DC Chemicals' products qualify for U.S. tariff exemptions. We guarantee no price increases due to customs duties and maintain stable supply, continuing to deliver reliable research solutions to our American clients.
| Cas No.: | 1943733-16-1 |
| Synonyms: | YU-238259，YU 238259 |
| SMILES: | C1=CC(OC)=CC=C1S(=O)(=O)NCC1=CC=C(C(=O)NCCC2=CC=C(Cl)C=N2)C=C1 |
| Formula: | C22H22ClN3O4S |
| M.Wt: | 459.95 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research. |
| Target: | HDR[1] |
| In Vivo: | YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice[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]. |
| 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 Administration: | 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: | [1]. Stachelek GC, et al. YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors. Mol Cancer Res. 2015 Oct;13(10):1389-97. |
MSDS
COA
| LOT NO. | DOWNLOAD |
|
|
|
| 2018-0101 |
|
| 2018-0101 |
|