PD153035 is an ATP-competitive, quinazoline-based, potent inhibitor of EGFR with an IC50 of 29 pM and Ki of 5.2 pM. [1] PD153035 is selective against PDGFR, FGFR, CSF-1, IR, and Src at concentrations as high as 50 uM. EGF-dependent mitogenesis was inhibited 50% by PD153035 at a concentration of 80 nM. [1]

In cell lines with high levels of EGFR overexpression (Difi, A431, MDA-MB-468), complete inhibition of EGFR autophosphorylation was achieved at concentrations of ?75 nM. In all other EGFR-expressing cell lines, receptor phosphorylation was completely inhibited at dosages of 350 nM or higher. [2]

PD153035 treatment decreases protein expression of iNOS, TNFa, and IL-6, suggesting reduction of M1 proinflammatory state in ATMs, resulting in an improvement in insulin signaling and sensitivity. Prolonged treatment was shown to improve glucose tolerance, reduction in insulin resistance, and a decrease in insulin receptor substrate-1 Ser307 phosphorylation in JNK and inhibition of NF-kB kinase (IKKb) activation. [3]

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.