YU238259
目录号 : GC19390
An inhibitor of homology-dependent DNA repair
Cas No.:1943733-16-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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 experiment: | 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. | |
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
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 uM. YU238259 (0-5 uM) 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 uM) 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].
YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice[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.
| Cas No. | 1943733-16-1 | SDF | |
| Canonical SMILES | COC1=CC=C(S(NCC2=CC=C(C(NCCC3=CC=C(Cl)C=N3)=O)C=C2)(=O)=O)C=C1 | ||
| 分子式 | C22H22ClN3O4S | 分子量 | 459.95 |
| 溶解度 | DMSO : ≥ 300 mg/mL (652.24 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1741 mL | 10.8707 mL | 21.7415 mL |
| 5 mM | 0.4348 mL | 2.1741 mL | 4.3483 mL |
| 10 mM | 0.2174 mL | 1.0871 mL | 2.1741 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。