1. Cell Cycle/DNA Damage
  2. CDK

LEE011 hydrochloride (Synonyms: Ribociclib hydrochloride)

Cat. No.: HY-15777A
Handling Instructions

LEE011 hydrochloride 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.
LEE011 hydrochloride Chemical Structure

LEE011 hydrochloride Chemical Structure

CAS No. : 1211443-80-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $80 In-stock
50 mg $150 In-stock
100 mg $250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of LEE011 hydrochloride:

    LEE011 hydrochloride purchased from MCE. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59.

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

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    • Biological Activity

    • Protocol

    • Technical Information

    • References

    Description

    LEE011 hydrochloride 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

    IC50: 10/39 nM (CDK4/6)[1]

    In Vitro

    Treating a panel of 17 neuroblastoma cell lines with LEE011 (Ribociclib) across a four-log dose range (10 to 10,000 nM). Treatment with LEE011 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. LEE011 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 LEE011 concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].

    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 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].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.1231 mL 10.6157 mL 21.2314 mL
    5 mM 0.4246 mL 2.1231 mL 4.2463 mL
    10 mM 0.2123 mL 1.0616 mL 2.1231 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    LEE011 (Ribociclib) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

    Cells are grown for 24 hours in 35 mm plates, treated with 500 nM LEE011 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 LEE011, 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]

    LEE011 (Ribociclib) is dissolved in 0.5 % methylcellulose (Mice)[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 LEE011 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
    Molecular Weight

    471.0

    Formula

    C₂₃H₃₁ClN₈O

    CAS No.

    1211443-80-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    LEE011 salt is dissolved in 0.5% methylcellulose[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    LEE011 hydrochloride
    Cat. No.:
    HY-15777A
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