| Identification | Back Directory | [Name]
PF-6274484 | [CAS]
1035638-91-5 | [Synonyms]
PF-6274484
PF-6274484 >=98% (HPLC)
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-2-propenamide
2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]- | [Molecular Formula]
C18H14ClFN4O2 | [MDL Number]
MFCD30182370 | [MOL File]
1035638-91-5.mol | [Molecular Weight]
372.78 |
| Hazard Information | Back Directory | [Description]
PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively. | [Uses]
PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively[1]. | [IC 50]
EGFR (WT): 0.18 nM (Ki); EGFRL858R/T790M: 0.14 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Schwartz PA, et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc Natl Acad Sci U S A. 2014;111(1):173-178. DOI:10.1073/pnas.1313733111 |
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| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
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