGFR having one or more mutations in exon 20 can be less than about 100 nM, less than about 50 nM, less than about 10 nM, less than about 1 nM, less than about 0.5 nM, or less than about 1 pM. In some embodiments, the IC50 value can be less than about 1 µM, less than about 500 nM, or less than about 250 nM. In some
embodiments, the mutant EGFR has one or more of the following insertions in the exon 20 domain: ASV or NPG. In other embodiments, the mutant EGFR has either or both of the DT and/or LT mutations. |
