EGFR-IN-73 (Compound 3f) 是最常见的 EGFR 突变EGFR Del19的有效抑制剂，IC50为 119 nM。
| 生物活性 | EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most commonEGFRmutationEGFRDel19with anIC50of 119 nM[1]. |
| IC50& Target[1] | EGFRdel19 119 nM (IC50) | EGFRL858R 820 nM (IC50) | EGFRWT >10 μM (IC50) | EGFRL858R/T790M >10 μM (IC50) |
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体外研究
(In Vitro) | EGFR-IN-73 (Compound 3f) (0.01 nM-10 μM; 72 h) is weakly active on the EGFR WT and a potent binder of the EGFR mutants EGFR d746-750 (Del19), EGFR d747-752/P753S, EGFR L858R, or EGFR d752-759 in addition to weaker interaction detected for other oncogenic mutants (FLT3 D835Y and FLT3 ITD D835V)[1].
EGFR-IN-73 shows excellent chemical stability under acid conditions with more than 95% after 3 h and also good stability at pH 7.4 above 80%[1].
Cell Proliferation Assay[1] | Cell Line: | Ba/F3 cell, EGFR WT, L858R, L858R/C797S, L858R/T790M, L858R/T790M/C797S, Del19, Del19/C797S, Del19/T790M, Del19/T790M/C797S, and Ex20 insertion mutants | | Concentration: | 0.01 nM-10 μM | | Incubation Time: | 72 h | | Result: | Did not inhibit EGFR WT growth, whereas inhibited both L858R and L858R/C979S mutants in the sub-micromolar range, with IC50values of 385.6 and 749.6 nM, respectively. Was even more potent in cells transduced with the Del19 and Del19/C797S mutations than on the other mutants in this series, with IC50values of 197.5 and 147.9 nM, respectively. |
Western Blot Analysis[1] | Cell Line: | Ba/F3 cells expressing various EGFR mutants | | Concentration: | 10, 100 and 1000 nM | | Incubation Time: | 8 h | | Result: | Showed significant activity at L858R and excellent activity at the Del19 and Del19/C797S mutant EGFR. Did not affect T790M and WT EGFR. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
