YU238259
Modify Date: 2025-09-18 17:48:18
YU238259 structure
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Common Name | YU238259 | ||
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| CAS Number | 1943733-16-1 | Molecular Weight | 459.9525 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H22ClN3O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of YU238259YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research. |
| Name | YU238259 |
|---|---|
| Synonym | More Synonyms |
| Description | YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research. |
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| Related Catalog | |
| Target |
HDR[1] |
| In Vitro | 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]. |
| In Vivo | YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice[1]. |
| Cell Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C22H22ClN3O4S |
|---|---|
| Molecular Weight | 459.9525 |
| InChIKey | BIHURSOREGLQBB-UHFFFAOYSA-N |
| SMILES | COc1ccc(S(=O)(=O)NCc2ccc(C(=O)NCCc3ccc(Cl)cn3)cc2)cc1 |
| Storage condition | -20℃ |
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| MFCD30532769 |