PD153035

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Chemical Information

Product name：PD153035	Purity：98% min
CAS NO：153436-54-5	Solubility：DMSO : 33.33 mg/mL (92.53 mM)
Molecular Formula：C₁₆H₁₄BrN₃O₂	Package：Package according to customer requirements
Molecular Weight：360.205	Storage：Store at -20℃

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Remarks

PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2).

EGFR Inhibitors Related Products:

Nazartinib; AZD3759; Erlotinib; CL-387785; AZ-5104; ARRY-380 analog; MTX-211; Osimertinib; Osimertinib mesylate; Olmutinib; Afatinib Dimaleate; Rociletinib; EGFR-IN-7

References

[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.