PF-06459988( PF 06459988 | PF06459988 | PF 6459988 )

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

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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.
In Vitro

Cell Cytotoxicity Assay Cell Line:NSCLC cell lines Concentration:0-10 μMIncubation Time:2 hours Result:Exibited excellent cellular potency to H1975 (L858R/T790M), PC9-DRH (Del/T790M), H3255 (L858R), PC9 (Del), HCC827 (Del) and A549 (WT) cell lines with IC50 values of 13, 7, 21, 140, 90 and 5100 nM, respectively. Showed high specificity to T790M-containing double mutan EGFRs.
In Vivo

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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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