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).
Synonyma:
PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
Přihlásitk zobrazení cen stanovených pro organizaci a smluvních cen
About This Item
Empirický vzorec (Hillův zápis):
C16H14BrN3O2
Číslo CAS:
Molekulová hmotnost:
360.21
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Doporučené produkty
Quality Level
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)
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
Osvědčení o analýze (COA)
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Dokumenty související s produkty, které jste v minulosti zakoupili, byly za účelem usnadnění shromážděny ve vaší Knihovně dokumentů.
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
Gaurav Agrahari et al.
The Journal of investigative dermatology, 140(3), 656-665 (2019-08-30)
The expressions of LL-37 and KLK-5 were found to be altered in various dermatoses, including atopic dermatitis, psoriasis, and rosacea. However, the downstream inflammatory effect of LL-37 and KLK-5 is not as well studied. In addition, there is little high-quality
Laleh Abbassi et al.
Nature communications, 12(1), 1438-1438 (2021-03-06)
Germ cells are physically coupled to somatic support cells of the gonad during differentiation, but this coupling must be disrupted when they are mature, freeing them to participate in fertilization. In mammalian females, coupling occurs via specialized filopodia that project
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