539652
PKCβII/EGFR Inhibitor
The PKCβII/EGFR Inhibitor, also referenced under CAS 145915-60-2, controls the biological activity of PKCβII/EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
PKCβII/EGFR Inhibitor, CG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
产品名称
PKCβII/EGFR Inhibitor, The PKCβII/EGFR Inhibitor, also referenced under CAS 145915-60-2, controls the biological activity of PKCβII/EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
InChI
1S/C20H13F2N3O2/c21-11-1-5-13(6-2-11)23-17-9-15-16(20(27)25-19(15)26)10-18(17)24-14-7-3-12(22)4-8-14/h1-10,23-24H,(H,25,26,27)
InChI key
RONQPWQYDRPRGG-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
orange
solubility
DMSO: 20 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR
EGFR
Product competes with ATP.
Reversible: yes
Target IC50: 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM against EGFR and PKC isozymes α, βI, and βII, respectively
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable symmetrical phthalimide compound that acts as a potent, reversible, and ATP-competitive inhibitor of EGFR and PKC isozymes α, βI, and βII (IC50 = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.
Other Notes
Kouroedov, A., et al. 2004. Circulation110, 91.
Lee, S.W., et al. 2003. Bone32, 217.
Perrotti, D., et al. 1998. EMBO J.17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol.10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res.1, 813.
Trinks, U., et al. 1994. J. Med. Chem.37, 1015.
Lee, S.W., et al. 2003. Bone32, 217.
Perrotti, D., et al. 1998. EMBO J.17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol.10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res.1, 813.
Trinks, U., et al. 1994. J. Med. Chem.37, 1015.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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