PD153035

• Description:

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

• Product Name Alternative:

  SU-5271; AG1517; ZM 252868

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  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

• Purity:

  98.56

• Solubility:

  DMSO : 33.33 mg/mL (ultrasonic)

• Smiles:

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

• Molecular Formula:

  C16H14BrN3O2

• Molecular Weight:

  360.21

• Precautions:

  H302, H315, H319, H335

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• Isoform:

  EGFR/ErbB1/HER1

• Citation 01:

  Biochim Biophys Acta Mol Basis Dis. 2024 Mar;1870 (3) :166981.|bioRxiv. 2025 January 18.|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 Nov 30;15 (4) :347-358.|J Toxicol Sci. 2023 Nov 14;48 (12) :655-663.|Nat Commun. 2018 Jun 5;9 (1) :2174.|Sci Rep. 2025 Nov 17;15 (1) :40227.|bioRxiv. 2024 Apr 4.

• CAS Number:

  [153436-54-5]