5.32912

CIP2A Inhibitor, TD-19

• Synonym(e): CIP2A Inhibitor, TD-19, N4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19
• Empirische Formel (Hill-System): C₃₀H₂₄N₄O₃
• CAS-Nummer: 1403933-79-8
• Molekulargewicht: 488.54
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 10 mg/mL (with warming; solution will fall out of solution at room temperature); DMF: soluble
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

A cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).

A cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem./physiol. Wirkung

Primary Target
CIP2A

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Chao, T.T., et al. 2014. J. Pharm. Exp. Ther.351,352.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable