513033
PD 168393
A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 700 pM).
Synonym(s):
PD 168393, 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline
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About This Item
Empirical Formula (Hill Notation):
C17H13BrN4O
CAS Number:
Molecular Weight:
369.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Brc1cc(ccc1)Nc2ncnc3c2cc(cc3)NC(=O)C=C
InChI
1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)
InChI key
HTUBKQUPEREOGA-UHFFFAOYSA-N
General description
A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 0.70 nM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys773. Excellent antitumor agent in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR
EGFR
Product competes with ATP.
Reversible: no
Target IC50: 700 pM against EGFR
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Avoid freeze/thaw cycles of solutions.
Other Notes
Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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