Molecular structure of PD 153035, CAS Number: 153436-54-5
PD 153035 (CAS 153436-54-5)
See product citations (5)
Alternate Names:
Tyrphostin AG 1517; 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline
Application:
PD 153035 is 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
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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.
PD 153035 (CAS 153436-54-5) References
- Signaling-inactive epidermal growth factor receptor/ligand complexes in intact carcinoma cells by quinazoline tyrosine kinase inhibitors. | Lichtner, RB., et al. 2001. Cancer Res. 61: 5790-5. PMID: 11479217
- 1,4-dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase. | Lee, JY., et al. 2001. Arch Pharm (Weinheim). 334: 357-60. PMID: 11822173
- Role of Ras in metal-induced EGF receptor signaling and NF-kappaB activation in human airway epithelial cells. | Wu, W., et al. 2002. Am J Physiol Lung Cell Mol Physiol. 282: L1040-8. PMID: 11943669
- Heparin-binding EGF-like growth factor gene transcription regulated by Cdx2 in the intestinal epithelium. | Uesaka, T., et al. 2002. Am J Physiol Gastrointest Liver Physiol. 283: G840-7. PMID: 12223343
- Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitors. | Rae, JM. and Lippman, ME. 2004. Breast Cancer Res Treat. 83: 99-107. PMID: 14997040
- Met5-enkephalin-induced cardioprotection occurs via transactivation of EGFR and activation of PI3K. | Cao, Z., et al. 2005. Am J Physiol Heart Circ Physiol. 288: H1955-64. PMID: 15563540
- Epidermal growth factor synergistically enhances interleukin-8 production in human gingival fibroblasts stimulated with interleukin-1beta. | Yucel-Lindberg, T. and Brunius, G. 2006. Arch Oral Biol. 51: 892-8. PMID: 16678783
- Diesel exhaust particulate-induced activation of Stat3 requires activities of EGFR and Src in airway epithelial cells. | Cao, D., et al. 2007. Am J Physiol Lung Cell Mol Physiol. 292: L422-9. PMID: 17028263
- LTD₄ induces HB-EGF-dependent CXCL8 release through EGFR activation in human bronchial epithelial cells. | McGovern, T., et al. 2010. Am J Physiol Lung Cell Mol Physiol. 299: L808-15. PMID: 20889674
- Domain-based biosensor assay to screen for epidermal growth factor receptor modulators in live cells. | Antczak, C., et al. 2012. Assay Drug Dev Technol. 10: 24-36. PMID: 22280060
- A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. | Fry, DW., et al. 1994. Science. 265: 1093-5. PMID: 8066447
- 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. | Bridges, AJ., et al. 1996. J Med Chem. 39: 267-76. PMID: 8568816
- Cytoskeletal and morphological changes associated with the specific suppression of the epidermal growth factor receptor tyrosine kinase activity in A431 human epidermoid carcinoma. | Nelson, JM. and Fry, DW. 1997. Exp Cell Res. 233: 383-90. PMID: 9194500
- EGF-receptor tyrosine kinase inhibition induces keratinocyte growth arrest and terminal differentiation. | Peus, D., et al. 1997. J Invest Dermatol. 109: 751-6. PMID: 9406816
- Inhibition of epidermal growth factor receptor kinase induces protease-dependent apoptosis in human colon cancer cells. | Karnes, WE., et al. 1998. Gastroenterology. 114: 930-9. PMID: 9558281
Inhibitor of:
EGFR, HB-EGF, Ig J chain, Olfr570, PICH_Ercc6l, and ZFP111.Activator of:
BC061194, LET-23, N-type Ca CP α1B, P/Q-type calcium channel α1A, TM4SF1, TMEM219, and VSTM1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PD 153035, 5 mg | sc-205909 | 5 mg | $146.00 |