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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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P288199-10mg
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10mg |
3
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$112.90
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P288199-50mg
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50mg |
2
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$444.90
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P288199-250mg
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250mg |
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
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$2,002.90
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High affinity and potent covalent EGFR kinase inhibitor
| 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. |
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 |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| 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 |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | Jan 03, 2025 | P288199 | |
| Certificate of Analysis | Aug 19, 2024 | P288199 | |
| Certificate of Analysis | Aug 19, 2024 | P288199 | |
| Certificate of Analysis | Aug 19, 2024 | P288199 |
| 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 |