Glucose-conjugated MGMT inhibitor
(Synonyms: 8-[2-氨基-6-[(4-溴-2-噻吩基)甲氧基]-9H-嘌呤-9-基]辛基BETA-D-吡喃葡萄糖苷,Glucose-conjugated MGMT inhibitor) 目录号 : GC36153
Glucose-conjugated MGMT inhibitor 是一种有效的 O6-甲基鸟嘌呤-DNA甲基转移酶 (MGMT) 抑制剂，体外（细胞提取物）的 IC50 为 32 nM，在 HeLa S3 细胞中的 IC50 为 10 nM。
Cas No.:382607-78-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | For the assays, 100 mg cell extract protein are used. In each assay, a negative and a positive sample, HeLa MR (MGMT-deficient) and HeLa S3 cell extract, respectively, are included. Incubation occurs in buffer contain-ing 700 mM HEPES-KOH (pH 7.8), 10 mM dithiothreitol and 50 mM EDTA for 90 min, which is the optimal time span for the reaction to be completed. Data are expressed as femtomoles of radioactivity trans-ferred from 3H-methylnitrosourea-labeled DNA to protein per milligram of protein within O6BTG-octylglucoside[1]. |
References: [1]. Jost Reinhard, et al. Inactivation of O6-methylguanine-DNA methyltransferase by glucose-conjugated inhibitors. Int.J.Cancer. (2001) 93,373-379. | |
Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells. MGMT|32 nM (IC50)
Glucose-conjugated MGMT inhibitor (O6BTG-octylglucoside) is a potent and non-toxic MGMT inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells[1].
[1]. Jost Reinhard, et al. Inactivation of O6-methylguanine-DNA methyltransferase by glucose-conjugated inhibitors. Int.J.Cancer. (2001) 93,373-379.
| Cas No. | 382607-78-5 | SDF | |
| 别名 | 8-[2-氨基-6-[(4-溴-2-噻吩基)甲氧基]-9H-嘌呤-9-基]辛基BETA-D-吡喃葡萄糖苷,Glucose-conjugated MGMT inhibitor | ||
| Canonical SMILES | [H][C@]1([C@]([H])(O[C@@](OCCCCCCCCN2C3=C(N=C2)C(OCC4=CC(Br)=CS4)=NC(N)=N3)([C@](O)([C@]1(O)[H])[H])[H])CO)O | ||
| 分子式 | C24H34BrN5O7S | 分子量 | 616.53 |
| 溶解度 | DMSO: 100 mg/mL (162.20 mM) | 储存条件 | Store at -20°C |
| 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 | 1.622 mL | 8.1099 mL | 16.2198 mL |
| 5 mM | 0.3244 mL | 1.622 mL | 3.244 mL |
| 10 mM | 0.1622 mL | 0.811 mL | 1.622 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。