PF-06459988 ( PF 06459988;PF06459988;PF 6459988 )

Catalog No. M11808 CAS No. 1428774-45-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-06459988
Note

Research use only, not for human use.
Brief Description

PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.
Description

PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively; exhibist selectivity over wild-type EGFR (IC50>5 uM); shows potential for treatment of EGFR T790M mutation in advanced NSCLC.Lung Cancer Phase 1 Discontinued
Synonyms

PF 06459988;PF06459988;PF 6459988
Pathway

Angiogenesis
Target

EGFR
Recptor

EGFR
Research Area

Cancer
Indication

Lung Cancer

CAS Number

1428774-45-1
Formula Weight

431.88
Molecular Formula

C19H22ClN7O3
Purity

>98% (HPLC)
Solubility

DMSO : 50 mg/mL 115.77 mM
SMILES

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

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-methoxy-1-pyrrolidinyl]-2-propen-1-one

1. Cheng H, et al. J Med Chem. 2016 Mar 10;59(5):2005-24.
2. Planken S, et al. J Med Chem. 2017 Apr 13;60(7):3002-3019.

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