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Dinaciclib

产品编号 T1912 CAS 779353-01-4

别名: SCH 727965, PS-095760

Dinaciclib (SCH 727965) 是一种 CDK 抑制剂，抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50分=3/1/1/4 nM)，具有选择性。Dinaciclib 具有潜在的抗肿瘤活性，可以抑制胸甘 (dThd) DNA 的整合。

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Dinaciclib, CAS 779353-01-4

规格	价格/CNY	货期
2 mg	￥ 498	现货
5 mg	￥ 797	现货
10 mg	￥ 1,240	现货
50 mg	￥ 3,781	现货
1 mL * 10 mM (in DMSO)	￥ 877	现货

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选择批次

纯度: 99.75%

纯度: 99.73%

纯度: 99.65%

纯度: 99.22%

纯度: 99.18%

纯度: 98.99%

纯度: 98.21%

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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	Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 score = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.
靶点活性	CDK1:3 nM (cell free), CDK9:4 nM (cell free), CDK5:1 nM (cell free), CDK2:1 nM (cell free)
体外活性	方法：人胰腺癌细胞系 MIAPaCa-2 和 Pa20C 用 Dinaciclib (0.5-128 nM) 处理 72 h，使用 MTT Assay 检测细胞活力。结果：Dinaciclib 以剂量依赖的方式抑制 MIAPaCa-2 和 Pa20C 细胞的生长，GI50 分别约为 10 和 20 nM。[1] 方法：人骨肉瘤细胞系 SaOs-2 和 U2OS 用 Dinaciclib (5-62 nmol/L) 处理 4-24 h，使用 Western Blot 检测靶点蛋白表达水平。结果：Dinaciclib 消除骨肉瘤细胞中 CDK 底物的磷酸化。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Dinaciclib (40 mg/kg，20% (w/v) HPBCD) 腹腔注射给携带人胰腺癌肿瘤 JH033 或 Panc286 的 CD1 nu/nu athymic 小鼠，每周两次，持续四周。结果：Dinaciclib 抑制一组低渗透癌症异种移植物的体内生长。[1] 方法：为检测体内抗肿瘤活性，将 Dinaciclib (8-48 mg/kg) 腹腔注射给携带卵巢癌肿瘤 A2780 的 BALB/c 小鼠，每天一次，持续十天。结果：Dinaciclib 在体内具有剂量依赖性的抗肿瘤活性，并且在低于 MTD 的剂量水平下几乎完全抑制肿瘤生长。[3]
激酶实验	Recombinant cyclin/CDK holoenzymes were purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes were typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mmol/L Tris-HCl (pH 8.0), 10 mmol/L MgCl2, 1 mmol/L DTT, and 0.1 mmol/L sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μmol/L substrate solution (a biotinylated peptide derived from histone H1) were mixed and combined with 10 μL of diluted SCH 727965. The reaction was started by the addition of 50 μL of 2 μmol/L ATP and 0.1 μCi of 33P-ATP. Kinase reactions were incubated for 1 hour at room temperature and were stopped by the addition of 0.1% Triton X-100, 1 mmol/L ATP, 5 mmol/L EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads were captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads were washed twice with 2 mol/L NaCl and twice with 2 mol/L NaCl containing 1% phosphoric acid. The signal was then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves were generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values were derived by nonlinear regression analysis [1].
细胞实验	A2780 cells were plated into six-well tissue culture dishes and allowed to adhere. Cells were then exposed to differing concentrations of SCH 727965 or a DMSO control vehicle for 24 hours, followed by a brief (30 min) pulsed exposure to bromodeoxyuridine (BrdUrd). Cells were then harvested, immunostained using FITC-conjugated antibodies specific for BrdUrd, counter-stained with propidium iodide/RNase A solution, and analyzed using flow cytometry. Fluorescence-activated cell sorting analyses were done on a FACSCalibur instrument. FITC-positive BrdUrd staining and propidium iodide signal allowed assessment of ongoing DNA replication and the cell cycle stage. Percentages of the cell population in each cell cycle stage were plotted for each test article concentration [1].
动物实验	For tumor implantation, specific cell lines were grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4 × 10^7 to 5 × 10^7 cells per milliliter. Nude mice were injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) were measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L × W × H)/2. When the tumor volume reached ～100 mm^3, the animals were randomized to treatment groups (10 mice/group) and treated i.p. with either SCH 727965 or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights were measured during and after the treatment periods. Data were expressed as means ± SEM. Animals were euthanized according to the Institutional Animal Care and Use Committee guidelines [1].

别名	SCH 727965, PS-095760
化合物与蛋白结合的复合物	BRDT in complex with Dinaciclib
分子量	396.49
分子式	C21H28N6O2
CAS No.	779353-01-4

存储

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

溶解度

DMSO: 50 mg/mL (126.11 mM)

Ethanol: 8 mg/mL (20.17 mM), Heating 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 / Ethanol	1 mM	2.5221 mL	12.6107 mL	25.2213 mL	63.0533 mL
	5 mM	0.5044 mL	2.5221 mL	5.0443 mL	12.6107 mL
	10 mM	0.2522 mL	1.2611 mL	2.5221 mL	6.3053 mL
	20 mM	0.1261 mL	0.6305 mL	1.2611 mL	3.1527 mL
DMSO	50 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2611 mL
DMSO	100 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6305 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Feldmann G, et al. Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models. Cancer Biol Ther. 2011 Oct 1;12(7):598-609. 2. Fu W, et al. The cyclin-dependent kinase inhibitor SCH 727965 (dinacliclib) induces the apoptosis of osteosarcoma cells. Mol Cancer Ther. 2011 Jun;10(6):1018-27. 3. Parry D, et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. 4. Lin B, Li Y, Wang T, et al. CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK[J]. Oncogene. 2020, 39(37): 6024-6040.

文献引用

1. Wang Z, Chen D, Guan D, et al. Material properties of phase-separated TFEB condensates regulate the autophagy-lysosome pathway. Journal of Cell Biology. 2022, 221(5): e202112024 2. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 3. Lin B, Li Y, Wang T, et al. CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK. Oncogene. 2020, 39(37): 6024-6040 4. Ly T T G, Yun J, Ha J S, et al. Inhibitory Effect of Etravirine, a Non-Nucleoside Reverse Transcriptase Inhibitor, via Anterior Gradient Protein 2 Homolog Degradation against Ovarian Cancer Metastasis. International Journal of Molecular Sciences. 2022, 23(2): 944. 5. Pu Y, Yan D, Tu L, et al. CDK Inhibition Reverses Acquired 5-Fluorouracil Resistance in Hepatocellular Carcinoma Cells. Disease Markers. 2022 6. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.

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

Dinaciclib 779353-01-4 Apoptosis Cell Cycle/Checkpoint CDK inhibit Inhibitor SCH 727965 SCH727965 PS-095760 Cyclin dependent kinase PS095760 PS 095760 SCH-727965 inhibitor

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Dinaciclib

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

文献引用

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剂量换算

体内实验配液计算器

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