PD 153035 Hydrochloride

• CAT Number: I001926
• CAS Number: 153436-54-5
• Molecular Formula: C₁₆H₁₄BrN₃O₂.HCl
• Molecular Weight: 396.67
• Purity: ≥95%
• Target: EGFR
• Solubility: 10 mM in DMSO
• Storage: Store at RT
• IC50: 5.2/29 pM(Ki/IC50) [1]
• InChI: InChI=1S/C16H14BrN3O2.ClH/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11;/h3-9H,1-2H3,(H,18,19,20);1H
• InChIKey: ZJOKWAWPAPMNIM-UHFFFAOYSA-N
• SMILES: COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC.Cl

PD 153035 hydrochloride(CAT: I001926) represents a breakthrough in the realm of targeted kinase inhibition and cancer research. This compound, also referred to as PD153035 (ZM 252868; AG 1517), stands out as a potent and specific inhibitor of the epidermal growth factor receptor (EGFR). With a remarkable Ki of 5.2 pM and IC50 of 29 pM, PD 153035 hydrochloride demonstrates exceptional selectivity and affinity for EGFR. Notably, its minimal impact on other receptors such as PDGFR, FGFR, CSF-1, InsR, and Src enhances its specificity.

Reference

[1]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994, 265(5175), 1093-1095.
[2]. Bos M, 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(11), 2099-2106.
[3]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996, 13(4), 295-302.
[4]. Prada PO, 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.