Fig. 1 · Structure

Cat. No.: A10208
CAS No.: 238750-77-1
Formula: C₂₁H₃₀N₂O₆
Mol. Weight: 406.5

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Tosedostat (CHR2797)

Name: Tosedostat (CHR2797)
Brand: Adooq Bioscience
SKU: A10208
Availability: InStock

Cat. No. A10208 CAS 238750-77-1

Aminopeptidase inhibitor

CHR-2797 (Tosedostat) is a novel metalloenzyme inhibitor that exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity.

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Biological Activity

Cellular Effect

Cell Line	Activity	Value	Description	Reference
HL-60	EC50	4.7 μM	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 28803047]
MOLT-4	EC50	2.1 μM	Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay	[PMID: 28803047]
Vero	CC50	13 μM	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 28803047]

In Vitro Studies

In U937 leukemia cells, tosedostat (1 μM for 24 h) slowed fluorescent peptide breakdown relative to untreated cells. Continued degradation and variable fragment profiles showed that inhibition was incomplete and heterogeneous. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Cellular peptide processing after tosedostat exposure

Cell-based study · U937 human leukemia cells; intact-cell peptide reporter assay with ensemble and single-cell electrophoretic analysis [1]

Tosedostat slowed reporter breakdown compared with untreated cells. Multiple fragments remained detectable, and continued processing and variable single-cell patterns showed incomplete inhibition.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Fluorescent reporter fragment profiles	Qualitative electropherogram comparison Slower, ongoing reporter degradation; heterogeneous single-cell fragment patterns	[1]

Literature-Reported Treatment Conditions

Treatment concentration: 1 μM
Exposure duration: 24 h before reporter loading
Method: Exposure in fresh culture medium
Reported limits: Treatment solvent and a matched solvent-only control are not specified in the relevant treatment paragraph; comparison is to untreated cells.

Methods and source locations

Compound reported in the paper: Tosedostat; Compound label in the paper: CHR-2797

Evidence for named tosedostat; no Adooq product or lot validation.

Experimental Section: Cell culture and treatment; Results and Discussion, paragraphs accompanying Figures 2–3; Figures 2–3 and captions

Fluorescent reporter fragment profiles: Microfluidic chemical cytometry; ensemble electrophoresis and K-FAM/internal-standard controls — Figures 2–3 and captions; Results and Discussion, untreated-cell and tosedostat-treated-cell paragraphs

In Vivo Studies

In a U266 bone-marrow myeloma mouse model, intraperitoneal tosedostat attenuated tumor-associated bioluminescence compared with untreated tumor-bearing controls. The study used 75 mg/kg, 6 days per week for 4 weeks. [2]

Tosedostat in a bone-marrow myeloma mouse model

Animal study · Female NOD/SCIDγc-null mice bearing luciferase-tagged U266 human myeloma in bone marrow [2]

Tosedostat attenuated the endpoint bioluminescence signal relative to untreated tumor-bearing controls. This was a preclinical model result.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Post-treatment tumor-associated bioluminescence	Between-group comparison Lower than untreated tumor-bearing control; p<0.05	[2]

Conditions shared by the study groups

Route: Intraperitoneal
Frequency: 6 days out of 7 each week
Treatment course: 4 weeks, beginning 5 weeks after tumor-cell inoculation
Vehicle: DMSO stock diluted with PBS; final DMSO fraction unspecified

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Tosedostat monotherapy 75 mg/kg	Untreated tumor-bearing mice (assigned n=6); bortezomib comparator assigned n=9; non-inoculated untreated negative control also included.	Lower endpoint BLI versus untreated tumor-bearing mice (Figure 3B(ii), p<0.05).	[2]

Tosedostat monotherapy: Model: U266-luciferase-bearing NOD/SCIDγc-null mice; Reported limits: Tosedostat group assigned n=9; analyzed BLI n and reasons for fewer plotted points not specified. Pretreatment imaging is described as week 4 in Methods, but week 5/day 35 in Figure 3.

Methods and source locations

Compound reported in the paper: Tosedostat

Named parent-drug evidence; no Adooq lot validation.

Materials and Methods: Cell Lines, Patient Cells and Reagents; Treatment schedules; In vivo bioluminescence imaging; Statistical analysis. Results: The intra-tibial model of myeloma bone disease can be used to monitor drug response; Figure 3A–B and caption

Post-treatment tumor-associated bioluminescence: IVIS average radiance; one-way ANOVA with Bonferroni post-test (Figure 3B caption) — Figure 3B(ii), caption; Results: The intra-tibial model of myeloma bone disease can be used to monitor drug response

Tosedostat monotherapy · Materials and Methods: Cell Lines, Patient Cells and Reagents; Treatment schedules; In vivo bioluminescence imaging; Statistical analysis. Results: The intra-tibial model of myeloma bone disease can be used to monitor drug response; Figure 3A–B and caption

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	238750-77-1
Applications	Aminopeptidase inhibitor
Formula	C₂₁H₃₀N₂O₆
Molecular Weight	406.5
Synonyms	CHR2797
SMILES	CC(C)C[C@H]([C@@H](C(=O)NO)O)C(=O)N[C@@H](C1=CC=CC=C1)C(=O)OC2CCCC2

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	49 mg/mL (120.55 mM)
Water	Insoluble
Ethanol	5 mg/mL (12.3 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Michelle L. Kovarik, Pavak K. Shah, Paul M. Armistead, et al. Microfluidic Chemical Cytometry of Peptide Degradation in Single Drug-Treated Acute Myeloid Leukemia Cells Analytical Chemistry (2013). PMID: 23590517 DOI: 10.1021/ac4002029 Source material
[2] Rosemary A. Fryer, Timothy J. Graham, Emma M. Smith, et al. Characterization of a Novel Mouse Model of Multiple Myeloma and Its Use in Preclinical Therapeutic Assessment PLOS ONE (2013). PMID: 23437401 DOI: 10.1371/journal.pone.0057641 Source material