YU238259
Based on 1 Customer Validation
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
For research use only. We do not sell to patients.
- Purity: 98.56%
- CAS No.: 1943733-16-1
- Formula: C22H22ClN3O4S
- Molecular Weight:459.95
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
HDR[1]
YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD50 of 8.5 μM. YU238259 (0-5 μM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 μM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss[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.
Chemical Information
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CAS No. 1943733-16-1
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Appearance Solid
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Molecular Weight 459.95
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Formula C22H22ClN3O4S
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Color White to off-white
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SMILES
COC1=CC=C(S(NCC2=CC=C(C(NCCC3=CC=C(Cl)C=N3)=O)C=C2)(=O)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 110 mg/mL (239.16 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 (protect from 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 (protect from 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)
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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.
Protocol
U2OS reporter cell lines (DR-GFP or EJ5-GFP) are pretreated in triplicate with varying concentrations of YU238259 for 24 h, after which 4 μg of SCE-I plasmid is transfected into 1 × 106 cells/replicate using an Amaxa Nucleofector. Transfected cells are reseeded on 6-well plates and cultured with YU238259 for an additional 72 h. The percentage of GFP-positive cells is quantified by flow cytometry. Data analysis is performed using FlowJo software. Error bars represent the standard deviation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
069(nu)/070(nu/+) athymic nude mice, at 4-5 weeks age, are injected subcutaneously with 3 × 106 DLD-1 or DLD-1 BRCA2-KO cells suspended in 100 μL PBS. Tumor take rate is >80%. When tumors reach 100 mm3 geometric mean volume, the mice are injected with 3 mg/kg YU238259 or its 3:1 DMSO:PBS vehicle, or 5 mg/kg YU128440 or its 1:19 DMSO:PBS vehicle (IP, 100 μL total in each case). Treatment is repeated 3×/week (Mon/Wed/Fri) for a total of 12 doses of YU238259 and 4 doses of YU128440. Tumor growth is assessed by external caliper. Mice are euthanized when individual tumor volumes exceed 1000 mm3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 (protect from 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 | 2.1741 mL | 10.8707 mL | 21.7415 mL | 54.3537 mL |
| 5 mM | 0.4348 mL | 2.1741 mL | 4.3483 mL | 10.8707 mL | |
| 10 mM | 0.2174 mL | 1.0871 mL | 2.1741 mL | 5.4354 mL | |
| 15 mM | 0.1449 mL | 0.7247 mL | 1.4494 mL | 3.6236 mL | |
| 20 mM | 0.1087 mL | 0.5435 mL | 1.0871 mL | 2.7177 mL | |
| 25 mM | 0.0870 mL | 0.4348 mL | 0.8697 mL | 2.1741 mL | |
| 30 mM | 0.0725 mL | 0.3624 mL | 0.7247 mL | 1.8118 mL | |
| 40 mM | 0.0544 mL | 0.2718 mL | 0.5435 mL | 1.3588 mL | |
| 50 mM | 0.0435 mL | 0.2174 mL | 0.4348 mL | 1.0871 mL | |
| 60 mM | 0.0362 mL | 0.1812 mL | 0.3624 mL | 0.9059 mL | |
| 80 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6794 mL | |
| 100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5435 mL |