4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE
4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE Basic information
- Product Name:
- 4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE
- Synonyms:
-
- PD 174265
- 4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE
- N-[4-(3-bromoanilino)quinazolin-6-yl]propanamide
- PD 174265 - CAS 216163-53-0 - Calbiochem
- Propanamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-
- N-(4-((3-Bromophenyl)amino)quinazolin-6-yl)propionamide
- CAS:
- 216163-53-0
- MF:
- C17H15BrN4O
- MW:
- 371.23
- Mol File:
- 216163-53-0.mol
4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE Chemical Properties
- storage temp.
- -20°C
- solubility
- DMF: 30 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml
- form
- Yellow solid
- color
- Light yellow to yellow
4-[(3-BROMOPHENYL)AMINO]-6-PROPIONYLAMIDOQUINAZOLINE Usage And Synthesis
Description
PD 174265 is a potent, cell-permeable inhibitor of the tyrosine kinase activity of the epidermal growth factor (EGF) receptor (IC50 = 0.45 nM). It is effective in cells, blocking tyrosine phosphorylation induced by either EGF or heregulin (IC50s = 39 and 220 nM, respectively). The action of PD 174265 is reversible, which makes it a useful tool for comparative studies with irreversible inhibitors of EGFR kinase activity.
Uses
PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR tyrosine kinase activity.
General Description
A potent, cell-permeable, reversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 450 pM). The reversible nature of this compound makes it a less effective antitumor agent than PD 168393 (Cat. No. 513033).
Biochem/physiol Actions
Target IC50: 450 pM against EGF receptor (EGFR) tyrosine kinase activity
Enzyme inhibitor
This substituted quinazoline (FWfree-base = 371.24 g/mol), also known as 4- [(3-bromophenyl)amino]-6-propionylamidoquinazoline, inhibits epidermal growth factor receptor (EGFR) protein-tyrosine kinase, IC50 = 0.45 nM. PD 174265 selectively targets and irreversibly inactivates the epidermal growth factor receptor tyrosine kinase through specific, covalent modification of a Cys-773. See also PD 168393
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