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; Ki = 6 pM).
Synonyme(s) :
PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
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A propos de cet article
Formule empirique (notation de Hill) :
C16H14BrN3O2
Numéro CAS:
Poids moléculaire :
360.21
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Service technique
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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
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; Ki = 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
EGFR
Product competes with ATP.
Reversible: yes
Target Ki: 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.
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)
Classe de stockage
11 - Combustible Solids
wgk
WGK 1
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