PD 153035An extremely potent and specific inhibitor of EGFR tyrosine kinase activity

PD 153035 (CAS 153436-54-5)

PD 153035 | CAS 153436-54-5 is rated 5.0 out of 5 by 1.
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Synonym: Tyrphostin AG 1517; 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline
Application: An extremely potent and specific inhibitor of EGFR tyrosine kinase activity
CAS Number: 153436-54-5
Purity: >98%
Molecular Weight: 360.21
Molecular Formula: C16H14BrN3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PD 153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of the EGFR (epidermal growth factor receptor; IC50 = 25 pM; Kι = 6 pM). PD 153035 rapidly suppresses auto-phosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. PD 153035 also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation.


References

1. Fry, D.W., et al. 1994. Science. 265: 1093-1095. PMID: 8066447
2. Bridges, A.J., et al. 1996. J. Med. Chem. 39: 267-276. PMID: 8568816

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at -20° C
Melting Point :
190.23° C (Predicted)
Boiling Point :
472.15° C at 760 mmHg (Predicted)
Density :
1.50 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
EGFR: IC50 = 0.025 nM (human); Balb/MK: IC50 = 0.2 µM (Sus scrofa); SK-BR-3: IC50 = 0.82 µM (human); FBPase: IC50 = 1 µM (human); Flk-1: IC50 = 1.49 µM (human)
Ki Data :
EGFR: Ki= 0.006 nM (human)
pK Values :
pKb: 5.55 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
4705
MDL Number :
MFCD00934896
SMILES :
COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC

Download SDS (MSDS)

Certificate of Analysis

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PD 153035  Product Citations

See how others have used PD 153035. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 28797129  Go, YY. et al. 2017. PLoS ONE. 12: e0182716.

PMID: # 27086143  Centuori, SM. et al. 2016. Biochim. Biophys. Acta. 1861: 663-70.

PMID: # 24982815  Zhu, HJ. et al. 2014. Am J Nucl Med Mol Imaging. 4: 293-302.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Lin YC; et al Lin YC; et al. (PubMed ID:24106166) confirmed that PD 153035, an EGFR inhibitor, partially supresses the IL-8 gene in human gastric carcinoma cells. -SCBT Publication Review
Date published: 2015-03-16
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