pf-06459988

PF-06459988 是一种新型的的、有效的、具有口服活性的、不可逆的和选择性的表皮生长因子受体（ EGFR） 突变体抑制剂。PF-06459988 对含 T790M 的 EGFRs 双突变体具有高效性和高亲和力，对 WT EGFR 具有极小的活性。PF-06459988 使治疗癌症的候选药物。

(3S, 4S)-PF-06459988 is the less active S enantiomer of PF-06459988, which is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 exhibits excellent selectivity against EGFR wild-type due to its minimally reactive electrophile, which reduces the likelihood of off-target labeling.