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).
Synonim(y):
PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
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About This Item
Wzór empiryczny (zapis Hilla):
C16H14BrN3O2
Numer CAS:
Masa cząsteczkowa:
360.21
Kod UNSPSC:
12352200
NACRES:
NA.77
Polecane produkty
Poziom jakości
Próba
≥97% (HPLC)
Postać
solid
siła działania
25 pM IC50
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
protect from light
kolor
white
rozpuszczalność
DMSO: 5 mg/mL
Warunki transportu
ambient
temp. przechowywania
−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)
Klucz InChI
LSPANGZZENHZNJ-UHFFFAOYSA-N
Opis ogólny
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.
Działania biochem./fizjol.
Cell permeable: yes
Primary Target
EGFR
EGFR
Product competes with ATP.
Reversible: yes
Target Ki: 6 pM against epidermal growth factor receptor (EGFR)
Ostrzeżenie
Toxicity: Standard Handling (A)
Rekonstytucja
Following reconstitution aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.
Inne uwagi
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.
Informacje prawne
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
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 1
Certyfikaty analizy (CoA)
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Masz już ten produkt?
Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.
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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