化合物 Dinaciclib|T1912

Dinaciclib
779353-01-4

￥498 2mg 起订

￥797 5mg 起订

￥1240 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Dinaciclib

英文名称：: Dinaciclib

CAS号：: 779353-01-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.75%

产品类别：: 抑制剂

货号：: T1912

Product Introduction

Bioactivity

名称	Dinaciclib
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.
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].
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].
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].
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (126.11 mM) Ethanol : 8 mg/mL (20.17 mM), Heating is recommended.
关键字	inhibit \| Inhibitor \| SCH727965 \| Cyclin dependent kinase \| CDK \| Apoptosis \| PS095760 \| PS 095760 \| Dinaciclib \| SCH-727965
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SCH 727965|||PS-095760|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子