AZD1208
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:07:20
點(diǎn)擊數(shù)：
產(chǎn)品名稱：AZD1208
產(chǎn)品描述：
| 產(chǎn)品描述 | AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases. |
| 靶點(diǎn)活性 | Pim1:0.4 nM, Pim3:1.9 nM, Pim2:5 nM |
| 體外活性 | AZD1208劑量依賴性抑制MOLM-16和KG-1a異種移植在體內(nèi)的生長(zhǎng). |
| 體內(nèi)活性 | AZD1208在培養(yǎng)的MOLM-16細(xì)胞中引起細(xì)胞周期停滯和細(xì)胞凋亡。 這伴隨著BAD,4EBP1和p70S6K磷酸化的劑量依賴性降低。 另外,AZD1208導(dǎo)致有效抑制來自骨髓抽吸物的原代AML細(xì)胞的集落生長(zhǎng)并下調(diào)Pim靶標(biāo)的磷酸化。 |
| 激酶實(shí)驗(yàn) | The activity of purified human PIM-1, PIM-2 and PIM-3 enzymes on substrate FL-Ahx-Bad (FITC-(AHX)RSRHSSYPAGT-COOH) is determined using a mobility shift assay on a Caliper LC3000 reader. The PIM-1 assay is performed in a 12 mL reaction containing 50 mM HEPES (pH 7.5), 1 mM DTT, 0.01% Tween 20, 50 mg/mL BSA, 10 mM MgCl2, 1.5 mM FL-Ahx-Bad peptide, 100 mM ATP, 2.5 nM PIM-1 and various amount of inhibitor. The reaction is quenched after 90 minute incubation at 25?C with?5 mL of stop mix consisting of 100 mM HEPES, 121 mM EDTA, 0.8% Coating Reagent 3 and 0.01% Tween 20. The ATP and enzyme concentrations for the PIM-2 assay are 5 mM and 2.5 nM, respectively, while 50 mM of ATP and 0.33 nM of enzyme is used for PIM-3 assays. For high [ATP] screenings, 5 mM ATP is used with 0.67 nM enzyme for both PIM-1 and PIM-2 or 0.11 nM PIM-3. Fluorescence of phosphorylated and unphosphorylated substrate is detected and a ratiometric value is calculated to determine percent turnover. IC50 values are determined from dose-response data using IDBS ActivityBase software. |
| 細(xì)胞實(shí)驗(yàn) | AZD1208 is dissolved in DMSO. MOLM-16 cells, purchased from DSMZ and cultured in RPMI containing 10% fetal bovine serum (FBS) and 1% L-glutamine, are plated at 20,000 cells per well in 96 well plates overnight. Cells are treated for 72 hours with compound or control vehicle (dimethyl sulfoxide) and cell viability is measured after the addition of Cell Titer-Blue for 4 hours at 37?C and reading of fluorescence on a Tecan Infinite? 200. The GI50 is determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment. |
| 分子量 | 379.48 |
| 分子式 | C21H21N3O2S |
| CAS No. | 1204144-28-4 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 7.6 mg/mL (20 mM)),with gentle warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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