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Key Documents

PZ0243

Sigma-Aldrich

PF-06672131

≥95% (HPLC)

Synonym(s):

(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-(2-propyn-1-yloxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide, (E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(prop-2-yn-1-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide, Probe 8

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About This Item

Empirical Formula (Hill Notation):
C23H21ClFN5O2
CAS Number:
Molecular Weight:
453.90
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

room temp

SMILES string

FC(C=C1)=C(Cl)C=C1NC2=NC=NC3=CC(OCC#C)=C(NC(/C=C/CN(C)C)=O)C=C32

Biochem/physiol Actions

PF-06672131 is a selective EGFR kinase inhibitor thought to covalently react with active-site cysteine residues in the ATP binding pocket. PF-06672131 has been used as a probe for proteomic analysis to identify off-target binding substrates. The dimethylaminomethyl (DMAM) group appears to increase compound stability in cancer cells with a resultant increase in protein reactivity from selective EGFR binding to widespread proteome-wide reactivity after treatment.

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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The aim of the Cravatt research group is to understand the roles that mammalian enzymes play in physiological and pathological processes and to use this knowledge to identify novel therapeutic targets for the treatment of human disease. To achieve these goals, they develop and apply new technologies that bridge the fields of chemistry and biology, ascribing to the philosophy that the most significant biomedical problems require creative multidisciplinary approaches for their solution. The group's technological innovations address fundamental challenges in systems biology that are beyond the scope of contemporary methods. For instance, enzymes are tightly regulated by post-translational events in vivo, meaning that their activity may not correlate with expression as measured by standard genomic and proteomic approaches. Considering that it is an enzyme's activity, rather than abundance that ultimately dictates its role in cell physiology and pathology, the Cravatt group has introduced a set of proteomic technologies that directly measures this parameter. These activity-based protein profiling (ABPP) methods exploit the power of chemistry to engender new tools and assays for the global analysis of enzyme activities. The enzyme activity profiles generated by ABPP constitute unique molecular portraits of cells and tissues that illuminate how metabolic and signaling networks are regulated in vivo. Additionally, by evaluating enzymes based on functional properties rather than mere abundance, ABPP acquires high-content proteomic information that is enriched in novel markers and targets for the diagnosis and treatment of human disease.

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