Ribociclib (LEE011)

Catalog No.S7440

Ribociclib (LEE011) Chemical Structure

Molecular Weight(MW): 434.54

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

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6 Customer Reviews

  • IB analysis of whole cell lysates derived from mouse CT26 or 4T1 tumor cell lines treated with or without the CDK4/6 inhibitor, ribociclib.

    Nature, 2017, 553(7686):91-95. Ribociclib (LEE011) purchased from Selleck.

    The combination of a different mTOR inhibitor temsirolimus (4 μM) and a different CDK4/6 inhibitor ribociclib (4 μM) is also synergistic against GICs (***P < 0.0001; one-way ANOVA with post-hoc Tukey analysis).

    Clin Cancer Res, 2017, 23(22):6958-6968. Ribociclib (LEE011) purchased from Selleck.

  • The effects of the CDK inhibitor abemaciclib, palbociclib, and ribociclib on Trop2 ICD cleavage. CDK inhibitors decreased Trop2 ICD abundance after the second day of CDK inhibitor treatment.

    Cancer Res, 2016, 76(22):6723-6734. Ribociclib (LEE011) purchased from Selleck.

    SJSA cells were treated with the alternate CDK4/6 inhibitors Ribociclib (LEE011) and Abemaciclib (LY2835219) for 30 h, alone or in combination with Nutlin at 20 µM for 6 h.

    Cell Death Dis, 2018, 9(9): 918. Ribociclib (LEE011) purchased from Selleck.

  • (B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.

    Transl Oncol, 2016, 9(3):197-202.. Ribociclib (LEE011) purchased from Selleck.

    Analysis of apoptosis in leukemia cells induced by LEE011. Annexin V staining of cells following 48-h treatment with LEE011 at 2 or 5 µM compared with DMSO controls. Following 5-µM LEE011 treatment, the K562 apoptotic cell percentage was 5.9 ± 0.75 vs. 1.2 ± 0.66% for the DMSO group, P = 0.001; in MV4-11 cells, the apoptotic cell percentage was 24.2 ± 3.06 vs. 0.53 ± 0.40% for the DMSO group, P = 0.005; in U937 cells, the apoptotic cell percentage was 9.9 ± 2.81 vs. 0.57 ± 0.42% for the DMSO group, P = 0.027; in HL-60 cells, the apoptotic cell percentage was 28.23 ± 6.01 vs. 0.9 ± 0.8% for the DMSO group, P = 0.015; in THP-1 cells, the apoptotic cell percentage was 1.76 ± 0.4 vs. 1.56 ± 0.45% for the DMSO group, P = 0.59; in CCRF cells, the apoptotic cell percentage was 13.77 ± 3.16 vs. 1.2 ± 0.36% for the DMSO group, P = 0.019; in NB4 cells, the apoptotic cell percentage was 12.1 ± 1.35 vs. 0.86 ± 0.25% for the DMSO group, P = 0.004; and in SHI-1 cells the apoptotic cell percentage was 12.6 ± 2.81 vs. 1.87 ± 0.75% for the DMSO group, P = 0.017. These analyses were repeated three times. *P < 0.05; **P < 0.01

    Cancer Cell Int, 2017, 17:35. Ribociclib (LEE011) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
Features Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
In vitro

LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DFSP105 NVnXXpNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF6yVYUzPCCq M3v0TGdKPTB;Mke2JI5O M1XsXFI2QDV{MEW4
Myoblast Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHXO|IhcA>? NWHtUHh5UUN3ME2xNFM2KG6P NGCx[FUzPThzMEO3OS=>
IMRS NULFfWd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17tb|czKGh? M1L2OWlEPTB;OEezJI5O NHjDVGozPThzMEO3OS=>
SKNAS NEX5N3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki2O|IhcA>? M3nVUGlEPTExvK6xNFAxOCCwTR?= MWGyOVgyODN5NR?=
Rh28 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XyPFczKGh? M{PlPWlEPTB;OES1JI5O M4[0clI2QDFyM{e1
Rh41 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPDeGc4OiCq NH6xPYJKSzVyPUexPFchdk1? MXeyOVgyODN5NR?=
CW9019 M13Mcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjSfZI4OiCq MkXzTWM2OD17OUGyJI5O NVr6OYhqOjV6MUCzO|U>
Rh5 M4q0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mln6O|IhcA>? Ml;LTWM2OO,:nkGwNFAxKG6P M4rSRVI2QDFyM{e1
Rh30 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUniephLPzJiaB?= MVXJR|Ux97zgMUCwNFAhdk1? M{nk[VI2QDFyM{e1
778 NYfJcWt1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jE[VczKGh? M1;I[olvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWe0XGU4OjVyMki0Olk>
449 NUD4eW8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\hPII4OiCq MXHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGPpdY0zPTB{OES2PS=>
LP3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDSZXU4OiCq MYjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXXjUoxSOjVyMki0Olk>
LP6 M13ad2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDiWnpmPzJiaB?= M{fRVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NFjSfnczPTB{OES2PS=>
LP8 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYC3NkBp MV3pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M3foV|I2ODJ6NE[5
LPS141 M1HVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfxU2Y4OiCq NF3XV2pqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MkD2NlUxOjh2Nkm=
778 MnvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LieVMvOzNizszN NUnYOI5NOjRiaB?= MVHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NYfhfY0xOjVyMki0Olk>
449 NF3DXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDkN{4{OyEQvF2= MWGyOEBp NYG2UYQx\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NEXKNGUzPTB{OES2PS=>
LP3 NED5b4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HKb|MvOzNizszN NWLEZ4VMOjRiaB?= NV3RN5dN\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MnXMNlUxOjh2Nkm=
LP6 NIPPbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjR[4Y{NjN|IN88US=> MkDlNlQhcA>? NVuzWmNL\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NVP6SJVUOjVyMki0Olk>
LP8 NYLQdIlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPWN{4{OyEQvF2= M1\sS|I1KGh? MX3k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MUmyOVAzQDR4OR?=
LPS141 NIn0SIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOzMlM{KM7:TR?= NVPkT4hQOjRiaB?= NHm3bHhl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MYeyOVAzQDR4OR?=
IMR5 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX2zcJdOOjRiaB?= NWm0fGVMTE2VTx?= MYDJR|UxRTF{NjDuUS=> M3PwO|I1ODR3MUe5
BE2C NXvhWW16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\RNlQhcA>? NWX2cmNpTE2VTx?= M4XF[WlEPTB;MUO0JI5O NIjwU3AzPDB2NUG3PS=>
1643 NVHHb3lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLkNlQhcA>? MYPEUXNQ NHPjPYlKSzVyPUG0O{BvVQ>? M4frTlI1ODR3MUe5
SKNSH MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjJUXgzPCCq NYPEN2JKTE2VTx?= M1LpbmlEPTB;MUS4JI5O NH3yN3EzPDB2NUG3PS=>
SY5Y M1XNNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vFelI1KGh? M3;WNmROW09? M{\Nc2lEPTB;MUW0JI5O MVGyOFA1PTF5OR?=
NGP MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVeyOEBp MWDEUXNQ NUHUcJFHUUN3ME2xO|Uhdk1? M2LTd|I1ODR3MUe5
KELLY NInWXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuyOEBp NXG1dphHTE2VTx?= NYjXZ3lPUUN3ME2yNlAhdk1? NGDJV4EzPDB2NUG3PS=>
CHP134 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYiyOEBp MUTEUXNQ MUPJR|UxRTJ5MzDuUS=> M2HGR|I1ODR3MUe5
NLF MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HBSFI1KGh? NVLaW3dHTE2VTx?= NYi4ZZhuUUN3ME2zNlghdk1? M3:4WlI1ODR3MUe5
LAN5 NWfWXY53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOyOEBp MoXZSG1UVw>? M4DhfWlEPTB;NEK5JI5O NX\x[FdMOjRyNEWxO|k>
NB69 MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfUPZVkOjRiaB?= NYr3elR2TE2VTx?= MYPJR|UxRTd|ODDuUS=> MmjtNlQxPDVzN{m=
SKNDZ NG\tNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonrNlQhcA>? NXjPXHJvTE2VTx?= M2rHTGlEPTB;OECxJI5O MXmyOFA1PTF5OR?=
NBSD NXjqfmFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W5W|I1KGh? M2LQU2ROW09? M3;zemlEPTB;MUmwNEBvVQ>? MnLyNlQxPDVzN{m=
SKNF1 NVq1WJVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDxNlQhcA>? MlrHSG1UVw>? NEjDXYhKSzVyPUO1NFAhdk1? M1X4TVI1ODR3MUe5
EBC1 NVm1e5hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3GyPFI1KGh? NEXMT3hFVVOR MmezTWM2OD14NECwJI5O Ml73NlQxPDVzN{m=
SKNAS M1fZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTnNlQhcA>? MXHEUXNQ NHLyNYtKSzVy78{eNVAxODBibl2= M4XwRlI1ODR3MUe5
NB16 NXq4TZJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTaVWR5OjRiaB?= NX;PN5U2TE2VTx?= NEnnUVhKSzVy78{eNVAxODBibl2= NV:yVYk2OjRyNEWxO|k>
RPE1 M1W2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4j5TVI1KGh? M2[0e2ROW09? MUTJR|Ux97zgMUCwNFAhdk1? NUDUcHZZOjRyNEWxO|k>

... Click to View More Cell Line Experimental Data

In vivo LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. [1]

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines.
  • Concentrations: 10 μM
  • Incubation Time: ~100 hours
  • Method:

    A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts.
  • Formulation: 0.5% methylcellulose
  • Dosages: ~200 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 7 mg/mL (16.1 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 434.54
Formula

C23H30N8O

CAS No. 1211441-98-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03701334 Not yet recruiting Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 27 2018 Phase 3
NCT03740334 Not yet recruiting Acute Lymphoblastic Leukemia ALL Dana-Farber Cancer Institute|Novartis November 30 2018 Phase 1
NCT03673124 Not yet recruiting Low Grade Serous Carcinoma Gynecologic Oncology Group|Novartis November 30 2018 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2018 Phase 2
NCT03671330 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis August 29 2018 Phase 2
NCT03477396 Active not recruiting Estrogen Receptor and/or Progesterone Receptor Positive|HER2/Neu Negative|Stage IV Breast Cancer AJCC v6 and v7 City of Hope Medical Center|National Cancer Institute (NCI) June 14 2018 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID