Biochem/physiol Actions

Primary TargetCIP2A

General description

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)