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).
Sinonimo/i:
PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
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About This Item
Formula empirica (notazione di Hill):
C16H14BrN3O2
Numero CAS:
Peso molecolare:
360.21
Codice UNSPSC:
12352200
NACRES:
NA.77
Prodotti consigliati
Livello qualitativo
Saggio
≥97% (HPLC)
Forma fisica
solid
Potenza
25 pM IC50
Produttore/marchio commerciale
Calbiochem®
Condizioni di stoccaggio
OK to freeze
protect from light
Colore
white
Solubilità
DMSO: 5 mg/mL
Condizioni di spedizione
ambient
Temperatura di conservazione
−20°C
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)
LSPANGZZENHZNJ-UHFFFAOYSA-N
Descrizione generale
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.
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.
Azioni biochim/fisiol
Cell permeable: yes
Primary Target
EGFR
EGFR
Product competes with ATP.
Reversible: yes
Target Ki: 6 pM against epidermal growth factor receptor (EGFR)
Attenzione
Toxicity: Standard Handling (A)
Ricostituzione
Following reconstitution aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.
Altre note
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.
Note legali
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
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 1
Certificati d'analisi (COA)
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A J Bridges et al.
Journal of medicinal chemistry, 39(1), 267-276 (1996-01-05)
4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (32, PD 153035) is a very potent inhibitor (IC50 0.025 nM) of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR), binding competitively at the ATP site. Structure-activity relationships for close analogues of 32 are very steep.
D W Fry et al.
Science (New York, N.Y.), 265(5175), 1093-1095 (1994-08-19)
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or
Albrecht Stenzinger et al.
Cells, tissues, organs, 184(2), 76-87 (2007-03-16)
The novel protein PTPIP51 (protein tyrosine phosphatase-interacting protein 51), which has been found to interact with protein tyrosine phosphatases of the PTP1B/TcPTP subfamily, is expressed in all suprabasal layers of human epidermis. Hence, a human keratinocyte cell line (HaCaT) grown
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