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- CAS号：
1619903-54-6
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥1176.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥495.0 |
| 规格： | 5mg | 产品价格： | ￥1192.0 |
| 规格： | 10mg | 产品价格： | ￥1856.0 |
| 规格： | 25mg | 产品价格： | ￥3064.0 |
| 规格： | 50mg | 产品价格： | ￥4368.0 |
| 规格： | 100mg | 产品价格： | ￥5944.0 |
| 规格： | 200mg | 产品价格： | ￥7864.0 |
Product Introduction
Bioactivity
| 名称 | LY2857785 |
| 描述 | LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM). |
| 细胞实验 | Solid tumor cells are plated in poly-D-lysine coated and hematologic cell lines are seeded in noncoated 96-well plates overnight before being treated with LY2857785. Solid tumor cells are fixed with Prefer for 20 minutes at room temperature and permeated with 0.1% Triton X-100 in PBS for 15 minutes. Caspase-3 expression is measured by immunofluorescence with anti-activated caspase-3. Terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) activity is measured with In Situ Cell Death Detection Kit. Both assays are analyzed on Acumen Explorer laser-scanning fluorescence microplate cytometer. Hematologic tumor cells are assayed for cell viability with CellTiter-Glo Luminescent Cell Viability Assay. |
| 激酶实验 | CDK7 and CDK9 reaction mixtures contain 10 mM Tris-HCl (pH 7.4), 10 mM HEPES, 5 mM DTT, 10 μM ATP, 0.5 μCi 33p-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 2% DMSO, 0.05 mM CDK7/9ptide, and 2 nM CDK7/Mat1/cyclin H, or 2 nM CDK9/cyclin T1, respectively. CDK8/cyclin C reaction is performed in HEPES 30 mM, DTT 2 mM, MgCl2 5 mM, 0.015% Triton X-100, 5 μM ATP, and 400 nM of RBER-CHKStide containing 20 nM of enzyme. LY2857785 in DMSO is diluted serially 1:3 for dose-response. Reactions are carried out in 96-well polystyrene plates. The reactions are incubated at room temperature for 60 minutes and followed by termination with 10% H3PO4 or 10% trichloroacetic acid (TCA). For the filter binding assay, reactions are transferred to 96-well filter plates and measured by Microbeta scintillation counter. For ADP Transcreener Fluorescent Polarization Assays, reactions are quenched with ADP detection mix, incubated 2 hours at room temperature and then FP is measured at λex=610 nm, λem=670 nm on a Tecan Ultra 384 plate reader. The concentration of ADP product is calculated from millipolarization (μP) using a prepared ADP/ATP dilution series as a standard curve. Kinase profiling are carried out in 96-well polystyrene plates. Briefly, in a final volume of 25 μL the enzyme is incubated with the appropriate buffer, peptide substrate, and the diluted LY2857785. Reactions are initiated by the addition of ATP/[33P] and the ATP mix is incubated at room temperature for 40 minutes. Reactions are quenched with the addition of 5 μL of 3% phosphoric acid, 10 μL of the reaction are spotted onto a filter mat, washed 3 times for 5 minutes in 75 mM phosphoric acid and once in methanol. Once the filters are dry, they are submitted to scintillation counting. |
| 动物实验 | For xenograft models, human cancer cells A375, U87MG, MV-4-11, and HCT116 are implanted into female nude rats or athymic nude female mice. The animals are dosed with saline, Rapamycin, or LY2857785, respectively. MV-4-11 xenografts in nude mice are treated by LY2857785 (4, 8, and 18 mg/kg) i.v. bolus. MV-4-11 xenografts in nude rats are treated with LY2857785 (3, 6, and 9 mg/kg) 4-hour i.v. infusion. An untreated vehicle control group is administered saline i.v. every 3 days. Flow cytometry analysis is conducted using Beckman Coulter's CXP software. Statistical significance of the effect of LY2857785 and/or control compounds is assessed by the Dunnett method, one-way ANOVA. |
| 体外活性 | At the cellular level, LY2857785 inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells (IC50s: 0.089 and 0.042 μM). However, LY2857785 only induces a moderate G2-M DNA content increase, from 35% to 55%, with EC50 0.135 μM. LY2857785 shows potent compound exposure- and time-dependent cell proliferation inhibition in MV-4-11, RPMI8226, and L363 cells. When incubated between 4 to 24 hours, the cell growth inhibition potency reaches a maximal effect at 8 hours for MV-4-11, RPMI8226, and L363 cells (IC50s: 0.04, 0.2, and 0.5 μM). LY2857785-induced cancer cell apoptosis is also time-dependent, reaching maximal potency at 8 hours with IC50 0.5 μM in L363 cells. |
| 体内活性 | In HCT116 xenograft tumor-bearing mice, LY2857785 demonstrates dose-dependent RNAP II CTD P-Ser2 inhibition potently (TED50: 4.4 mg/kg; TEC50: 0.36 μM). LY2857785 also shows the significant duration of CTD P-Ser2 inhibition for 3 to 6 hours at TED70 (8 mg/kg) in HCT116 and MV-4-11 nude mice xenograft models. In the nude rat MV-4-11 xenograft model, LY2857785 similarly shows dose-dependent CTD P-Ser2 inhibition for 8 hours at TED70 (7 mg/kg) and TED90 (10 mg/kg). |
| 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 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.23 mM), Sonication is recommended. DMSO : 10 mg/mL (22.29 mM), Sonication is recommended. |
| 关键字 | LY-2857785 | LY2857785 | LY 2857785 | Inhibitor | inhibit | Cyclin dependent kinase | CDK9 | CDK8 | CDK7 | CDK | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Pancreatic Cancer Compound Library | Kinase Inhibitor Library | Apoptosis Compound Library | Anti-Aging Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 LY2857785【1619903-54-6】
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