PD153035 Hydrochloride

• CAT Number: I002379
• CAS Number: 183322-45-4
• Molecular Formula: C16H14BrN3O2 • HCl
• Molecular Weight: 396.7
• Purity: ≥95%
• Synonyms: AG-1517
• Target: EGFR
• Solubility: DMSO <1.2mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: Room Temperature
• IC50: 5.2/29 pM(Ki/IC50) [1]
• IUPAC Name: N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine;hydrochloride
• 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

PD153035 HCl (Cat No.: I002379) is a highly potent and specific inhibitor of the Epidermal Growth Factor Receptor (EGFR). Its remarkable binding affinity is reflected in its Ki (inhibition constant) of 5.2 pM and an IC50 (half-maximal inhibitory concentration) of 29 pM. PD153035 HCl demonstrates exceptional selectivity for EGFR, with minimal impact on other receptor kinases, including PGDFR, FGFR, CSF-1, InsR, and Src. This makes it a valuable tool for researchers studying EGFR-related signaling pathways and potential therapeutic interventions targeting EGFR-driven diseases, particularly in the field of oncology. If you need to, please contact us in time, and we will reply to you as soon as possible within 24 hours.

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.