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YU238259

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Chemical Structure| 1943733-16-1 同义名 : -
CAS号 : 1943733-16-1
货号 : A699629
分子式 : C22H22ClN3O4S
纯度 : 99%+
分子量 : 459.946
MDL号 : MFCD30532769
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(228.29 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 YU238259 is a novel DNA double-strand break repair inhibitor exhibiting potent synthetic lethality in the setting of DNA damage response and DNA repair defects. YU238259 specifically inhibits homology-dependent DNA repair, but not non-homologous end-joining, in cell-based GFP reporter assays at concentration of 5μM. Treatment with YU238259 was not only synergistic with ionizing radiation, etoposide, and PARP inhibition, but this synergism was heightened by BRCA2 deficiency. Also it significantly delayed growth of BRCA2-deficient human tumor xenografts in nude mice through administration at dose of 3mg/kg, i.p., 3 days per week for 12 doses, even in the absence of concomitant DNA-damaging therapy.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL

参考文献

[1]Stachelek GC, Peterson-Roth E, 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.