RTx-152
Based on 1 Customer Validation
RTx-152 is a potent and selective Polθ-pol allosteric inhibitor with an IC50 of 6.2 nM. RTx-152 binds to the allosteric pocket of the Polθ-pol finger domain, locking it in a closed conformation on the DNA substrate, thereby effectively inhibiting its catalytic cycle. RTx-152 synergizes with Olaparib (HY-10162) in BRCA2-deficient cells and synergizes with PARP inhibitors in homologous recombination-deficient cells. RTx-152 can be used for research on homologous recombination-deficient cancers such as BRCA2 mutations.
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- Pureza : 99.71%
- No. CAS: 3035072-48-8
- Fòrmula: C20H16F7N3O3
- Peso molecular:479.35
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Human pol θ 6.2 nM (IC50) |
In Vitro
RTx-152 (1.25-5 μM; 10-12 days) synergizes with Olaparib to inhibit colony formation in the DLD1 BRCA2-null cell line[1].
RTx-152 (10 μM; 5-40 min) specifically traps Polθ-pol on a DNA/DNA template in a closed conformation through allosteric binding in in vitro biochemical assays and resists endonuclease digestion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3035072-48-8
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Appearance Solid
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Peso molecular 479.35
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Fòrmula C20H16F7N3O3
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Color White to off-white
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SMILES
FC(F)(F)C1=CC(N2CCN(C)C2=O)=C(OC(N(C3=CC=C(F)C=C3)C)=O)C(C(F)(F)F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (104.31 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (5.22 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.
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)
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 (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 (sealed storage, away from moisture and light). 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 | 2.0862 mL | 10.4308 mL | 20.8616 mL | 52.1540 mL |
| 5 mM | 0.4172 mL | 2.0862 mL | 4.1723 mL | 10.4308 mL | |
| 10 mM | 0.2086 mL | 1.0431 mL | 2.0862 mL | 5.2154 mL | |
| 15 mM | 0.1391 mL | 0.6954 mL | 1.3908 mL | 3.4769 mL | |
| 20 mM | 0.1043 mL | 0.5215 mL | 1.0431 mL | 2.6077 mL | |
| 25 mM | 0.0834 mL | 0.4172 mL | 0.8345 mL | 2.0862 mL | |
| 30 mM | 0.0695 mL | 0.3477 mL | 0.6954 mL | 1.7385 mL | |
| 40 mM | 0.0522 mL | 0.2608 mL | 0.5215 mL | 1.3038 mL | |
| 50 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0431 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3477 mL | 0.8692 mL | |
| 80 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6519 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.5215 mL |
RTx-152 Related Classifications
HY-161431 Related Classifications
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Keywords
- RTx-152
- 3035072-48-8
- RTx152
- RTx 152
- DNA/RNA Synthesis
- BRCA2-mutant cancer
- BRCA2-null cells
- PARP inhibitors
- Polθ polymerase-domain inhibitor
- allosteric pocket
- closed Polθ-pol conformation
- closed-to-open transition
- conformational fit
- fingers subdomain
- homologous recombination deficient cells
- Inhibitor
- inhibitor
- inhibit