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233100

Sigma-Aldrich

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).

Synonym(s):

CL-387,785, N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785

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About This Item

Empirical Formula (Hill Notation):
C18H13BrN4O
CAS Number:
194423-06-8
Molecular Weight:
381.23
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

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

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

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.
A cell-permeable and irreversible inhibitor of EGF-stimulated autophosphorylation of tyrosine residues in the epidermal growth factor receptor (EGFR) in vivo (IC50 = 250-490 pM) and blocks EGF-mediated growth. Also inhibits proliferation of cells that overexpress EGFR or c-Erb-2 (IC50 = 31-125 nM) by covalently binding to EGFR.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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