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
• Empirical Formula (Hill Notation): C₁₇H₁₃BrN₄O
• CAS Number: 194423-15-9
• Molecular Weight: 369.22
• MDL number: MFCD02179207
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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
• 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

Description

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.

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 700 pM). 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

Product competes with ATP.

Reversible: no

Target IC₅₀: 700 pM against EGFR

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable