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

Tosedostat  (Synonyms: CHR-2797)

製品番号: HY-14807 純度: 99.68%
COA 取扱説明書 Technical Support

Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.

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Tosedostat

Tosedostat 構造式

CAS 番号 : 238750-77-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 181 在庫あり
Solution
10 mM * 1 mL in DMSO USD 181 在庫あり
Solid
1 mg $78 在庫あり
5 mg $165 在庫あり
10 mg $250 在庫あり
25 mg $450 在庫あり
50 mg $675 在庫あり
100 mg $1010 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Tosedostat 関連抗体

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Aminopeptidase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CD13 LTA4H

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines[1].

IC50 & Target

Aminopeptidase[1]
Cellular Effect
Cell Line Type Value Description References
HL-60 EC50
4.7 3
Compound: 3
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28803047]
HL-60 EC50
4.7 3
Compound: 3
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28803047]
MOLT-4 EC50
2.1 3
Compound: 3
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
[PMID: 28803047]
MOLT-4 EC50
2.1 3
Compound: 3
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
[PMID: 28803047]
HL-60 EC50
4.7 3
Compound: 3
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28803047]
Vero CC50
13 3
Compound: 3
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
[PMID: 28803047]
Vero CC50
13 3
Compound: 3
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
[PMID: 28803047]
MOLT-4 EC50
2.1 3
Compound: 3
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
[PMID: 28803047]
Vero CC50
12.73 3
Compound: 4
Cytotoxicity against African green monkey Vero cells by MTT assay
Cytotoxicity against African green monkey Vero cells by MTT assay
[PMID: 38917665]
Vero CC50
13 3
Compound: 3
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
[PMID: 28803047]
体外実験

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].

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

Tosedostat 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

406.47

分子式

C21H30N2O6
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC1CCCC1)[C@@H](NC([C@@H]([C@H](O)C(NO)=O)CC(C)C)=O)C2=CC=CC=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (246.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.68%

COA (249 KB) HNMR (234 KB) LCMS (85 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4602 mL 12.3010 mL 24.6021 mL 61.5052 mL
5 mM 0.4920 mL 2.4602 mL 4.9204 mL 12.3010 mL
10 mM 0.2460 mL 1.2301 mL 2.4602 mL 6.1505 mL
15 mM 0.1640 mL 0.8201 mL 1.6401 mL 4.1003 mL
20 mM 0.1230 mL 0.6151 mL 1.2301 mL 3.0753 mL
25 mM 0.0984 mL 0.4920 mL 0.9841 mL 2.4602 mL
30 mM 0.0820 mL 0.4100 mL 0.8201 mL 2.0502 mL
40 mM 0.0615 mL 0.3075 mL 0.6151 mL 1.5376 mL
50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2301 mL
60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0251 mL
80 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7688 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6151 mL
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Tosedostat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tosedostat238750-77-1CHR-2797CHR2797CHR 2797AminopeptidaseInhibitorinhibitorinhibit

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