1. Cell Cycle/DNA Damage
  2. CDK
  3. Ribociclib succinate

Ribociclib succinate  (Synonyms: LEE011 succinate)

Cat. No.: HY-15777B Purity: 99.93%
COA Handling Instructions

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

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

Ribociclib succinate Chemical Structure

Ribociclib succinate Chemical Structure

CAS No. : 1374639-75-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 144 In-stock
100 mg USD 216 In-stock
200 mg USD 348 In-stock
500 mg USD 624 In-stock
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Customer Review

Based on 56 publication(s) in Google Scholar

Other Forms of Ribociclib succinate:

Top Publications Citing Use of Products

51 Publications Citing Use of MCE Ribociclib succinate

WB

    Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22.  [Abstract]

    Head-to-head comparison of the effect of PD 0332991 and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

    Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM for 72 h.

    Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59.  [Abstract]

    Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

    Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59.  [Abstract]

    Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

    IC50 & Target[1]

    CDK4

    10 nM (IC50)

    CDK6

    39 nM (IC50)

    In Vitro

    Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].

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

    In Vivo

    CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment[2].

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

    Clinical Trial
    Molecular Weight

    552.63

    Formula

    C27H36N8O5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5.OC(CCC(O)=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 9.38 mg/mL (16.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 4.17 mg/mL (7.55 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8095 mL 9.0476 mL 18.0953 mL
    5 mM 0.3619 mL 1.8095 mL 3.6191 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 3.12 mg/mL (5.65 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.93%

    References
    Cell Assay
    [2]

    Cells are grown for 24 hours in 35 mm plates, treated with 500 nM Ribociclib for 6 days, and then fixed and stained overnight. Cells are then imaged for SA-β-gal using an Axio Observer D.1 phase contrast microscope. The percentage of SA-β-gal positive cells is determined by counting the number of positive cells present in three separate microscope frames, and then normalizing to the control. To assess apoptotic activity, cells are plated in triplicate in 96 well plates, treated with Ribociclib, and assayed for caspase 3/7 activation 16 hours after treatment with Caspase-Glo 3/7. Cells treated with SN-38 are used as a positive control[2].

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

    Animal Administration
    [2]

    Mice[2]
    The BE2C, NB-1643, or EBC1 cell line-derived xenografts are implanted subcutaneously into the right flank of CB17 SCID-/- mice. Animals bearing engrafted tumors of 200-600 mm3 are then randomized to oral treatment with 200 mg/kg Ribociclib in 0.5 % methylcellulose (n=10) or vehicle (n=10) daily for a total of 21 days. Tumor burden is determined periodically throughout treatment according to the formula (π/6)×d2, where d represents the mean tumor diameter obtained by caliper measurement.

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

    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.8095 mL 9.0476 mL 18.0953 mL 45.2382 mL
    5 mM 0.3619 mL 1.8095 mL 3.6191 mL 9.0476 mL
    DMSO 10 mM 0.1810 mL 0.9048 mL 1.8095 mL 4.5238 mL
    15 mM 0.1206 mL 0.6032 mL 1.2064 mL 3.0159 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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    Product Name:
    Ribociclib succinate
    Cat. No.:
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