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Merck
CN

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.

Synonym(s):

PKCβII/EGFR Inhibitor, CG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353

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About This Item

Empirical Formula (Hill Notation):
C20H13F2N3O2
CAS Number:
145915-60-2
Molecular Weight:
365.33
MDL number:
MFCD00938569
UNSPSC Code:
12352200

Key Documents

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Quality Level

100

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

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

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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

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.

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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