SGI-1776
作者：齊岳
發(fā)布時間：2023-08-23
09:36:15
點擊數(shù)：
產(chǎn)品名稱：SGI-1776
產(chǎn)品描述：
| 產(chǎn)品描述 | SGI-1776 has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias. |
| 靶點活性 | FLT3:44 nM, Pim1:7 nM, Pim3:69 nM, Pim2:363 nM |
| 體外活性 | SGI-1776已經(jīng)顯示出針對白血病和實體瘤細胞系模型的臨床前活性,其IC50值為0.005-11.68 mM.在31個實體瘤異種移植物中的9個和8個可評估的ALL異種移植物中的1個中,SGI-1776誘導(dǎo)體內(nèi)EFS分布的顯著差異.SGI-1776對攜帶MV-4-11的小鼠模型有效. |
| 體內(nèi)活性 | SGI-1776誘導(dǎo)CLL細胞劑量依賴性凋亡。SGI-1776誘導(dǎo)CLL細胞凋亡,作用機理涉及Mcl-1減少。SGI-1776在體外,具有毒性,且平均相對IC50值為3.1 mM。SGI-1776除了Pim, 也有效靶向作用于FLT3 ,IC50 = 44 nM。SGI-1776誘導(dǎo)AML細胞凋亡,這種作用存在濃度依賴性。SGI-1776 作用于AML原代細胞,具有毒性,且導(dǎo)致Mcl-1蛋白降低。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | SGI-1776 free base, Pim-Kinase Inhibitor IX |
| 分子量 | 405.425 |
| 分子式 | C20H22F3N5O |
| CAS No. | 1025065-69-3 |
存儲
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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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