TNG348
Based on 1 Customer Validation
TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) .
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 2839740-79-1
- Formula: C27H23F6N9O
- Molecular Weight:603.52
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
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Drug Repurposing Compound Library
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Oxygen Sensing Compound Library
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Ubiquitination Compound Library
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Orally Active Compound Library
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Transcription Factor-Targeted Library
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Posttranslational Modification Library
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Biological Activity
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JNK1 |
TNG348 (30 nM, 300 nM) exhibits selective cytotoxicity against BRCA1/2 mutant cell lines and shows synergistic effects in combination with PARP inhibitors in BRCA1/2 mutant and HRD+ cell lines[1].
TNG348 inhibits USP1, leading to increased levels of monoubiquitinated PCNA and FANCD2, thereby interfering with the DNA repair process[2].
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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CAS No. 2839740-79-1
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Appearance Solid
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Molecular Weight 603.52
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Formula C27H23F6N9O
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Color White to light yellow
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SMILES
FC(F)(C1=CN(C)C(C2=CC=C(CN3C4=NC(C5=C(C6CC6)N=CN=C5OC)=NC=C4N(CC(F)(F)F)C3=N)C=C2)=N1)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (165.69 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 (4.14 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.
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.
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
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 | 1.6569 mL | 8.2847 mL | 16.5695 mL | 41.4236 mL |
| 5 mM | 0.3314 mL | 1.6569 mL | 3.3139 mL | 8.2847 mL | |
| 10 mM | 0.1657 mL | 0.8285 mL | 1.6569 mL | 4.1424 mL | |
| 15 mM | 0.1105 mL | 0.5523 mL | 1.1046 mL | 2.7616 mL | |
| 20 mM | 0.0828 mL | 0.4142 mL | 0.8285 mL | 2.0712 mL | |
| 25 mM | 0.0663 mL | 0.3314 mL | 0.6628 mL | 1.6569 mL | |
| 30 mM | 0.0552 mL | 0.2762 mL | 0.5523 mL | 1.3808 mL | |
| 40 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0356 mL | |
| 50 mM | 0.0331 mL | 0.1657 mL | 0.3314 mL | 0.8285 mL | |
| 60 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6904 mL | |
| 80 mM | 0.0207 mL | 0.1036 mL | 0.2071 mL | 0.5178 mL | |
| 100 mM | 0.0166 mL | 0.0828 mL | 0.1657 mL | 0.4142 mL |
TNG348 Related Classifications
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