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(3S,4S)-PF-06459988

Names

[ CAS No. ]:
1858291-14-1

[ Name ]:
(3S,4S)-PF-06459988

Biological Activity

[Description]:

(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

EGFR[1]


[References]

[1]. Cheng, H., et al. Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. Journal of Medicinal Chemistry, 59(5), 2005–2024.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H22ClN7O3

[ Molecular Weight ]:
431.88

Related Compounds