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).

• Synonyma: CL-387,785, N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785
• Empirický vzorec (Hillův zápis): C₁₈H₁₃BrN₄O
• Číslo CAS: 194423-06-8
• Molekulová hmotnost: 381.23
• MDL number: MFCD02179194
• UNSPSC Code: 12352200
• NACRES: NA.77

Vlastnosti

• Název produktu: 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: 100

Popis

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

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.

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

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable