Name: PD153035 hydrochloride
Price: 204.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    PD153035 (4-(3-Bromoanilino)-6,7-dimethoxyquinazoline) is an extremely potent epidermal growth factor receptor (EGFR) inhibitor that competitively binds at the ATP site with the half maximal inhibition concentration IC50 of 0.025 nM resulting in the inhibition of the tyrosine kinase activity of the EGFR [1].
    PD153035 has been found to inhibit EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively leading to suppression of proliferation and clonogenicity in those cell lines [2].
    Besides exerting potent inhibition against EGFRs, PD153035 also inhibits the closely related HER2/neu receptor but to a lesser degree [2].
    
    [1] Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, Denny WA. 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] Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. 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 Nov;3(11):2099-106.
- Properties
  - Alternative Name
    
    ZM252868,PD153035 HCL; N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
    
    CAS Number
    
    153436-54-5
    
    Molecular Formula
    
    C16H14BrN3O2·HCl
    
    Molecular Weight
    
    396.67
    
    Appearance
    
    A solid
    
    Purity
    
    99.60%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥3.97 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at RT
    
    * For Research Use Only
- Reference
  - 1. Duggan BM, Foley KP, et al."Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia." Sci Rep. 2017 May 8;7(1):1578. PMID:28484277

PD153035 hydrochloride

PD153035 hydrochloride

Background

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