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PF 6274484 - ≥98%(HPLC), high purity , CAS No.1035638-91-5

    Grade & Purity:
  • ≥98%(HPLC)
In stock
Item Number
P288199
Grouped product items
SKU Size
Availability
Price Qty
P288199-10mg
10mg
3
$112.90
P288199-50mg
50mg
2
$444.90
P288199-250mg
250mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$2,002.90

High affinity and potent covalent EGFR kinase inhibitor

Basic Description

Synonyms PF-6274484 | N-4-(3-Chloro-4-fluorophenyl)amino-7-methoxy-6-quinazolinyl-2-propenamide | N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-2-propenamide
Specifications & Purity ≥98%(HPLC)
Biochemical and Physiological Mechanisms High affinity and potent covalent EGFR kinase inhibitor (Ki= 0.14 nM). Inhibits autophosphorylation of WT and mutant EGFR in tumor cells (IC50values are 5.8 and 6.6 nM, respectively).
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

PF 6274484 is a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM. PF 6274484 inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Diazanaphthalenes
Subclass Benzodiazines
Intermediate Tree Nodes Quinazolines
Direct Parent Quinazolinamines
Alternative Parents Methoxyanilines  Anisoles  N-arylamides  Alkyl aryl ethers  Aminopyrimidines and derivatives  Chlorobenzenes  Fluorobenzenes  Aryl fluorides  Aryl chlorides  Imidolactams  Heteroaromatic compounds  Acrylic acids and derivatives  Secondary carboxylic acid amides  Azacyclic compounds  Hydrocarbon derivatives  Amines  Carbonyl compounds  Organofluorides  Organochlorides  Organic oxides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Quinazolinamine - Methoxyaniline - Anisole - Phenol ether - Aniline or substituted anilines - N-arylamide - Alkyl aryl ether - Aminopyrimidine - Halobenzene - Chlorobenzene - Fluorobenzene - Monocyclic benzene moiety - Aryl halide - Benzenoid - Imidolactam - Pyrimidine - Aryl chloride - Aryl fluoride - Acrylic acid or derivatives - Heteroaromatic compound - Secondary carboxylic acid amide - Carboxamide group - Azacycle - Ether - Carboxylic acid derivative - Organic nitrogen compound - Organohalogen compound - Organochloride - Carbonyl group - Organofluoride - Organonitrogen compound - Organooxygen compound - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Amine - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
External Descriptors Not available

Associated Targets(Human)

ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (297 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name N-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]prop-2-enamide
INCHI InChI=1S/C18H14ClFN4O2/c1-3-17(25)24-15-7-11-14(8-16(15)26-2)21-9-22-18(11)23-10-4-5-13(20)12(19)6-10/h3-9H,1H2,2H3,(H,24,25)(H,21,22,23)
InChIKey TUYDDIWQXWTNSW-UHFFFAOYSA-N
Smiles COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)C=C
Isomeric SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)C=C
PubChem CID 74766099
Molecular Weight 372.78

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

4 results found

Lot Number Certificate Type Date Item
L2420096 Certificate of Analysis Jan 03, 2025 P288199
K2101094 Certificate of Analysis Aug 19, 2024 P288199
K2101095 Certificate of Analysis Aug 19, 2024 P288199
K2101097 Certificate of Analysis Aug 19, 2024 P288199

Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 37.28, Max Conc. mM: 100
Molecular Weight 372.800 g/mol
XLogP3 3.900
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 5
Exact Mass 372.079 Da
Monoisotopic Mass 372.079 Da
Topological Polar Surface Area 76.100 Ų
Heavy Atom Count 26
Formal Charge 0
Complexity 512.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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