CL-387,785-CAS 194423-06-8-Calbiochem

C₁₈H₁₃BrN₄O

381.23

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.
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.

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

Toxicity: Standard Handling (A)

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

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.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

pale yellow

DMSO: 200 mg/mL

ambient

−20℃

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1