Tosposertib
Based on 1 Customer Validation
Tosposertib (TU2218 free base) is an ALK5/VEGFR2 dual inhibitor (IC50 = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer.
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- Pureza: 99.89%
- No. CAS: 1418305-55-1
- Fòrmula: C17H15N7
- Peso molecular:317.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ALK5 1.2 nM (IC50) |
VEGFR2 4.9 nM (IC50) |
Tosposertib (TU2218) shows a half maximal inhibitory concentration (IC50) of 101 nM in the SMAD2 phosphorylation assay using human whole blood and an IC50 of 52.5 nM in the VEGFR2 phosphorylation assay in human umbilical vein endothelial cells (HUVECs)[1].
Tosposertib (0.5-5 μM, 24 h) can reverse the TGFβ-mediated inhibition of IFNγ expression in CD4+ and CD8+ T cells in human peripheral blood mononuclear cells (PBMCs)[1].
Tosposertib (0.5-5 μM, 72 h) significantly restores TGFβ-induced inhibition of IFNγ secretion in Human PBMCs cells[1].
Tosposertib (0.2-5 μM) upregulates the expression of NKG2D receptor, is inhibited by TGFβ, and restores the killing activity of NK92 cells against K562 cells[1].
Tosposertib (0.5-5 μM, 48 h) can restore the decreased IFNγ level caused by co-culturing Human PBMCs with MCF-7 or HT-1080 cancer cells[1].
Tosposertib (0.5-2.5 μM, 5 days) concentration-dependently restores regulator T cell (Treg)-inhibited effector T cell (Teff) proliferation and reduces Treg activity[1].
Tosposertib upregulates the expression of adhesion-related genes (such as VCAM-1 and ICAM-1) in HUVECs stimulated by TNFα and VEGF, and downregulates cell division-related genes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1418305-55-1
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Appearance Solid
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Peso molecular 317.35
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Fòrmula C17H15N7
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Color White to light yellow
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SMILES
CC1=CC=CC(C(NC2=NCCN23)=C3C4=CN5N=CN=C5C=C4)=N1
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Synonyms
TU2218 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (315.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (7.88 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.88 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.
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.
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kim NH, et al. ALK5/VEGFR2 dual inhibitor Tosposertib alone or in combination with immune checkpoint inhibitors enhances immune-mediated antitumor effects. Cancer Immunol Immunother. 2024 Aug 6;73(10):190. [Content Brief]
[2]. Lee JY, et al., 2-pyridyl substituted imidazoles as alk5 and/or alk4 inhibitors. WO2013009140
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. 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 |
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| DMSO | 1 mM | 3.1511 mL | 15.7555 mL | 31.5109 mL | 78.7774 mL |
| 5 mM | 0.6302 mL | 3.1511 mL | 6.3022 mL | 15.7555 mL | |
| 10 mM | 0.3151 mL | 1.5755 mL | 3.1511 mL | 7.8777 mL | |
| 15 mM | 0.2101 mL | 1.0504 mL | 2.1007 mL | 5.2518 mL | |
| 20 mM | 0.1576 mL | 0.7878 mL | 1.5755 mL | 3.9389 mL | |
| 25 mM | 0.1260 mL | 0.6302 mL | 1.2604 mL | 3.1511 mL | |
| 30 mM | 0.1050 mL | 0.5252 mL | 1.0504 mL | 2.6259 mL | |
| 40 mM | 0.0788 mL | 0.3939 mL | 0.7878 mL | 1.9694 mL | |
| 50 mM | 0.0630 mL | 0.3151 mL | 0.6302 mL | 1.5755 mL | |
| 60 mM | 0.0525 mL | 0.2626 mL | 0.5252 mL | 1.3130 mL | |
| 80 mM | 0.0394 mL | 0.1969 mL | 0.3939 mL | 0.9847 mL | |
| 100 mM | 0.0315 mL | 0.1576 mL | 0.3151 mL | 0.7878 mL |
Tosposertib Related Classifications
HY-172240 Related Classifications
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