化合物 Roscovitine|T2095

Seliciclib
186692-46-6

￥415 5mg 起订

￥734 10mg 起订

￥995 25mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Roscovitine

英文名称：: Seliciclib

CAS号：: 186692-46-6

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：: 99.88%

产品类别：: 抑制剂

货号：: T2095

Product Introduction

Bioactivity

名称	Seliciclib
描述	Seliciclib (Roscovitine) is a potent inhibitor of Cdk2/cyclin E (IC50=0.1 µM). Seliciclib also inhibits Cdk7/cyclin H, Cdk5/p35 and Cdc2/cyclin B (IC50=0.49/0.16/0.65 µM). Seliciclib has antitumor activity.
细胞实验	L1210 cells taken from exponentially growing cultures in RPMT-1640 medium supplemented with 10% foetal calf serum, penicillin and streptomycin, were counted using a hemocytometer, seeded at 5X10^4 cells/ml in tissue-culture 96-wells plates in the presence or absence of various concentrations of roscovitine or olomoucine and incubated at 37°C under 5% CO,. For reversion of the roscovitine effect, L1210 cells cultured two days in the presence or absence of roscovitine were washed in phosphate-buffered saline to remove any trace of the drug, counted and reseeded in fresh medium containing no drug. Cell growth was monitored daily using the microculture tetrazolium assay. Cell cycle analysis was performed on cells that were fixed in ethanol, treated with 100 μg/ml RNase and stained with propidium iodide. We used a Coulter EPICS Elite flow cytometer for acquisition and the Multicycle software for analysis of the data. All assays were performed in triplicate and experiments repeated at least twice [1].
激酶实验	Kinases activities were assayed at 30°C in buffer C (unless otherwise specified). Blank values were substracted from the data and activities calculated as the molar amount of phosphate incorporated in protein acceptor during a 10-min incubation. Controls were performed with appropriate dilutions of Me2SO. In a few cases, phosphorylation of the substrate was assessed by autoradiography after SDS/PAGE [1].
动物实验	Male athymic nude mice (5-6 weeks old) were obtained from the National Cancer Institute. Mice were housed in the animal facilities of the Georgetown University Division of Comparative Medicine. All animal work was done under protocols approved by the Georgetown University Animal Care and Use Committee. Mice were inoculated s.c. into the right posterior flank with 4 × 10^6 A4573 cells in 100 μL of Matrigel basement membrane matrix. Xenografts were grown to a mean tumor volume of 129 ± 30 mm^3. Roscovitine was first dissolved in either absolute methanol or DMSO (1 volume). A carrier solution was produced by using a diluent containing 10% Tween 80, 20% N-N-dimethylacetamide, and 70% polyethylene glycol 400. Mice were randomized into two groups (six animals per group) and treatment was initiated. One group was treated with roscovitine, administered as a single daily i.p. injection, at a dose of 50 mg/kg, for either 5 days or two 5-day series with a 2-day break in between. The control group received i.p. injections of the carrier solution following identical schedules. All mice were sacrificed by asphyxiation with CO2. Roscovitine-treated mice were euthanized either 7 days after the first injection or up to 4 weeks after completion of the treatment. At those times, tumors were removed, measured, and prepared for TUNEL assays. Primary tumor volumes were calculated by the formula V = (1/2)a × b2, where a is the longest tumor axis and b is the shortest tumor axis. Data are given as mean values ± SE in quantitative experiments. Statistical analysis of differences between groups was done by a one-way ANOVA followed by an unpaired Student's t-test [4].
体外活性	方法: MM 细胞系 MM.1S、OPM2、RPMI、U266、Dox-40、LR5、MM1.R 用 Seliciclib (10-100 µM) 处理 24 h，通过 MTT assay 检测细胞活力。结果: Seliciclib 在 24 h 内产生剂量依赖性细胞毒性，IC50 范围为 15-25 µM。[1] 方法: 套细胞淋巴瘤 (MCL) 细胞 Granta-519、NCEB-1、REC-1 和 JeKo-1 用 Seliciclib (25-50 µM) 处理 24-48 h，通过 Flow cytometry 检测细胞周期。结果: 用 IC50 剂量的 Seliciclib 处理 24 h 后，Granta-519、NCEB-1 和 REC-1 细胞中检测到 G2-M 期细胞的积聚，与对照组相比，JeKo-1 细胞在 48 h 时检测到细胞的积聚。用 Seliciclib 处理 24 和 48 h 后，除 Granta-519 外，所有细胞的 sub-G1 峰都明显增加，表明细胞凋亡。[2]
体内活性	方法: 为检测体内抗肿瘤活性，将 Seliciclib (300 mg/kg/d) 在 Zeitgeber 时间 (ZT) 3、11 或 19 口服给药给携带 Glasgow 骨肉瘤的 B6D2F1 小鼠，持续 5 天。结果: 与对照组相比，Seliciclib 在 ZT3 或 ZT11 给药后将肿瘤生长减少了 55%，在 ZT19 给药后减少了 35%。[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	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (141.06 mM) Ethanol : 6 mg/mL (16.92 mM)
关键字	CYC-202 \| inhibit \| CYC 202 \| Seliciclib \| Inhibitor \| Cyclin dependent kinase \| CDK
相关产品	Sodium Oxamate \| Ribociclib \| Palbociclib monohydrochloride \| Abemaciclib methanesulfonate \| CASIN \| Olomoucine \| Palbociclib \| GW 441756 \| Dinaciclib \| Ro-3306 \| GSK 3 Inhibitor IX \| Abemaciclib
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 表型筛选靶点鉴定库 \| 抗癌药物库

Roscovitine|||R-roscovitine|||CYC202|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