324673
EGFR/ErbB-2 Inhibitor
The EGFR/ErbB-2 Inhibitor, also referenced under CAS 179248-61-4, controls the biological activity of EGFR/ErbB-2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
EGFR/ErbB-2 Inhibitor, 4557W, 4-(4-Benzyloxyanilino)-6,7-dimethoxyquinazoline
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About This Item
Empirical Formula (Hill Notation):
C23H21N3O3
CAS Number:
Molecular Weight:
387.43
MDL number:
UNSPSC Code:
12352202
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
methanol: 1 mg/mL, DMSO: 25 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
N(c3ccc(cc3)OCc4ccccc4)c1ncnc2c1cc(c(c2)OC)OC
InChI
1S/C23H21N3O3/c1-27-21-12-19-20(13-22(21)28-2)24-15-25-23(19)26-17-8-10-18(11-9-17)29-14-16-6-4-3-5-7-16/h3-13,15H,14H2,1-2H3,(H,24,25,26)
InChI key
DNOKYISWMVFYFA-UHFFFAOYSA-N
General description
A cell-permeable 4-anilino quinazoline compound that acts a potent, reversible, and ATP-competitive inhibitors of EGFR and c-erbB2 (IC50 = 20 nM and 79 nM, respectively), members of the type I growth factor receptor family that is involved in breast cancer development and progression. Shown to effectively inhibit the proliferation (IC50 = ~ 1.2-2.5 µM) of tumor cells overexpressing EGRF or c-erbB-2.
A cell-permeable, potent, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of EGFR (IC50 = 20 nM) and c-erbB2 (IC50 = 79 nM), members of the type I growth factor receptor family implicated in the development and progression of various forms of cancer, including breast and small lung cell carcinoma. Shown to effectively inhibit the proliferation (IC50 ~1.2-2.5 µM) of tumor cells overexpressing EGRF or c-erbB-2.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR
EGFR
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM and 79 nM, against EGFR and c-erbB2, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Cockerill, S., et al. 2001. Bioorg. Med. Chem. Lett.11, 1401.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
Storage Class
11 - Combustible Solids
wgk
WGK 1
Certificates of Analysis (COA)
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