234490

PD 153035

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM).

• Synonym(s): PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
• Empirical Formula (Hill Notation): C₁₆H₁₄BrN₃O₂
• CAS Number: 153436-54-5
• Molecular Weight: 360.21
• MDL number: MFCD00934896
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• potency: 25 pM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: Brc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC
• InChI: 1S/C16H14BrN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
• InChI key: LSPANGZZENHZNJ-UHFFFAOYSA-N

Description

General description

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM). Rapidly suppresses autophosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. Also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. A 10 mM (500 µg/139 µl) solution of PD 153035 (Cat. No. 234491) in DMSO is also available.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: yes

Target K_i: 6 pM against epidermal growth factor receptor (EGFR)

Preparation Note

Following reconstitution aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Bridges, A.J., et al. 1996. J. Med. Chem. 39, 267.
Fry, D.W., et al. 1994. Science265, 1093.

Legal Information

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 1