A potent EGFR kinase inhibitor
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Alternative(s)
14879PD 153035 (hydrochloride)
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PD 153035

Item No. 18080

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-bromophenyl)-6,7-dimethoxy-4-quinazolinamine
CAS Number
153436-54-5
Synonyms
  • AG-1517
  • NSC 669364
  • SU 5271
Molecular Formula
C16H14BrN3O2
Formula Weight
360.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.3 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2)(1:8): 0.11 mg/mlEthanol: 0.2 mg/ml
λmax
222, 255, 346 nm
SMILES
COC(C(OC)=C1)=CC2=C1N=CN=C2NC3=CC(Br)=CC=C3
InChi Code
InChI=1S/C16H14BrN3O2/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)
InChi Key
LSPANGZZENHZNJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PD 153035 is a potent, reversible inhibitor of EGFR kinase (Ki = 5.2 pM; IC50 = 29 pM).1 It less effectively inhibits HER2 (IC50 = 2.3 µM) and has little effect on several other receptor and non-receptor tyrosine kinases.1 PD 153035 has been shown to rapidly suppress autophosphorylation of EGFR in fibroblasts and human epidermoid carcinoma cells, as well as to selectively block EGF-mediated cellular processes, including mitogenesis and early gene expression.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fry, D.W., Kraker, A.J., McMichael, A., et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science 265(5175), 1093-1095 (1994).

    2. Bos, M., Mendelsohn, J., Kim, Y.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. 3(11), 2099-2106 (1997).

    3. Rae, J.M., and Lippman, M.E. Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitors. Breast Cancer Res. Treat. 83(2), 99-107 (2004).