PD153035

• UNSPSC Description:

  PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

• Target Antigen:

  EGFR

• Type:

  Reference compound

• Related Pathways:

  JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/pd153035.html

• Solubility:

  DMSO : 33.33 mg/mL (ultrasonic)

• Smiles:

  COC1=C(C=C(C2=C1)N=CN=C2NC3=CC(Br)=CC=C3)OC

• Molecular Weight:

  360.21

• References & Citations:

  [1]Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.|[2]Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.|[3]Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.|[4]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.Biochim Biophys Acta Mol Basis Dis. 2023 Dec 13:166981.|Cell Death Dis. 2022 Jul 25;13(7):647.|Elife. 2015 Feb 10;4:e05178.|Gen Comp Endocrinol. 2020 Dec 1;299:113616.|Int J Stem Cells. 2022 Jun 30.|J Toxicol Sci. 2023 Nov 14;48(12):655-663.|Nat Commun. 2018 Jun 5;9(1):2174.|bioRxiv. 2024 Apr 4.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 1

• CAS Number:

  153436-54-5