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Merck
CN

PZ0296

PF-06459988

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C19H22ClN7O3
CAS Number:
1428774-45-1
Molecular Weight:
431.88
NACRES:
NA.77
PubChem Substance ID:
329823819
UNSPSC Code:
12352200
MDL number:
MFCD28987462

Key Documents

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Product Name

PF-06459988, ≥98% (HPLC)

InChI key

ODMXWZROLKITMS-RISCZKNCSA-N

SMILES string

ClC1=CNC2=C1C(OC[C@@H]3[C@@H](OC)CN(C(C=C([H])[H])=O)C3)=NC(NC4=CN(C)N=C4)=N2

InChI

1S/C19H22ClN7O3/c1-4-15(28)27-7-11(14(9-27)29-3)10-30-18-16-13(20)6-21-17(16)24-19(25-18)23-12-5-22-26(2)8-12/h4-6,8,11,14H,1,7,9-10H2,2-3H3,(H2,21,23,24,25)/t11-,14+/m1/s1

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear

storage temp.

room temp

Quality Level

100

Biochem/physiol Actions

PF-06459988 is an orally available irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms including the secondary acquired resistance mutation T790M. PF-06459988 has minimal activity against wild-type EGFR (WT EGFR).

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
075M4741V

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Hengmiao Cheng et al.
Journal of medicinal chemistry, 59(5), 2005-2024 (2016-01-13)
First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients' disease progresses, often driven by a second-site mutation in the EGFR kinase domain (T790M). Another liability of the first

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