(3S,4S) -PF-06459988

(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].

Product Specifications

CAS Number

[1858291-14-1]

UNSPSC

12352005

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/3s-4s-pf-06459988.html

Concentration

10mM

Purity

98.97

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

C=CC(N1C[C@@H](COC2=C3C(NC=C3Cl)=NC(NC4=CN(C)N=C4)=N2)[C@H](OC)C1)=O

Molecular Formula

C19H22ClN7O3

Molecular Weight

431.88

References & Citations

[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.