AG-1517 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).
CAS Number: 153436-54-5
Molecular Weight: 360.21
Chemical Name: N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not soluble in water.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AG-1517 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM. AG-1517 has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. AG-1517 rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. AG-1517 causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC50 is less than 1 pM in most cases.
AG-1517 levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of AG-1517 falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors.
- Zhang GN, Zhang YK, Wang YJ, Gupta P, Ashby CR Jr, Alqahtani S, Deng T, Bates SE, Kaddoumi A, Wurpel JND, Lei YX, Chen ZS. Epidermal growth factor receptor (EGFR) inhibitor PD153035 reverses ABCG2-mediated multidrug resistance in non- small cell lung cancer: In vitro and in vivo. Cancer Lett. 2018 Jun 28;424:19-29. doi: 10.1016/j.canlet.2018.02.040. Epub 2018 Mar 5. PMID: 29518481.
- Prada PO, Ropelle ER, Mourão RH, de Souza CT, Pauli JR, Cintra DE, Schenka A, Rocco SA, Rittner R, Franchini KG, Vassallo J, Velloso LA, Carvalheira JB, Saad MJA. Statement of Retraction. EGFR Tyrosine Kinase Inhibitor (PD153035) Improves Glucose Tolerance and Insulin Action in High-Fat Diet-Fed Mice. Diabetes 2009;58:2910-2919. DOI: 10.2337/db08-0506. PMID: 19696185. Diabetes. 2017 Jul;66(7):2059. doi: 10.2337/db17-rt07a. Epub 2017 Apr 27. PMID: 28450418; PMCID: PMC5482084.
- Prada PO, Ropelle ER, Mourão RH, de Souza CT, Pauli JR, Cintra DE, Schenka A, Rocco SA, Rittner R, Franchini KG, Vassallo J, Velloso LA, Carvalheira JB, Saad MJ. Expression of Concern. EGFR Tyrosine Kinase Inhibitor (PD153035) Improves Glucose Tolerance and Insulin Action in High-Fat Diet-Fed Mice. Diabetes 2009;58:2910-2919. DOI: 10.2337/db08-0506. PMID: 19696185. Diabetes. 2017 Apr;66(4):1098. doi: 10.2337/db17-ec04a. Epub 2017 Feb 10. PMID: 28188141; PMCID: PMC6973588.
- Dai D, Li XF, Wang J, Liu JJ, Zhu YJ, Zhang Y, Wang Q, Xu WG. Predictive efficacy of (11)C-PD153035 PET imaging for EGFR-tyrosine kinase inhibitor sensitivity in non-small cell lung cancer patients. Int J Cancer. 2016 Feb 15;138(4):1003-12. doi: 10.1002/ijc.29832. Epub 2015 Sep 22. PMID: 26334931.
- Leon Carrion S, Sutter CH, Sutter TR. Combined treatment with sodium butyrate and PD153035 enhances keratinocyte differentiation. Exp Dermatol. 2014 Mar;23(3):211-4. doi: 10.1111/exd.12333. PMID: 24451036; PMCID: PMC4046644.
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