EGFR Inhibitor II, BIBX1382-CAS 196612-93-8-Calbiochem

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一般描述

A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC₅₀= 3 nM) and in culture (IC₅₀= 0.15, 1.82, and 3.2 ?M in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC₅₀= 3.4 ?M) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 ?M. Its antitumor efficacy has also been demonstrated in a murine xenograft modelin vivo(10 mg/kg, daily, p.o.).
A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC₅₀= 3 nM) and in culture (IC₅₀= 0.15, 1.82, and 3.2 ?M in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC₅₀= 3.4 ?M) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 ?M. Its antitumor efficacy has also been demonstrated in a murine xenograft modelin vivo(daily p.o. dose 10 mg/kg).

包装

5 mg in Plastic ampoule

生化/生理作用

Cell permeable: yes
Target IC₅₀: 3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 ?M in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells
Primary Target
EGFR (ErbB-1, HER-1)
Product competes with ATP.
Reversible: yes

警告

Toxicity: Irritant (B)

其他说明

Solca, F.F., et al. 2004.J. Pharm. Exp. Ther.311,502.
Egeblad, M., et al. 2001.Biochem. Biophys. Res. Commun.281,25.
Nuijen, B., et al. 2000.Int. J. Pharm.194,261.
Tocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.

法律信息

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

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