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Submit ReviewPD 153035 hydrochloride
Description: EGFR-kinase inhibitor
Alternative Names: ZM 252868
Chemical Name: 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline hydrochloride
Biological Activity for PD 153035 hydrochloride
An extremely potent inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase, with an IC50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Technical Data for PD 153035 hydrochloride
| M. Wt | 396.67 |
| Formula | C16H14BrN3O2.HCl |
| Storage | Store at RT |
| CAS Number | 183322-45-4 |
| PubChem ID | 11246488 |
| InChI Key | ZJOKWAWPAPMNIM-UHFFFAOYSA-N |
| Smiles | BrC1=CC=CC(NC3=NC=NC2=CC(OC)=C(OC)C=C23)=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for PD 153035 hydrochloride
References for PD 153035 hydrochloride
References are publications that support the biological activity of the product.
Bos et al (1997) 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 2099 PMID: 9815602
Bridges et al (1996) 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. 39 267 PMID: 8568816
Fry et al (1994) A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science 265 1093 PMID: 8066447
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5 Citations for PD 153035 hydrochloride
Citations are publications that use Tocris products. Selected citations for PD 153035 hydrochloride include:
Lahey et al (2017) Signaling pathways induced by serine proteases to increase intestinal epithelial barrier function. PLoS One 12 e0180259 PMID: 28671992
Marshall et al (2018) Analysis of the Intrinsic Self-Organising Properties of Mesenchymal Stromal Cells in Three-Dimensional Co-Culture Models with Endothelial Cells. Bioengineering (Basel) 5 PMID: 30373192
Swanson et al (2012) Inhibition of epidermal growth factor receptor tyrosine kinase ameliorates collagen-induced arthritis. J Immunol 188 3513 PMID: 22393153
Taylor et al (2014) Hepatic nonparenchymal cells drive metastatic breast cancer outgrowth and partial epithelial to mesenchymal transition. Breast Cancer Res Treat 144 551 PMID: 24610032
Xu (2007) EGFR activation results in enhanced cyclooxygenase-2 expression through p38 mitogen-activated protein kinase-dependent activation of the Sp1/Sp3 transcription factors in human gliomas. Cancer Res 67 6121 PMID: 17616668
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