TMX-4113
Based on 1 Customer Validation
TMX-4113 is a FPFT-2216 (HY-145319) (Molecular glue) analog and degrader of PDE6D and CK1α. TMX-4113 does not inhibit the growth of KRASG12C-dependent cancer cells. TMX-4113 can be used in the research of multiple myeloma, pancreatic ductal adenocarcinoma, non-small cell lung cancer and gastric adenocarcinoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.08%
- No. CAS: 2766385-92-4
- Fòrmula: C12H12N4O2S2
- Peso molecular:308.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PDE6D |
CK1α |
In Vitro
TMX-4113 (40 nM-1 µM; 4 h) selectively degrades PDE6D and CK1α in MM.1S cells, without degrading IKZF1 or IKZF3 in MOLT4, Jurkat or MM.1S cells[1].
TMX-4113 (3 days) exerts no inhibitory effect on the proliferation of MIA PaCa-2 cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4, Jurkat, MM.1S
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Concentration:1 µM; 200 nM; 40 nM
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Incubation Time:4 h
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Result:Potently degraded PDE6D with DC50 values lower than those of TMX-4100 across MOLT4, Jurkat, and MM.1S cells.
Did not degrade IKZF1 or IKZF3 in any of the three cell lines.
Degraded over 50% of CK1α at a dose of 40 nM in MM.1S cells.
Chemical Information
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No. CAS 2766385-92-4
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Appearance Solid
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Peso molecular 308.38
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Fòrmula C12H12N4O2S2
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Color Off-white to light yellow
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SMILES
O=C(C(N1N=NC(C2=CSC=C2SC)=C1)CC3)NC3=O
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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
In Vitro:
DMSO : 100 mg/mL (324.28 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)
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: ≥ 2.5 mg/mL (8.11 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 (8.11 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:
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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 (288 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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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2428 mL | 16.2138 mL | 32.4275 mL | 81.0688 mL |
| 5 mM | 0.6486 mL | 3.2428 mL | 6.4855 mL | 16.2138 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2428 mL | 8.1069 mL | |
| 15 mM | 0.2162 mL | 1.0809 mL | 2.1618 mL | 5.4046 mL | |
| 20 mM | 0.1621 mL | 0.8107 mL | 1.6214 mL | 4.0534 mL | |
| 25 mM | 0.1297 mL | 0.6486 mL | 1.2971 mL | 3.2428 mL | |
| 30 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7023 mL | |
| 40 mM | 0.0811 mL | 0.4053 mL | 0.8107 mL | 2.0267 mL | |
| 50 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6214 mL | |
| 60 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3511 mL | |
| 80 mM | 0.0405 mL | 0.2027 mL | 0.4053 mL | 1.0134 mL | |
| 100 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8107 mL |
TMX-4113 Related Classifications
HY-145320 Related Classifications
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Keywords
- TMX-4113
- 2766385-92-4
- TMX4113
- TMX 4113
- Phosphodiesterase (PDE)
- Casein Kinase
- Molecular Glues
- Drug Derivative
- gastric adenocarcinoma
- CRL4CRBN E3 ubiquitin ligase
- non-small cell lung cancer
- pancreatic ductal adenocarcinoma
- PDE6D
- multiple myeloma
- MM.1S cells
- CK1α
- proteasome pathway
- KRASG12C-dependent cancer cells
- Inhibitor
- inhibitor
- inhibit