WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205648

CAS#: 238750-77-1

Description: Tosedostat is a proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death.

Price and Availability


USD 150
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USD 450
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Tosedostat, 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.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 205648
Name: Tosedostat
CAS#: 238750-77-1
Chemical Formula: C21H30N2O6
Exact Mass: 406.21039
Molecular Weight: 406.47
Elemental Analysis: C, 62.05; H, 7.44; N, 6.89; O, 23.62

Synonym: CHR2797; CHR-2797; CHR 2797; Tosedostat.

IUPAC/Chemical Name: (S)-cyclopentyl 2-((R)-2-((S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl)-4-methylpentanamido)-2-phenylacetate


InChi Code: InChI=1S/C21H30N2O6/c1-13(2)12-16(18(24)20(26)23-28)19(25)22-17(14-8-4-3-5-9-14)21(27)29-15-10-6-7-11-15/h3-5,8-9,13,15-18,24,28H,6-7,10-12H2,1-2H3,(H,22,25)(H,23,26)/t16-,17+,18+/m1/s1

SMILES Code: O=C(OC1CCCC1)[C@@H](NC([C@@H]([C@H](O)C(NO)=O)CC(C)C)=O)C2=CC=CC=C2

Technical Data

Solid powder

>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).

Soluble in DMSO, not 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:

Additional Information



1. Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia By Jenkins, Christopher; Hewamana, Saman; Krige, David; Pepper, Chris; Burnett, Alan From Leukemia Research (2011), 35(5), 677-681.

2. Phase I/II clinical study of tosedostat, an inhibitor of aminopeptidases, in patients with acute myeloid leukemia and myelodysplasia By Loewenberg, Bob; Morgan, Gareth; Ossenkoppele, Gert I.; Burnett, Alan K.; Zachee, Pierre; Duehrsen, Ulrich; Dierickx, Daan; Mueller-Tidow, Carsten; Sonneveld, Pieter; Krug, Utz; et al From Journal of Clinical Oncology (2010), 28(28), 4333-4338.

3. A Phase Ib dose-escalation study to evaluate safety and tolerability of the addition of the aminopeptidase inhibitor tosedostat (CHR-2797) to paclitaxel in patients with advanced solid tumours By van Herpen, C. M. L.; Eskens, F. A. L. M.; de Jonge, M.; Desar, I.; Hooftman, L.; Bone, E. A.; Timmer-Bonte, J. N. H.; Verweij, J. From British Journal of Cancer (2010), 103(9), 1362-1368.

4. Quinazoline derivatives and methods of treatment By Tung, Roger From U.S. Pat. Appl. Publ. (2010), US 20100260674 A1 20101014.

5. Surface topographies for non-toxic bioadhesion control By Brennan, Anthony B.; Long, Christopher James; Bagan, Joseph W.; Schumacher, James Frederick; Spiecker, Mark M. From U.S. Pat. Appl. Publ. (2010), US 20100226943 A1 20100909.

6. Starving to succeed By Davenport, Emma L.; Aronson, Lauren I.; Davies, Faith E. From Autophagy (2009), 5(7), 1052-1054.

7. Gene expression biomarkers of aminopeptidase inhibition in tumor-derived cell lines By Krige, David; Drummond, Alan Hastings From PCT Int. Appl. (2009), WO 2009098451 A2 20090813.

8. A First-in-Man Phase I and Pharmacokinetic Study on CHR-2797 (Tosedostat), an Inhibitor of M1 Aminopeptidases, in Patients with Advanced Solid Tumors By Reid, Alison H. M.; Protheroe, Andrew; Attard, Gerhardt; Hayward, Nikki; Vidal, Laura; Spicer, James; Shaw, Heather M.; Bone, Elizabeth A.; Carter, Joanne; Hooftman, Leon; et al From Clinical Cancer Research (2009), 15(15), 4978-4985.

9. Tosedostat: aminopeptidase inhibitor oncolytic By Owen, R. T.; Castaner, R.; Bolos, J. From Drugs of the Future (2009), 34(2), 115-118.

10. Aminopeptidase inhibition as a targeted treatment strategy in myeloma By Moore, Hannah E.; Davenport, Emma L.; Smith, Emma M.; Muralikrishnan, Srikanth; Dunlop, Alan S.; Walker, Brian A.; Krige, David; Drummond, Alan H.; Hooftman, Leon; Morgan, Gareth J.; et al From Molecular Cancer Therapeutics (2009), 8(4), 762-770.

11. Dosing schedules of leukotriene synthesis inhibitors for human therapy By Hermann, David J.; Hartman, Daniel L.; Van Ess, Peter James; Wang, Wenping From PCT Int. Appl. (2008), WO 2009002746 A1 20081231.

12. CHR-2797: An Antiproliferative Aminopeptidase Inhibitor that Leads to Amino Acid Deprivation in Human Leukemic Cells By Krige, David; Needham, Lindsey A.; Bawden, Lindsay J.; Flores, Nicolas; Farmer, Hannah; Miles, Lauren E. C.; Stone, Erica; Callaghan, Juliana; Chandler, Stephen; Clark, Vanessa L.; et al From Cancer Research (2008), 68(16), 6669-6679.

13. Preparation of cytostatic hydroxamic acid derivatives of amino acids By Pearson, Lindsey Ann; Ayscough, Andrew Paul; Huxley, Philip; Drummond, Alan From U.S. (2002), US 6462023 B1 20021008.

14. Antibacterial hydroxamic acid derivatives By Hunter, Michael George; Beckett, Raymond Paul; Clements, Martin John; Whittaker, Mark From PCT Int. Appl. (2000), WO 2000044373 A1 20000803.

15. Hydroxamic acid derivatives as inhibitors of beta-amyloid production By Johnstone, Mandy; Ayscough, Andrew Paul From PCT Int. Appl. (2000), WO 2000009119 A1 20000224.

16. Hydroxamic acid derivatives of amino acids as antiinflammatories By Ayscough, Andrew Paul; Whittaker, Mark From PCT Int. Appl. (1999), WO 9940910 A1 19990819.

17. Aminopeptidase N (CD13) as a target for cancer chemotherapy By Wickstrom Malin; Larsson Rolf; Nygren Peter; Gullbo Joachim From Cancer science (2011), 102(3), 501-8.