513033

PD 168393

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

• Synonim(y): PD 168393, 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline
• Wzór empiryczny (zapis Hilla): C₁₇H₁₃BrN₄O
• Numer CAS: 194423-15-9
• Masa cząsteczkowa: 369.22
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD02179207
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 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
• 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

Opis

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

Reversible: no

Target IC₅₀: 700 pM against EGFR

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

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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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable