| 名称 | SGI-1776 |
| 描述 | SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias. |
| 细胞实验 | Cells are cultured in IMDM (ATCC) supplemented with 10% FBS and grown in a 37oC incubator with 5% CO2. Cells are routinely tested for Mycoplasma infection using a commercially available kit. Cells are treated with DMSO or various concentrations of SGI-1776 for 24 hours. Cells (1×106) are washed, then resuspended in 100 μL of annexin binding buffer, mixed with 5 μL of FITC solution and 5 μL of propidium iodide (PI; 50 μg/mL) solution. For each sample, 1×104 cells are measured using a Becton Dickinson FACSCalibur flow cytometer. (Only for Reference) |
| 激酶实验 | Kinase Assays: Kinase inhibition is measured by the use of radiometric assays performed by KinaseProfiler service. Assays contain a peptide substrate, known purified recombinant human kinases, gamma-labeled ATP, magnesium ion, and a fixed concentration (1 μM) of SGI-1776. In a final reaction volume of 25 μL, 5 to 10 mU of Pim1/2/3 is incubated with 8 mM of MOPS, pH 7.0; 0.2 mM ethylene diamine tetraacetic acid; 100 μM KKRNRTLTV;10 mM MgAcetate; and [γ-32P-ATP] . The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 5 μL of a 3% phosphoric acid solution. Then, 10 μL of the reaction is spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mM phosphoric acid and once in methanol before it is dried and measured via a scintillation counter. |
| 体外活性 | SGI-1776已经显示出针对白血病和实体瘤细胞系模型的临床前活性,其IC50值为0.005-11.68 mM.在31个实体瘤异种移植物中的9个和8个可评估的ALL异种移植物中的1个中,SGI-1776诱导体内EFS分布的显著差异.SGI-1776对携带MV-4-11肿瘤的小鼠模型有效. |
| 体内活性 | SGI-1776诱导CLL细胞剂量依赖性凋亡。SGI-1776诱导CLL细胞凋亡,作用机理涉及Mcl-1减少。SGI-1776在体外,具有毒性,且平均相对IC50值为3.1 mM。SGI-1776除了Pim, 也有效靶向作用于FLT3 ,IC50 = 44 nM。SGI-1776诱导AML细胞凋亡,这种作用存在浓度依赖性。SGI-1776 作用于AML原代细胞,具有毒性,且导致Mcl-1蛋白降低。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 55.55 mg/ml (137.03 mM), Sonication is recommended.
Ethanol : 75 mg/mL (184.99 mM), Sonication is recommended.
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| 关键字 | SGI-1776 | SGI1776 | SGI 1776 | Pim3 | Pim2 | Pim1 | Pim | FLT3 | Autophagy | Apoptosis |
| 相关产品 | Naringin | Guanidine hydrochloride | L-Glutamic acid | Gefitinib | Cysteamine hydrochloride | Alginic acid | Dextran sulfate sodium salt (MW 5000) | Hydroxychloroquine | Stavudine | L-Ascorbic acid sodium salt | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 临床失败化合物库 | 抗衰老化合物库 | 膜蛋白靶向化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库 |