Tyroserleutide hydrochloride
Based on 1 Customer Validation
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis.
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- Pureté: 99.92%
- CAS No.: 852982-42-4
- Formule: C18H28ClN3O6
- Masse moléculaire:417.88
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Stockage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
In Vitro
Tyroserleutide (YSL) exhibits immuno-modulating effects, such as enhancing concanavalin (ConA) induced proliferation of mouse spleen lymphocytes, phagocytosis of mouse peritoneal macrophages, and the activity of natural killer (NK) cells[1].
Tyroserleutide (YSL), an immunologically therapeutic tripeptide, can promote hepatocarcinoma cell (H22) apoptosis through downregulating Bcl-2 and cyclin D1 expression[2].
Tyroserleutide is an ideal choice for inducing apoptosis of liver tumor cells[2].
Tyroserleutide inhibits tumor growth and does not cause severe toxicities in the major organs. Tyroserleutide can inhibit tumor cell migration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Kun-Ming mice (18-22 g, 6 week old) with H22 tumor model[1]
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Dosage:10, 20, 40, and 80 μg/kg
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Administration:Injection (i.p.) one time every day until mice were dead.
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Result:Survival times are 25.53±14.14, 25.82±14.29, 30.47±17.89, 35.06±20.90 days for 10, 20, 40, and 80 μg/kg, respectively.
Chemical Information
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CAS No. 852982-42-4
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Appearance Solid
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Masse moléculaire 417.88
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Formule C18H28ClN3O6
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Color White to off-white
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (598.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (4.79 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Fu Z, et al. Effects of Tyroserleutide on phosphatidylinositol 3'-kinase/AKT pathway in human hepatocellular carcinoma cell. J Drug Target. 2014 Feb;22(2):146-55. [Content Brief]
[2]. Wang C, et al. Studies on the large scale synthesis and anti-tumor activity of YSL. Prep Biochem Biotechnol. 2003 Aug;33(3):189-95. [Content Brief]
[3]. Liang P, et al. pH-Triggered Conformational Change of Antp-Based Drug Delivery Platform for Tumor Treatment with Combined Photothermal Therapy and Chemotherapy. Adv Healthc Mater. 2019 Aug;8(15):e1900306. [Content Brief]
[4]. Che X, Lu R, Fu Z, et al. Therapeutic effects of tyroserleutide on lung metastasis of human hepatocellular carcinoma SK-HEP-1 and its mechanism affecting ICAM-1 and MMP-2 and -9. Drug Des Devel Ther. 2018;12:3357-3368. [Content Brief]
[5]. Yao Z, Qiu S, Wang L, et al. Tripeptide tyroserleutide enhances the antitumor effects of macrophages and stimulates macrophage secretion of IL-1beta, TNF-alpha, and NO in vitro. Cancer Immunol Immunother. 2006;55(1):56-60. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3930 mL | 11.9652 mL | 23.9303 mL | 59.8258 mL |
| DMSO | 5 mM | 0.4786 mL | 2.3930 mL | 4.7861 mL | 11.9652 mL |
| 10 mM | 0.2393 mL | 1.1965 mL | 2.3930 mL | 5.9826 mL | |
| 15 mM | 0.1595 mL | 0.7977 mL | 1.5954 mL | 3.9884 mL | |
| 20 mM | 0.1197 mL | 0.5983 mL | 1.1965 mL | 2.9913 mL | |
| 25 mM | 0.0957 mL | 0.4786 mL | 0.9572 mL | 2.3930 mL | |
| 30 mM | 0.0798 mL | 0.3988 mL | 0.7977 mL | 1.9942 mL | |
| 40 mM | 0.0598 mL | 0.2991 mL | 0.5983 mL | 1.4956 mL | |
| 50 mM | 0.0479 mL | 0.2393 mL | 0.4786 mL | 1.1965 mL | |
| 60 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9971 mL | |
| 80 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL | |
| 100 mM | 0.0239 mL | 0.1197 mL | 0.2393 mL | 0.5983 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tyroserleutide hydrochloride Related Classifications
HY-106263B Related Classifications
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