2. Cell Cycle/DNA Damage
  3. CDK
  4. (R)-Roscovitine

(R)-Roscovitine  (Synonyms: Seliciclib; CYC202)

製品番号: HY-30237 純度: 99.84%
COA 取扱説明書

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(R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

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(R)-Roscovitine 構造式

(R)-Roscovitine 構造式

CAS 番号 : 186692-46-6

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 87 在庫あり
Solution
10 mM * 1 mL in DMSO USD 87 在庫あり
Solid
5 mg USD 50 お問い合わせ
10 mg USD 79 在庫あり
50 mg USD 198 在庫あり
100 mg USD 264 在庫あり
200 mg USD 370 在庫あり

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カスタマーレビュー

Based on 25 publication(s) in Google Scholar

(R)-Roscovitine 関連抗体

Top Publications Citing Use of Products

    (R)-Roscovitine purchased from MedChemExpress. Usage Cited in: Neuroreport. 2018 Mar 7;29(4):241-246.  [Abstract]

    R-E 235da1 exposure increases Cdk5 activity. Protein expression levels of P-histone H1 and Cdk5. P-histone H1 levels represent the activity of Cdk5. Bands for Cdk5 are the input. R-E 235da1 exposure increased Cdk5 activity.

    CDK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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    製品説明

    (R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

    IC50 & Target[1]

    cdc2/cyclin B

    0.65 μM (IC50)

    cdk2/cyclin A

    0.7 μM (IC50)

    Cdk2/cyclin E2

    0.7 μM (IC50)

    CDK5/p35

    0.16 μM (IC50)

    GST-erk1

    30 μM (IC50)

    erk1

    34 μM (IC50)

    erk2

    14 μM (IC50)

    IR tyrosine kinase

    70 μM (IC50)

    体外実験

    (R)-Roscovitine (Seliciclib) displays high efficiency and high selectivity towards some cyclin-dependent kinases. The kinase specificity of Seliciclib is investigated with 25 highly purified kinases (including protein kinase A, G and C isoforms, myosin light-chain kinase, casein kinase 2, IR tyrosine kinase, c-src, v-abl). Most kinases are not significantly inhibited by (R)-Roscovitine. Cdc2, Cdk2, and Cdk5 only are substantially inhibited (IC50 values of 0.65, 0.7, and 0.2 μM, respectively). Cdk4k and Cdk6 are very poorly inhibited by (R)-Roscovitine (IC50>100 μM). Extracellular regulated kinases erk1 and erk2 are inhibited with an IC50 of 34 μM and 14 μM, respectively. (R)-Roscovitine inhibits the proliferation of mammalian cell lines with an average IC50 of 16 μM[1]. (R)-Roscovitine (Seliciclib) decreases the level of CDK5 and p35 with upregulation of E-cadherin, but downregulation of Vimentin and Collagen IV. Moreover, (R)-Roscovitine inhibits the ability of high glucose cultured NRK52E cells to migrate and invade[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    (R)-Roscovitine 関連抗体
    体内実験

    Compare with normal controls, (R)-Roscovitine (Seliciclib) downregulates phosphorylated ERK1/2 and PPARγ with concomitant increase in E-cadherin, but decrease in Vimentin and Collagen IV. Correspondingly, (R)-Roscovitine decreases renal tubulointerstitial fibrosis of diabetic rats. (R)-Roscovitine is effective in decreasing tubulointerstitial fibrosis via the ERK1/2/PPARγ pathway in diabetic rats[2]. (R)-Roscovitine (Seliciclib) (16.5 mg/kg) significantly reduces the rate of tumor growth and increases survival of treated mice. Strikingly, (R)-Roscovitine treatment leads to complete tumor disappearance in one mouse (25%); moreover, no tumor regrowth in this mouse is found 5 months after completion of the treatment. Mouse weights do not differ significantly between mice treated with (R)-Roscovitine and control mice, and behavioral differences between the two groups are also negligible. These results suggest that (R)-Roscovitine can be used effectively as a selective tumor growth inhibitor in HPV+ head and neck cancer[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    354.45

    分子式

    C19H26N6O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC[C@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(C=N3)C(C)C)=N1)CC
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (282.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8213 mL 14.1064 mL 28.2127 mL
    5 mM 0.5643 mL 2.8213 mL 5.6425 mL
    10 mM 0.2821 mL 1.4106 mL 2.8213 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.84%

    COA (252 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    Rat kidney tubular epithelial cells (NRK52E) are used. CDK5 inhibitor (R)-Roscovitine (Seliciclib) (Ros.; 10 μM) and activator p35 (15 μM), PPARγ agonist BRL 49653 (Rosi.; 50 nM), and ERK1/2 inhibitor U0126 (50 nM) are used to treat NRK52E cells. Cells in each group are treated for 72 hours and then harvested for further analyses[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2][3]

    Rats[2]
    Male Sprague Dawley rats (6-8 weeks of age) are given intraperitoneally a single injection of either Streptozotocin (65 mg/kg) diluted in 0.1 M citrate buffer pH 4.5 (diabetic) or citrate buffer (non-diabetic). Plasma glucose concentrations are determined using the glucose oxidase method on a glucose analyzer three days after the injection. Rats with a glucose level over 16.7 mM are considered diabetic and thus included in the study. Plasma glucose level is measured once every week. To investigate the effect of CDK5 inhibition on renal tubulointerstitial fibrosis, Seliciclib (25 mg/kg) is injected peritoneally to diabetic rats every day till sacrifice. DMSO is included as controls.
    Mice[3]
    Exponentially growing UMSCC47 cells are injected subcutaneously into the sacral area of female NUDE mice. Each mouse is inoculated with 2×105 cells in 50% matrigel and 50% PBS at a volume of 100 μL. After tumors reach a measurable size, the mice are given 16.5 mg/kg doses of intraperitoneal Seliciclib or vehicle injections. Body weight, tumor growth, and general behavior are monitored. Tumor volumes are measured every 3 days. Mice are sacrificed when the tumor exceeded a size of 0.5cm3.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 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
    15 mM 0.1881 mL 0.9404 mL 1.8808 mL 4.7021 mL
    20 mM 0.1411 mL 0.7053 mL 1.4106 mL 3.5266 mL
    25 mM 0.1129 mL 0.5643 mL 1.1285 mL 2.8213 mL
    30 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3511 mL
    40 mM 0.0705 mL 0.3527 mL 0.7053 mL 1.7633 mL
    50 mM 0.0564 mL 0.2821 mL 0.5643 mL 1.4106 mL
    60 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1755 mL
    80 mM 0.0353 mL 0.1763 mL 0.3527 mL 0.8816 mL
    100 mM 0.0282 mL 0.1411 mL 0.2821 mL 0.7053 mL
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    (R)-Roscovitine Related Classifications

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    (R)-Roscovitine186692-46-6Seliciclib CYC202CYC202CYC 202CYC-202CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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