PF 6274484

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Cat.No. 5939 - PF 6274484 | C18H14ClFN4O2 | CAS No. 1035638-91-5
Description: High affinity and potent covalent EGFR kinase inhibitor
Chemical Name: N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-2-propenamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

High affinity and potent covalent EGFR kinase inhibitor (Ki = 0.14 nM). Inhibits autophosphorylation of WT and mutant EGFR in tumor cells (IC50 values are 5.8 and 6.6 nM, respectively).

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 372.78
Formula C18H14ClFN4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1035638-91-5
PubChem ID 74766099
InChI Key TUYDDIWQXWTNSW-UHFFFAOYSA-N
Smiles COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1NC(C=C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.28 100
ethanol 3.73 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 372.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.68 mL 13.41 mL 26.83 mL
5 mM 0.54 mL 2.68 mL 5.37 mL
10 mM 0.27 mL 1.34 mL 2.68 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Schwartz et al (2014) Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc.Natl.Acad.Sci.U.S.A. 111 173 PMID: 24347635


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Literature in this Area

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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