PD-153035 (AG-1517)
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 202174

CAS#: 153436-54-5 (free base)

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).


Price and Availability

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Price

10mg
USD 90
100mg
USD 450
1g
USD 1450
Size
Price

25mg
USD 150
200mg
USD 650
2g
USD 2150
Size
Price

50mg
USD 250
500mg
USD 1050
5g
Ask price

PD-153035, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202174
Name: PD-153035 (AG-1517)
CAS#: 153436-54-5 (free base)
Chemical Formula: C16H14BrN3O2
Exact Mass: 359.02694
Molecular Weight: 360.2
Elemental Analysis: C, 53.35; H, 3.92; Br, 22.18; N, 11.67; O, 8.88


Related CAS #: 153436-54-5 (free base)   183322-45-4 (HCl)    

Synonym: PD-153035; PD 153035; PD153035; SU-5271; SU 5271; SU5271; AG-1517; AG 1517; AG1517; NSC 669364; NSC-669364; NSC669364; WHIP 79.

IUPAC/Chemical Name: N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine

InChi Key: LSPANGZZENHZNJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14BrN3O2/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/h3-9H,1-2H3,(H,18,19,20)

SMILES Code: COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC


Technical Data

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, not soluble in water.

Shelf Life:
>5 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).

Harmonized System Code:
293490


Additional Information

Related CAS#
183322-45-4 (PD153035 HCl)
153436-54-5 (PD153035 free base)
 
 


References

 1: 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. Epub 2011 Sep 8. PubMed PMID: 21903741.

2: 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. Epub 2010 Dec 2. PubMed PMID: 21130075.

3: 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. PubMed PMID: 20498724; PubMed Central PMCID: PMC2871796.

4: 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. Epub 2009 Aug 20. PubMed PMID: 19696185; PubMed Central PMCID: PMC2780887.

5: 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. Epub 2009 Jan 21. PubMed PMID: 19164239.

6: 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. PubMed PMID: 17624262.

7: 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. Epub 2007 Jul 2. PubMed PMID: 17608728.

8: 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. PubMed PMID: 17286282.

9: 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. PubMed PMID: 17127174.

10: 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. PubMed PMID: 17019730.

11: 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. PubMed PMID: 15867774.

12: 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. PubMed PMID: 15686998.

13: 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. PubMed PMID: 15562758.

14: Goossens JF, Bouey-Bencteux E, Houssin R, Hénichart JP, Colson P, Houssier C, Laine W, Baldeyrou B, Bailly C. DNA interaction of the tyrosine protein kinase inhibitor PD153035 and its N-methyl analogue. Biochemistry. 2001 Apr 17;40(15):4663-71. PubMed PMID: 11294633.

15: Egeblad M, Mortensen OH, van Kempen LC, Jäättelä M. BIBX1382BS, but not AG1478 or PD153035, inhibits the ErbB kinases at different concentrations in intact cells. Biochem Biophys Res Commun. 2001 Feb 16;281(1):25-31. PubMed PMID: 11178955.

16: Fredriksson A, Johnström P, Thorell JO, von Heijne G, Hassan M, Eksborg S, Kogner P, Borgström P, Ingvar M, Stone-Elander S. In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants. Life Sci. 1999;65(2):165-74. PubMed PMID: 10416822.

17: Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. 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. 1997 Nov;3(11):2099-106. PubMed PMID: 9815602.

18: Kunkel MW, Hook KE, Howard CT, Przybranowski S, Roberts BJ, Elliott WL, Leopold WR. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302. PubMed PMID: 8824347.