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

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

Cat. No.: HY-30237 Purity: 98.73%
COA Handling Instructions

(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.

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

(R)-Roscovitine Chemical Structure

(R)-Roscovitine Chemical Structure

CAS No. : 186692-46-6

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 87 In-stock
Solid
10 mg USD 79 In-stock
50 mg USD 198 In-stock
100 mg USD 264 In-stock
200 mg USD 370 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 23 publication(s) in Google Scholar

(R)-Roscovitine Related Antibodies

Top Publications Citing Use of Products

    (R)-Roscovitine purchased from MCE. 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.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (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)

    In Vitro

    (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].

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

    (R)-Roscovitine Related Antibodies
    In Vivo

    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].

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

    354.45

    Appearance

    Solid

    Formula

    C19H26N6O
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (282.13 mM)

    *"≥" 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
    *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

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

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

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.73%

    COA (252 KB) LCMS (262 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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].

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

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    (R)-Roscovitine Related Classifications

    Help & FAQs
    • 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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    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

    Keywords:

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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    (R)-Roscovitine
    Cat. No.:
    HY-30237
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.