WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H591342
CAS#: 586347-97-9 (nitrate)
Description: PD153035 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).
Hodoodo Cat#: H591342
Name: PD153035 nitrate
CAS#: 586347-97-9 (nitrate)
Chemical Formula: C16H15BrN4O5
Exact Mass: 0.00
Molecular Weight: 423.223
Elemental Analysis: C, 45.41; H, 3.57; Br, 18.88; N, 13.24; O, 18.90
Related CAS #: 153436-54-5 (free base) 183322-45-4 (HCl) 205195-07-9 (xHCl) 586347-97-9 (nitrate)
Synonym: PD153035 nitrate; PD-153035; PD 153035; AG 1517 nitrate; AG-1517; AG1517;
IUPAC/Chemical Name: N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine nitrate
InChi Key: KIZNJUVOWWXKTJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H14BrN3O2.HNO3/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11;2-1(3)4/h3-9H,1-2H3,(H,18,19,20);(H,2,3,4)
SMILES Code: COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.O[N+]([O-])=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 423.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message
Sent On: Tue Apr 14 16:45:05 2020
20 selected items
PubMed Results
Items 1-20 of 20 (Display the 20 citations in PubMed)
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: Sun J, Cai L, Zhang K, Zhang A, Pu P, Yang W, Gao S. A pilot study on EGFR- targeted molecular imaging of PET/CT With 11C-PD153035 in human gliomas. Clin Nucl Med. 2014 Jan;39(1):e20-6. doi: 10.1097/RLU.0b013e3182a23b73. PMID: 24335566.
7: Samén E, Arnberg F, Lu L, Olofsson MH, Tegnebratt T, Thorell JO, Holmin S, Stone-Elander S. Metabolism of epidermal growth factor receptor targeting probe [11C]PD153035: impact on biodistribution and tumor uptake in rats. J Nucl Med. 2013 Oct;54(10):1804-11. doi: 10.2967/jnumed.113.120493. Epub 2013 Sep 3. PMID: 24003078.
8: Meng X, Loo BW Jr, Ma L, Murphy JD, Sun X, Yu J. Molecular imaging with 11C-PD153035 PET/CT predicts survival in non-small cell lung cancer treated with EGFR-TKI: a pilot study. J Nucl Med. 2011 Oct;52(10):1573-9. doi: 10.2967/jnumed.111.092874. Epub 2011 Sep 8. PMID: 21903741.
9: Cheng CM, Lee YJ, Wang WT, Hsu CT, Tsai JS, Wu CM, Ou KL, Yang TS. Determining the binding mode and binding affinity constant of tyrosine kinase inhibitor PD153035 to DNA using optical tweezers. Biochem Biophys Res Commun. 2011 Jan 7;404(1):297-301. doi: 10.1016/j.bbrc.2010.11.110. Epub 2010 Dec 2. PMID: 21130075.
10: Cavalheiro RA, Marin RM, Rocco SA, Cerqueira FM, da Silva CC, Rittner R, Kowaltowski AJ, Vercesi AE, Franchini KG, Castilho RF. Potent cardioprotective effect of the 4-anilinoquinazoline derivative PD153035: involvement of mitochondrial K(ATP) channel activation. PLoS One. 2010 May 17;5(5):e10666. doi: 10.1371/journal.pone.0010666. PMID: 20498724; PMCID: PMC2871796.
11: 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. EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice. Diabetes. 2009 Dec;58(12):2910-9. doi: 10.2337/db08-0506. Epub 2009 Aug 20. Retraction in: Diabetes. 2017 Jul;66(7):2059. PMID: 19696185; PMCID: PMC2780887.
12: Liu N, Li M, Li X, Meng X, Yang G, Zhao S, Yang Y, Ma L, Fu Z, Yu J. PET- based biodistribution and radiation dosimetry of epidermal growth factor receptor-selective tracer 11C-PD153035 in humans. J Nucl Med. 2009 Feb;50(2):303-8. doi: 10.2967/jnumed.108.056556. Epub 2009 Jan 21. PMID: 19164239.
13: Grunt TW, Tomek K, Wagner R, Puckmair K, Zielinski CC. The DNA-binding epidermal growth factor-receptor inhibitor PD153035 and other DNA-intercalating cytotoxic drugs reactivate the expression of the retinoic acid receptor-beta tumor-suppressor gene in breast cancer cells. Differentiation. 2007 Nov;75(9):883-90. doi: 10.1111/j.1432-0436.2007.00199.x. Epub 2007 Jul 2. PMID: 17608728.
14: Wang H, Yu JM, Yang GR, Song XR, Sun XR, Zhao SQ, Wang XW, Zhao W. Further characterization of the epidermal growth factor receptor ligand 11C-PD153035. Chin Med J (Engl). 2007 Jun 5;120(11):960-4. PMID: 17624262.
15: Grunt TW, Tomek K, Wagner R, Puckmair K, Kainz B, Rünzler D, Gaiger A, Köhler G, Zielinski CC. Upregulation of retinoic acid receptor-beta by the epidermal growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB pathways. J Cell Physiol. 2007 Jun;211(3):803-15. doi: 10.1002/jcp.20990. PMID: 17286282.
16: Jia C, Zhou Z, Liu R, Chen S, Xia R. EGF receptor clustering is induced by a 0.4 mT power frequency magnetic field and blocked by the EGF receptor tyrosine kinase inhibitor PD153035. Bioelectromagnetics. 2007 Apr;28(3):197-207. doi: 10.1002/bem.20293. PMID: 17019730.
17: Samén E, Thorell JO, Fredriksson A, Stone-Elander S. The tyrosine kinase inhibitor PD153035: implication of labeling position on radiometabolites formed in vitro. Nucl Med Biol. 2006 Nov;33(8):1005-11. doi: 10.1016/j.nucmedbio.2006.09.008. PMID: 17127174.
18: Cole GW Jr, Alleva AM, Reddy RM, Maxhimer JB, Zuo J, Schrump DS, Nguyen DM. The selective epidermal growth factor receptor tyrosine kinase inhibitor PD153035 suppresses expression of prometastasis phenotypes in malignant pleural mesothelioma cells in vitro. J Thorac Cardiovasc Surg. 2005 May;129(5):1010-7. doi: 10.1016/j.jtcvs.2004.10.040. PMID: 15867774.
19: Rocco SA, Velho JA, Marin RM, de Arruda Rolim Filho L, Vercesi AE, Rittner R, Franchini KG. High performance liquid chromatography analysis of a 4-anilinoquinazoline derivative (PD153035), a specific inhibitor of the epidermal growth factor receptor tyrosine kinase, in rat plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Mar 25;817(2):297-302. doi: 10.1016/j.jchromb.2004.12.021. PMID: 15686998.
20: He XY, Huang JA, Xie W, Jiang LY, Wang YD. [Role of PD153035 in the induction of apoptosis of XG-1 myeloma cell line]. Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 2004 Oct;26(5):492-5. Chinese. PMID: 15562758.
