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PD153035 hydrochloridePotent EGFR inhibitor

PD153035 hydrochloride

Catalog No. A8199
Size Price Stock Qty
10mM (in 1mL DMSO) $65.00 In stock
Evaluation Sample $28.00 In stock
10mg $59.00 In stock
50mg $248.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PD153035 hydrochloride

Related Biological Data

PD153035 hydrochloride
Treatment of EGFR inhibitor PD153035

Related Biological Data

PD153035 hydrochloride
Treatment of EGFR inhibitor PD153035

Biological Activity

Description PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
Targets EGFR EGFR        
IC50 5.2 pM (Ki) 29 pM        

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Chemical Properties

Cas No. 153436-54-5 SDF Download SDF
Synonyms ZM252868,PD153035 HCL
Chemical Name N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC
Formula C16H14BrN3O2.HCl M.Wt 396.67
Solubility Limited solubility Storage Store at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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].

References:
[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.