MedKoo Biosciences: P2045

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MedKoo product information:

P2045

MedKoo Code#: 202114

Name: P2045

CAS#: 259746-53-7

Synonym: CA Index Name: Cyclo(N-methyl-L-homocysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl), (11')-thioether with 3-[(2-mercaptoacetyl)amino]-L-alanyl-4-amino-L-phenylalanyl-L-cysteinyl-L-threonyl-L-serine. Other Names: Cyclo(N-methyl-L-homocysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl), (11')-thioether with 3-[(mercaptoacetyl)amino]-L-alanyl-4-amino-L-phenylalanyl-L-cysteinyl-L-threonyl-L-serine (9CI); 119: PN: WO02060491 PAGE: 51 claimed protein; P 2045

　

IUPAC/Chemical name:

(2S,5S,8R,11S,14S)-21-((2S,5S,8R,11S,14S,17S)-8-((1H-indol-2-yl)methyl)-14-acetyl-11-(4-aminobutyl)-17-benzyl-5-(4-hydroxybenzyl)-3,6,9,12,15,18-hexaoxo-1,4,7,10,13,16-hexaazacyclooctadecan-2-yl)-14-amino-11-(4-aminobenzyl)-5-((R)-1-hydroxyethyl)-2-(hydroxymethyl)-8-(mercaptomethyl)-4,7,10,13,17-pentaoxo-19-thia-3,6,9,12,16-pentaazahenicosan-1-oic acid

Chemical structure:

Theoretical analysis:

Chemical Formula: C67H87N15O17S2
Exact Mass: 1437.58458
Molecular Weight: 1438.63
m/z: 1437.58458 (100.0%), 1438.58793 (72.5%), 1439.59129 (25.9%), 1439.58037 (9.0%), 1440.58373 (6.5%), 1440.59464 (6.1%), 1438.58161 (5.5%), 1439.58497 (4.0%), 1439.58882 (3.5%), 1440.59218 (2.5%), 1441.58708 (2.3%), 1438.58397 (1.6%), 1440.58832 (1.4%), 1439.58732 (1.2%), 1441.59800 (1.0%), 1438.59085 (1.0%)
Elemental Analysis: C, 55.94; H, 6.10; N, 14.60; O, 18.91; S, 4.46.

Availability and price:

This agent is not in stock, which may be available through custom synthesis.

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Information about this agent

P2045 is a somatostatin analog cyclopeptide. Rhenium Re188 P2045 is the Rhenium complex of P2045. Phase I clinical trials demonstrated that Re-188 P2045 was well tolerated. Tc-99m P2045 imaging allows identification of patients who may benefit from this treatment. Although responses were not seen, survival for these heavily pretreated patients is interesting and merits further research. [source: J Thorac Oncol. 2009 Dec;4(12):1550-4.]

Current developer: Xanthus Pharmaceuticals.

References

1: Edelman MJ, Clamon G, Kahn D, Magram M, Lister-James J, Line BR. Targeted radiopharmaceutical therapy for advanced lung cancer: phase I trial of rhenium Re188 P2045, a somatostatin analog. J Thorac Oncol. 2009 Dec;4(12):1550-4. PubMed PMID: 19884860.

2: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Oct;29(8):547-83. PubMed PMID: 18040531.

3: Cyr JE, Pearson DA, Wilson DM, Nelson CA, Guaraldi M, Azure MT, Lister-James J, Dinkelborg LM, Dean RT. Somatostatin receptor-binding peptides suitable for tumor radiotherapy with Re-188 or Re-186. Chemistry and initial biological studies. J Med Chem. 2007 Mar 22;50(6):1354-64. Epub 2007 Feb 22. PubMed PMID: 17315859.

4: Weiner RE, Thakur ML. Radiolabeled peptides in oncology: role in diagnosis and treatment. BioDrugs. 2005;19(3):145-63. Review. PubMed PMID: 15984900.

5: Rogers BE, Chaudhuri TR, Reynolds PN, Della Manna D, Zinn KR. Non-invasive gamma camera imaging of gene transfer using an adenoviral vector encoding an epitope-tagged receptor as a reporter. Gene Ther. 2003 Jan;10(2):105-14. PubMed PMID: 12571639.

6: Hemminki A, Zinn KR, Liu B, Chaudhuri TR, Desmond RA, Rogers BE, Barnes MN, Alvarez RD, Curiel DT. In vivo molecular chemotherapy and noninvasive imaging with an infectivity-enhanced adenovirus. J Natl Cancer Inst. 2002 May 15;94(10):741-9. PubMed PMID: 12011224.

7: Zinn KR, Chaudhuri TR, Krasnykh VN, Buchsbaum DJ, Belousova N, Grizzle WE, Curiel DT, Rogers BE. Gamma camera dual imaging with a somatostatin receptor and thymidine kinase after gene transfer with a bicistronic adenovirus in mice. Radiology. 2002 May;223(2):417-25. PubMed PMID: 11997547.

8: Chaudhuri TR, Rogers BE, Buchsbaum DJ, Mountz JM, Zinn KR. A noninvasive reporter system to image adenoviral-mediated gene transfer to ovarian cancer xenografts. Gynecol Oncol. 2001 Nov;83(2):432-8. PubMed PMID: 11606113.

9: Zinn KR, Chaudhuri TR, Buchsbaum DJ, Mountz JM, Rogers BE. Detection and measurement of in vitro gene transfer by gamma camera imaging. Gene Ther. 2001 Feb;8(4):291-9. PubMed PMID: 11313803.

10: Zinn KR, Chaudhuri TR, Buchsbaum DJ, Mountz JM, Rogers BE. Simultaneous evaluation of dual gene transfer to adherent cells by gamma-ray imaging. Nucl Med Biol. 2001 Feb;28(2):135-44. PubMed PMID: 11295424.

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