产品描述: | YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays. |
靶点: |
DNA-PK;DNA-PK; Others |
体内研究: |
Growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even without concomitant DNA-damaging therapy. |
细胞实验: |
U2OS cells were pretreated with 25 μM YU238259 or DMSO vehicle for 1 h and cells were then irradiated with 10 Gy IR. Cells were fixed at 8 h post-IR, stained with antibodies and Hoechst dye, and imaged. Foci were quantified using the InCell Analyzer algorithm developed by YCMD. Cells were scored as foci-positive if they contained ≥15 foci (BRCA1, pDNA-PK) or ≥20 foci (53BP1). |
动物实验: |
Animal Models: 069(nu)/070(nu/+) athymic nude mice. Formulation: 3:1 DMSO:PBS. Dosages: 3 mg/kg . Administration: i.p |
参考文献: |
1. Stachelek GC,etal.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. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.174 ml |
10.871 ml |
21.741 ml |
5 mM |
0.435 ml |
2.174 ml |
4.348 ml |
10 mM |
0.217 ml |
1.087 ml |
2.174 ml |
50 mM |
0.043 ml |
0.217 ml |
0.435 ml |
|
注意: |
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