1. Cell Cycle/DNA Damage
  2. CDK
  3. Seliciclib

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

Cat. No.: HY-30237 Purity: 99.94%
Handling Instructions

Seliciclib (Roscovitine) 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.

For research use only. We do not sell to patients.

Seliciclib Chemical Structure

Seliciclib Chemical Structure

CAS No. : 186692-46-6

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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Seliciclib purchased from MCE. Usage Cited in: Neuroreport. 2018 Mar 7;29(4):241-246.

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review


    Seliciclib (Roscovitine) 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)


    0.16 μM (IC50)


    30 μM (IC50)


    34 μM (IC50)


    14 μM (IC50)

    IR tyrosine kinase

    70 μM (IC50)

    In Vitro

    Seliciclib (Roscovitine) 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 Seliciclib (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 Seliciclib (Roscovitine) (IC50>100 μM). Extracellular regulated kinases erk1 and erk2 are inhibited with an IC50 of 34 μM and 14 μM, respectively. Seliciclib (Roscovitine) inhibits the proliferation of mammalian cell lines with an average IC50 of 16 μM[1]. Seliciclib decreases the level of CDK5 and p35 with upregulation of E-cadherin, but downregulation of Vimentin and Collagen IV. Moreover, Seliciclib (Roscovitine) inhibits the ability of high glucose cultured NRK52E cells to migrate and invade[2].

    In Vivo

    Compare with normal controls, Seliciclib (Roscovitine) downregulates phosphorylated ERK1/2 and PPARγ with concomitant increase in E-cadherin, but decrease in Vimentin and Collagen IV. Correspondingly, Seliciclib decreases renal tubulointerstitial fibrosis of diabetic rats. Seliciclib (Roscovitine) is effective in decreasing tubulointerstitial fibrosis via the ERK1/2/PPARγ pathway in diabetic rats[2]. Seliciclib (Roscovitine) (16.5 mg/kg) significantly reduces the rate of tumor growth and increases survival of treated mice. Strikingly, Seliciclib (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 Seliciclib and control mice, and behavioral differences between the two groups are also negligible. These results suggest that Seliciclib can be used effectively as a selective tumor growth inhibitor in HPV+ head and neck cancer[3].

    Clinical Trial
    Molecular Weight




    CAS No.



    OC[[email protected]](NC1=NC(NCC2=CC=CC=C2)=C3C(N(C=N3)C(C)C)=N1)CC


    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (282.13 mM)

    *"≥" means soluble, but saturation unknown.

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    Cell Assay

    Rat kidney tubular epithelial cells (NRK52E) are used. CDK5 inhibitor Seliciclib (Roscovitine) (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].

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

    Animal Administration

    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.
    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.

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


    Purity: 99.94%

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    SeliciclibRoscovitineCYC202R-roscovitineCYC 202CYC-202CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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