233100
CL-387,785
A cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC50 = 5 nM).
别名:
CL-387,785, N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785
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关于此项目
经验公式（希尔记法）:
C18H13BrN4O
化学文摘社编号:
分子量:
381.23
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
CL-387,785, A cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC50 = 5 nM).
SMILES string
Brc1cc(ccc1)Nc2ncnc3c2cc(cc3)NC(=O)C#CC
InChI
1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
InChI key
BTYYWOYVBXILOJ-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
pale yellow
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR kinase activity
EGFR kinase activity
Product does not compete with ATP.
Reversible: no
Target IC50: 250-490 pM inhibiting EGF-receptor (EGFR) kinase activity in vivo; 5 nM inhibiting EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC50 = 5 nM). Blocks EGF-mediated growth in A431 cells. Inhibits proliferation of EGFR or c-ErbB2 expressing cells (IC50 = 31-125 nM) by covalently binding to the EGFR.
Other Notes
Sweeney, W.E., et al. 2000. Kidney Int.57, 33.
Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.
Sweeney, W.E., et. al. 1999. Kidney Int.56, 406.
Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.
Sweeney, W.E., et. al. 1999. Kidney Int.56, 406.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
M Ivars et al.
The British journal of dermatology, 182(5), 1194-1204 (2019-08-02)
Acantholysis in pemphigus vulgaris (PV) may be triggered by desmoglein (Dsg) and non-Dsg autoantibodies. The autoantibody profile of each patient results in distinct intracellular signalling patterns. Based on our previous findings, we aimed to elucidate whether PV acantholysis in a
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