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).

• Szinonimák: CL-387,785, N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785
• Tapasztalati képlet (Hill-képlet): C₁₈H₁₃BrN₄O
• CAS-szám: 194423-06-8
• Molekulatömeg: 381.23
• MDL-szám: MFCD02179194
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• Forma: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; desiccated (hygroscopic); protect from light
• szín: pale yellow
• oldhatóság: DMSO: 200 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: −20°C
• 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)
• Nemzetközi kémiai azonosító kulcs: BTYYWOYVBXILOJ-UHFFFAOYSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

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

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 1
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable