达那唑

达那唑，Dinaciclib，Cas号 779353-01-4，纯度: 99.75%，是一种 CDK 抑制剂，抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50=3/1/1/4 nM)，具有选择性。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

关键词

达那唑

所属分类

抑制剂

目录号

T1912

获取报价

猜你喜欢

产品描述
产品组分
文件资源
营销中心
注意事项
FAQ
文献追踪

达那唑，Dinaciclib (SCH 727965) 是一种 CDK 抑制剂，抑制 CDK1、CDK2、CDK5 和 CDK9 (IC₅₀=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。

生物活性

产品描述	Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC₅₀ = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.
靶点活性 (IC₅₀)	CDK2:1 nM (cell free), CDK5:1 nM (cell free), CDK9:4 nM (cell free), CDK1:3 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

化学信息

分子量	396.49
分子式	C₂₁H₂₈N₆O₂
CAS No.	779353-01-4
Smiles	N(CC1=CN(=O)=CC=C1)C=2N3C(N=C(C2)N4[C@H](CCO)CCCC4)=C(CC)C=N3
密度	1.33 g/cm3

产品组分

内容	型号	规格	储存温度
达那唑	T1912-01	1mg	-20°C
达那唑	T1912-02	5mg	-20°C
达那唑	T1912-03	10mg	-20°C
达那唑	T1912-04	25mg	-20°C
达那唑	T1912-04	50mg	-20°C
达那唑	T1912-05	100mg	-20°C
达那唑	T1912-06	1mLx10mM in DMSO	-20°C
操作手册	1	1	常温

文件资源

营销中心
注意事项

保存建议厂家推荐蓝冰运输。当您收到产品后，按照说明书建议保存于-20°C。
FAQ
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.