SGI-1776
作者：齐岳
发布时间：2023-08-23
09:36:15
点击数：
产品名称：SGI-1776
产品描述：
| 产品描述 | SGI-1776 has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias. |
| 靶点活性 | FLT3:44 nM, Pim1:7 nM, Pim3:69 nM, Pim2:363 nM |
| 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。 |
| 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. |
| 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) |
| 别名 | SGI-1776 free base, Pim-Kinase Inhibitor IX |
| 分子量 | 405.425 |
| 分子式 | C20H22F3N5O |
| CAS No. | 1025065-69-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 75 mg/mL (185 mM)
Ethanol: 75 mg/mL (185 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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