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LY2857785

产品编号 TQ0060 CAS 1619903-54-6

LY2857785 是 I 型可逆的 ATP 竞争性 CDK9、CDK8和 CDK7抑制剂，IC50分别为 11 nM、16 nM 和 246 nM。

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LY2857785, CAS 1619903-54-6

规格	价格/CNY	货期
1 mg	￥ 619	现货
2 mg	￥ 892	现货
5 mg	￥ 1,490	现货
10 mg	￥ 2,320	现货
25 mg	￥ 3,830	现货
50 mg	￥ 5,650	现货
100 mg	￥ 7,660	现货
1 mL * 10 mM (in DMSO)	￥ 1,690	现货

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纯度: 96.00%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM).
靶点活性	CDK7:246 nM, CDK9:11 nM, CDK8:16 nM
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).
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.
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.
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.

分子量	448.6
分子式	C26H36N6O
CAS No.	1619903-54-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mg/mL (22.29 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2292 mL	11.1458 mL	22.2916 mL	55.7289 mL
	5 mM	0.4458 mL	2.2292 mL	4.4583 mL	11.1458 mL
	10 mM	0.2229 mL	1.1146 mL	2.2292 mL	5.5729 mL
	20 mM	0.1115 mL	0.5573 mL	1.1146 mL	2.7864 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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容积

分子量

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容积 (起始)

浓度 (终)

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参考文献

1. Yin T, et al. A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models. Mol Cancer Ther. 2014 Jun;13(6):1442-56. Mol Cancer Ther. 2014 Jun;13(6):1442-56.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LY2857785 1619903-54-6 Apoptosis Cell Cycle/Checkpoint CDK Cyclin dependent kinase Inhibitor inhibit LY 2857785 LY-2857785 inhibitor

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LY2857785

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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