GK921
目录号 : GC36142
An inhibitor of TG2
Cas No.:1025015-40-0
Sample solution is provided at 25 µL, 10mM.
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GK921 is an inhibitor of transglutaminase 2 (TG2; IC50 = 7.71 ?M).1 It is cytotoxic against a panel of eight renal cell carcinoma (RCC) cell lines (mean GI50 = 0.905 ?M). GK921 (8 mg/kg) suppresses tumor growth in ACHN and Caki-1 RCC mouse xenograft models.
1.Ku, B.M., Kim, S.-J., Kim, N., et al.Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft modelsJ. Cancer Res. Clin. Oncol.140(5)757-767(2014)
Kinase experiment: | TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2 |
Cell experiment: | Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1]. |
Animal experiment: | Mice: GK921 is dissolved in DMSO. Vehicle alone and GK921 (8 mg/kg) are administered orally once per day, 5 days/week, for 64 days. The size of the primary tumors is measured every 2-3 days using calipers. Tumor volume is calculated[1]. |
References: [1]. Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014 May;140(5):757-67. | |
| Cas No. | 1025015-40-0 | SDF | |
| Canonical SMILES | C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2 | ||
| 分子式 | C21H20N4O | 分子量 | 344.41 |
| 溶解度 | DMSO: ≥ 30 mg/mL (87.11 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 | 2.9035 mL | 14.5176 mL | 29.0352 mL |
| 5 mM | 0.5807 mL | 2.9035 mL | 5.807 mL |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9035 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet