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:
| Chemical Formula: | C16H14BrN3O2.HCl | |
| CAS #: | 153436-54-5,183322-45-4 | |
| Molecular Weight: | 396.67 | |
| Purity: | >98% | |
| Appearance: | Off White | |
| Chemical Name: | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride | |
| Solubility: | Up to 10 mM in DMSO | |
| Synonyms: | PD-153035, PD 153035, PD153035, AG 1517, SU 5271 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Fry et al., A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science, 1994, 265, 1093-1095. Pubmed ID: 8066447 |
| 2. | Bos et al., PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin. Cancer Res. 1997, 3, 2099-2106. Pubmed ID: 9815602 |
| 3. | Prada et al., EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice. Diabetes, 2009, 58(12), 2910-2919. Pubmed ID: 19696185 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
