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Seliciclib

产品编号 T2095 CAS 186692-46-6

别名: Roscovitine, R-roscovitine, CYC202

Seliciclib (Roscovitine) 是 Cdk2/cyclin E 的有效抑制剂，IC50为0.1 µM。它还抑制 Cdk7/cyclin H、Cdk5/p35 和 Cdc2/cyclin B，IC50为 0.49、0.16和0.65 µM。

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Seliciclib, CAS 186692-46-6

规格	价格/CNY	货期
5 mg	￥ 415	现货
10 mg	￥ 734	现货
25 mg	￥ 995	现货
50 mg	￥ 1,597	现货
100 mg	￥ 2,433	现货
200 mg	￥ 3,996	现货
1 mL * 10 mM (in DMSO)	￥ 457	现货

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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	Seliciclib (Roscovitine) is a potent inhibitor of Cdk2/cyclin E (IC50: 0.1 μM). It also inhibits Cdk7/cyclin H, Cdk5/p35, and Cdc2/cyclin B (IC50s: 0.49/0.16/0.65 μM).
靶点活性	CDK5-p35:0.16 μM (cell free), ERK2:14 μM (cell free), CDK2-CyclinE:0.7 μM (cell free), CDC2-cyclinB:0.65 μM (cell free), CDK2-CyclinA:0.7 μM (cell free)
体外活性	Most kinases are not significantly inhibited by roscovitine. cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p35 only are substantially inhibited (IC50 values of 0.65, 0.7, 0.7 and 0.2 μM, respectively). Extracellular regulated kinases erk1 and erk2 are inhibited with an IC50 of 34 microM and 14 microM, respectively. Roscovitine reversibly arrests starfish oocytes and sea urchin embryos in late prophase [1]. Roscovitine (25 microM) inhibited FCS-induced proliferation in cultured MC [2].
体内活性	In diabetic rats, CDK5 inhibitor roscovitine decreased renal fibrosis and improved renal function [3]. In vivo experiments showed that s.c. growth of ESFT xenografts was also significantly slowed by i.p. injection of roscovitine [4].
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].
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].
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].

别名	Roscovitine, R-roscovitine, CYC202
分子量	354.45
分子式	C19H26N6O
CAS No.	186692-46-6

存储

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

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)

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	2.8213 mL	14.1064 mL	28.2127 mL	70.5318 mL
	5 mM	0.5643 mL	2.8213 mL	5.6425 mL	14.1064 mL
	10 mM	0.2821 mL	1.4106 mL	2.8213 mL	7.0532 mL
DMSO	20 mM	0.1411 mL	0.7053 mL	1.4106 mL	3.5266 mL
	50 mM	0.0564 mL	0.2821 mL	0.5643 mL	1.4106 mL
	100 mM	0.0282 mL	0.1411 mL	0.2821 mL	0.7053 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. Meijer L, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36. 2. Pippin JW, et al. Direct in vivo inhibition of the nuclear cell cycle cascade in experimental mesangial proliferative glomerulonephritis with Roscovitine, a novel cyclin-dependent kinase antagonist. J Clin Invest. 1997 Nov 15;100(10):2512-20. 3. Bai X, et al. CDK5 promotes renal tubulointerstitial fibrosis in diabetic nephropathy via erk1/2/pparγ pathway. Oncotarget. 2016 Apr 27. 4. Tirado OM, et al. Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family tumor cells in vitro and in vivo. Cancer Res. 2005 Oct 15;65(20):9320-7. 5. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

文献引用

1. Li Q, Zhou Y, He W, et al. Platelet-armored nanoplatform to harmonize janus-faced IFN-γ against tumor recurrence and metastasis. Journal of Controlled Release. 2021 2. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973 3. Liang X L, Ouyang L, Yu N N, et al.Histone deacetylase inhibitor pracinostat suppresses colorectal cancer by inducing CDK5-Drp1 signaling-mediated peripheral mitofission.Journal of Pharmaceutical Analysis.2023 4. 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

Seliciclib 186692-46-6 Cell Cycle/Checkpoint CDK Roscovitine CYC-202 inhibit CYC 202 Inhibitor R-roscovitine CYC202 Cyclin dependent kinase inhibitor

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Seliciclib

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

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

Keywords