324832
EGFR Inhibitor II, BIBX1382
The EGFR Inhibitor II, BIBX1382, also referenced under CAS 196612-93-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
EGFR Inhibitor II, BIBX1382, N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
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关于此项目
经验公式（希尔记法）:
C18H19ClFN7 · 2HCl · 2H2O
化学文摘社编号:
分子量:
496.79
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
Fc1c(cc(cc1)Nc2ncnc3c2nc(nc3)NC4CCN(CC4)C)Cl
InChI
1S/C18H19ClFN7/c1-27-6-4-11(5-7-27)25-18-21-9-15-16(26-18)17(23-10-22-15)24-12-2-3-14(20)13(19)8-12/h2-3,8-11H,4-7H2,1H3,(H,21,25,26)(H,22,23,24)
InChI key
FTFRZXFNZVCRSK-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
yellow
solubility
water: 1 mg/mL, DMSO: 25 mg/mL
shipped in
ambient
Quality Level
General description
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 µM 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 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR (ErbB-1, HER-1)
EGFR (ErbB-1, HER-1)
Product competes with ATP.
Reversible: yes
Target IC50: 3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells
Other Notes
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.
Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun.281, 25.
Nuijen, B., et al. 2000. Int. J. Pharm.194, 261.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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