539652

PKC_βII/EGFR Inhibitor

The PKC_βII/EGFR Inhibitor, also referenced under CAS 145915-60-2, controls the biological activity of PKC_βII/EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: PKC_βII/EGFR Inhibitor, CG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
• Fórmula empírica (notación de Hill): C₂₀H₁₃F₂N₃O₂
• Número de CAS: 145915-60-2
• Peso molecular: 365.33
• Número MDL: MFCD00938569
• Código UNSPSC: 12352200

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: orange
• solubilidad: DMSO: 20 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 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)
• Clave InChI: RONQPWQYDRPRGG-UHFFFAOYSA-N

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

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

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable