1. Metabolic Enzyme/Protease
  2. Aminopeptidase
  3. Tosedostat

Tosedostat (Synonyms: CHR-2797)

Cat. No.: HY-14807 Purity: 99.65%
Handling Instructions

Tosedostat is an aminopeptidase inhibitor.

For research use only. We do not sell to patients.

Tosedostat Chemical Structure

Tosedostat Chemical Structure

CAS No. : 238750-77-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 134 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
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25 mg USD 490 In-stock
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50 mg USD 800 In-stock
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100 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Tosedostat is an aminopeptidase inhibitor.

IC50 & Target

Aminopeptidase[1]

In Vitro

Treatment of HL-60 cells with Tosedostat (CHR-2797) leads to an increase in the secretion of Stanniocalcin 2 (STC2) protein into the growth medium. Increases in SLC7A11 expression are detectable at 60 nM Tosedostat and as early as 2 h posttreatment. The IC50s for inhibition of proliferation by Tosedostat in U-937 and HuT 78 cell lines are 10 nM and >10 μM, respectively. Tosedostat treatment increases expression of amino acid deprivation response (AADR) genes in U-937 cells but not in HuT 78 cells[1]. By 24 h with 0.01 μM Tosedostat the mean MCA production is reduced to 77.8% of the untreated control cells; similarly the MCA production is reduced to 51.3% with 1 μM, 38.5% with 5 μM, and 35.3% with 10 μM Tosedostat[2].

In Vivo

Tosedostat (CHR-2797) is active as an anticancer agent in vivo in rodent cancer models, and a dose-response relationship has been shown in two models. The effect of Tosedostat is less apparent when the tumor burden is higher before treatment[1].

Clinical Trial
Molecular Weight

406.47

Formula

C₂₁H₃₀N₂O₆

CAS No.

238750-77-1

SMILES

O=C(OC1CCCC1)[[email protected]@H](NC([[email protected]@H]([[email protected]](O)C(NO)=O)CC(C)C)=O)C2=CC=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (61.51 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4602 mL 12.3010 mL 24.6021 mL
5 mM 0.4920 mL 2.4602 mL 4.9204 mL
10 mM 0.2460 mL 1.2301 mL 2.4602 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Cells are seeded at a density of 4×104/mL, cultured for 24 h, then treated with 0.06 to 6 μM Tosedostat (CHR-2797) for 24 h. After treatment, 5×104 cells are washed with PBS and seeded in 100 μL Cys/Met-free RPMI 1640 containing Tosedostat, supplemented with 10% dialyzed FBS. 1.5 μCi [35S]Cys/Met (>1,000 Ci/mmol) is added, and incubation continued for 1 h at 37°C. Cells are captured onto 96-well GF/B filter plates and washed twice with PBS before precipitation with 10% ice-cold trichloroacetic acid (TCA) for 1 h at 4°C. Precipitated proteins are washed four times with ice-cold 10% TCA and air-dried for 1 h. UltimaGold scintillation cocktail is added and allowed to mix for 1 h before scintillation counting using a scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Leukemic cells are washed and suspended in phosphate buffered saline (PBS). 100 μL of cell suspension (1×105 cells/mL) is mixed with 100 μL of Tosedostat (CHR-2797) (0.01 to 10 μM) and 200 μM L-alanine 4-methyl-coumaryl-7-amide (ala-MCA) in a 96 well plate in duplicate. The aminopeptidase activity is measured by detecting the fluorescent 7-amino-4-methylcoumarin (MCA) liberated from the cleavage of ala-MCA by cellular aminopeptidases (excitation 355 nm, emission 460 nm)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

A breeding colony of NOD/SCID IL2R gammanull mice are used in this study. The mice are inoculated subcutaneously in the right flank with 2×106 H929 myeloma cells in 50 μL RPMI-1640 and 50 μL MatrigelTM Basement Membrane Matrix Growth Factor Reduced. The mice are assigned into the following four treatment groups (10 animals per group): no treatment, Tosedostat 75 mg/kg, CHR-3996 30 mg/kg, and Tosedostat 75 mg/kg with concomitant CHR-3996 30 mg/kg. Tosedostat is administered daily by intra-peritoneal injection beginning four days after the tumour cells are inoculated. Caliper measurements of the longest perpendicular tumour diameters (length) and width are performed every other day to estimate the tumour volume[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.65%

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Keywords:

TosedostatCHR-2797CHR2797CHR 2797AminopeptidaseInhibitorinhibitorinhibit

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Tosedostat
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