TMX-3013
Based on 1 Customer Validation
TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).
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- Pureza: 98.02%
- No. CAS: 2488761-18-6
- Fòrmula: C17H14BrFN6O3S
- Peso molecular:481.30
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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
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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HY-L034
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Anti-Blood Cancer Compound Library
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Target Protein Ligand Library
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Cancer Stem Cells Compound Library
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
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Anti-Ovarian Cancer Compound Library
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Actividad biológica
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CDK1 0.9 nM (IC50) |
CDK2 <0.5 nM (IC50) |
CDK4 24.5 nM (IC50) |
CDK5 0.5 nM (IC50) |
CDK6 15.6 nM (IC50) |
TMX-6PEG-CA, a TMX3013-based covalent RIPTAC, selectively inhibits the viability of HaloTag-FKBP-expressing 293_HFL cells with a GI50 of 0.050 μM[1].
TMX-6PEG-FKBP, a TMX3013-based non-covalent RIPTAC, selectively inhibits the viability of HaloTag-FKBP-expressing 293_HFL cells with a GI50 of 0.011 μM[1].
TMX-3013 is a non-covalent picomolar CDK2 inhibitor that functions as the CDK2 homing ligand for the generation of NASA-based acylation probes[2].
TMX-3013 potently inhibits CDK2/cyclin A (<0.5 nM IC50), CDK1/cyclin B (0.9 nM IC50), and CDK5/p25 (0.5 nM IC50), with reduced potency against CDK4/cyclin D1 (24.5 nM IC50) and CDK6/cyclin D1 (15.6 nM IC50) in biochemical assays[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2488761-18-6
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Appearance Solid
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Peso molecular 481.30
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Fòrmula C17H14BrFN6O3S
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Color White to light yellow
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SMILES
NC(C1=C(C=CC=C1NC2=NC(NC3=CC=C(C=C3)S(N)(=O)=O)=NC=C2Br)F)=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
DMSO : 100 mg/mL (207.77 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.
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 (277 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]. Raina K, et al. Regulated induced proximity targeting chimeras-RIPTACs-A heterobifunctional small molecule strategy for cancer selective therapies. Cell Chem Biol. 2024;31(8):1490-1502.e42. [Content Brief]
[2]. Teng M, et al. Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 2021 Jul 21;12(8):1302-1307. [Content Brief]
[3]. Teng M, et al. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020;59(33):13865-13870. [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. 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 | 2.0777 mL | 10.3885 mL | 20.7771 mL | 51.9427 mL |
| 5 mM | 0.4155 mL | 2.0777 mL | 4.1554 mL | 10.3885 mL | |
| 10 mM | 0.2078 mL | 1.0389 mL | 2.0777 mL | 5.1943 mL | |
| 15 mM | 0.1385 mL | 0.6926 mL | 1.3851 mL | 3.4628 mL | |
| 20 mM | 0.1039 mL | 0.5194 mL | 1.0389 mL | 2.5971 mL | |
| 25 mM | 0.0831 mL | 0.4155 mL | 0.8311 mL | 2.0777 mL | |
| 30 mM | 0.0693 mL | 0.3463 mL | 0.6926 mL | 1.7314 mL | |
| 40 mM | 0.0519 mL | 0.2597 mL | 0.5194 mL | 1.2986 mL | |
| 50 mM | 0.0416 mL | 0.2078 mL | 0.4155 mL | 1.0389 mL | |
| 60 mM | 0.0346 mL | 0.1731 mL | 0.3463 mL | 0.8657 mL | |
| 80 mM | 0.0260 mL | 0.1299 mL | 0.2597 mL | 0.6493 mL | |
| 100 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL | 0.5194 mL |
TMX-3013 Related Classifications
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