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Chemical Structure| 238750-77-1 Chemical Structure| 238750-77-1

Structure of Tosedostat
CAS No.: 238750-77-1

Chemical Structure| 238750-77-1

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Tosedostat is a aminopeptidase inhibitor with IC50 of 220, > 1000 nM for aminopeptidase N and aminopeptidase B respectively.

Synonyms: CHR-2797

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Product Details of Tosedostat

CAS No. :238750-77-1
Formula : C21H30N2O6
M.W : 406.47
SMILES Code : ONC([C@@H](O)[C@@H](CC(C)C)C(N[C@@H](C1=CC=CC=C1)C(OC2CCCC2)=O)=O)=O
Synonyms :
CHR-2797
MDL No. :MFCD13185162
InChI Key :FWFGIHPGRQZWIW-SQNIBIBYSA-N
Pubchem ID :15547703

Safety of Tosedostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Candida glabrata ATCC 90030 4 μg/ml 6 h and 24 h To evaluate the antifungal activity of Tosedostat against Candida glabrata, results showed inhibitory effects. PMC3910836
Candida albicans SC5314 4 μg/ml 6 h and 24 h To evaluate the antifungal activity of Tosedostat against Candida albicans, results showed inhibitory effects. PMC3910836
U937 acute myeloid leukemia cells 1 μM 24 hours To investigate the inhibitory effect of Tosedostat on peptide degradation in U937 cells, results showed that Tosedostat significantly inhibited the degradation process. PMC3671928
U937 cells (human acute myeloid leukemia cells) 1, 2, 4, 8, 16 μM 95 days To evaluate the effect of Tosedostat on peptidase activity in U937 cells. Results showed changes in peptide degradation patterns with drug treatment, with the number of fragment peaks decreasing as dose increased. PMC3940261
RPMI-8226 cells 1 µM 24 hours To study the synergistic effect of Tosedostat with HDAC inhibitor CHR-3996, results showed that the combination significantly activates NFκB signaling pathway and induces apoptosis. PMC4627310
H929 cells 1 µM 24 hours To study the synergistic effect of Tosedostat with HDAC inhibitor CHR-3996, results showed that the combination significantly activates NFκB signaling pathway and induces apoptosis. PMC4627310

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID IL2Rγ-/- mice Multiple myeloma xenograft model Intra-peritoneal injection 75 mg/kg Daily administration for up to 28 days To study the in vivo synergistic effect of Tosedostat with HDAC inhibitor CHR-3996, results showed that the combination significantly inhibits tumor growth. PMC4627310

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02452346 Myelodysplastic Syndrome PHASE2 COMPLETED 2017-10-25 Weill Cornell Medical College,... More >> New York, New York, 10065, United States Less <<
NCT00737555 Solid Tumor PHASE1 COMPLETED 2025-03-08 UMC St Radboud, Nijmegen, 6525... More >> GA, Netherlands|Erasmus MC University Medical Centre- Location Centrum, Rotterdam, 3015 CE, Netherlands Less <<
NCT00780598 Acute Myeloid Leukemia|AML PHASE2 COMPLETED 2025-03-11 UCLA School of Medicine, Los A... More >>ngeles, California, 90095, United States|Washington Cancer Institute, Washington, District of Columbia, 20010, United States|M.D. Anderson Cancer Center Orlando, Orlando, Florida, 32806, United States|Emory University Clinic, Atlanta, Georgia, 30322, United States|University of Chicago Medical Center, Chicago, Illinois, 60637, United States|University of Michigan Health System, Ann Arbor, Michigan, 48109-0008, United States|Washington University, Oncology/Bone Marrow Transplant, St Louis, Missouri, 63110, United States|John Theurer Cancer Center, Hackensack University Medical Center,, Hackensack, New Jersey, 07601, United States|Montefiore Medical Center Weiler Division, Bronx, New York, 10461, United States|Monter Cancer Center, Lake Success, New York, 11042, United States|Memorial Sloan-Kettering Cancer Center, New York, New York, 10065, United States|Weill Cornell Medical College - New York Presbyterian Hospital, New York, New York, 10065, United States|Stony Brook University Medical Center, Stony Brook, New York, 11794-7007, United States|Duke Univeristy Medical Center, Durham, North Carolina, 27710, United States|Taussig Cancer Institute, Cleveland, Ohio, 44195, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Froedtert Hospital, Milwaukee, Wisconsin, 53226-3596, United States|Princess Margaret Hopsital, Toronto, Ontario, M5G 2M9, Canada|Royal Victoria Hospital, Montreal, Quebec, H3A 1A1, Canada|VUMC, Amsterdam, 1081 HV, Netherlands|Erasmus MC, Rotterdam, 3008 AE, Netherlands Less <<
NCT01180426 Acute Myeloid Leukemia PHASE2 UNKNOWN 2025-06-13 UCLA Division of Hematology/On... More >>cology, Los Angeles, California, 90095, United States|University of Michigan, Ann Arbor, Michigan, 48109-2800, United States|John Theurer Cancer Center, Hackensack, New Jersey, 07601, United States|New York Presbyterian Hospitacl, New York, New York, 10021, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|MD Anderson, Houston, Texas, 77030-4009, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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