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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Cited by 11 Publications

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.

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Choose Selective CDK Inhibitors

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 M2LsTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\4O4IzPCCq MW\HTVUxRTJ5NjDuUS=> M1fFVFI2QDV{MEW4
Myoblast MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXS3NkBp MmLETWM2OD1zMEO1JI5O NEjFS2szPThzMEO3OS=>
IMRS M2TDXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULSd5dmPzJiaB?= MW\JR|UxRTh5MzDuUS=> MmHxNlU5OTB|N{W=
SKNAS NXPr[WVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K1PVczKGh? M3j4SWlEPTExvK6xNFAxOCCwTR?= MVuyOVgyODN5NR?=
Rh28 Moi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrkO|IhcA>? M4fG[WlEPTB;OES1JI5O M3njWFI2QDFyM{e1
Rh41 NFXiPXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP4O|IhcA>? M1rHRWlEPTB;N{G4O{BvVQ>? MoTwNlU5OTB|N{W=
CW9019 NV3xSnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXy3ZpN3PzJiaB?= MlHmTWM2OD17OUGyJI5O NX;SRZNnOjV6MUCzO|U>
Rh5 M3;FT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;RSHU5PzJiaB?= NEPHT3pKSzVy78{eNVAxODBibl2= M2nmbFI2QDFyM{e1
Rh30 NIDwfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmryO|IhcA>? NXTKRVY2UUN3MP-8olExODByIH7N MkHRNlU5OTB|N{W=
778 NIPtTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITtO404OiCq NGiwcXVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M{TnZVI2ODJ6NE[5
449 NUTNcm9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHnVXBGPzJiaB?= NEf4RYlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWrWdGh4OjVyMki0Olk>
LP3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrDOIg4OiCq M37OdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXOyOVAzQDR4OR?=
LP6 NGLxVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nuSlczKGh? NFq2NVlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M4PrdFI2ODJ6NE[5
LP8 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LBZVczKGh? NGSwc25qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NX\MbmsxOjVyMki0Olk>
LPS141 M37vV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\4O|IhcA>? NFnrOHVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NH;GOpozPTB{OES2PS=>
778 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\XV|MvOzNizszN NV3ZT4tuOjRiaB?= NEOz[21l\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M2TBSVI2ODJ6NE[5
449 NVTkT2JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:ycFBiOy5|MzFOwG0> MkfsNlQhcA>? M2TMToRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NH;iXpAzPTB{OES2PS=>
LP3 NVvGdYpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2njXlMvOzNizszN NV\sVVlwOjRiaB?= MlrV[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MmHLNlUxOjh2Nkm=
LP6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTFN{4{OyEQvF2= M2jQUVI1KGh? NWXLbYVM\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MmHtNlUxOjh2Nkm=
LP8 NH:2[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOzMlM{KM7:TR?= NV;xTpE6OjRiaB?= M2[0[oRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NIPufXUzPTB{OES2PS=>
LPS141 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7Zd|M{NjN|IN88US=> MYCyOEBp MXTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NGXVcZYzPTB{OES2PS=>
IMR5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnhNHNqOjRiaB?= MmTHSG1UVw>? NYfjXoIyUUN3ME2xNlYhdk1? NXjqblJROjRyNEWxO|k>
BE2C M3HxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm4SHczPCCq MkG4SG1UVw>? MlGxTWM2OD1zM{Sgcm0> M1z4N|I1ODR3MUe5
1643 M1fSNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvGPZg5OjRiaB?= Mk\VSG1UVw>? M3zWbmlEPTB;MUS3JI5O NIS1THIzPDB2NUG3PS=>
SKNSH MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G5W|I1KGh? MljHSG1UVw>? NFLWS5RKSzVyPUG0PEBvVQ>? NX3IVWd{OjRyNEWxO|k>
SY5Y MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWyOEBp M33hUGROW09? M2TOTGlEPTB;MUW0JI5O MWWyOFA1PTF5OR?=
NGP MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSyOEBp MWrEUXNQ MnLWTWM2OD1zN{Wgcm0> MYOyOFA1PTF5OR?=
KELLY MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm2T4EzPCCq NVPYbYNITE2VTx?= NV7I[GJbUUN3ME2yNlAhdk1? NIjK[4IzPDB2NUG3PS=>
CHP134 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17ROVI1KGh? NITVSJFFVVOR MX\JR|UxRTJ5MzDuUS=> Ml7LNlQxPDVzN{m=
NLF NGKzbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7Sb2ozPCCq M{HTbmROW09? MUjJR|UxRTN{ODDuUS=> M3vSd|I1ODR3MUe5
LAN5 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLxNlQhcA>? MXrEUXNQ MWfJR|UxRTR{OTDuUS=> M{HZR|I1ODR3MUe5
NB69 NVq5V|lQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnaUIszPCCq MoXTSG1UVw>? NFfibm9KSzVyPUezPEBvVQ>? MUKyOFA1PTF5OR?=
SKNDZ M134Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXWNlQhcA>? MnzGSG1UVw>? MkC3TWM2OD16MEGgcm0> MkW2NlQxPDVzN{m=
NBSD NWrRW25GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrnPG8zPCCq MkD1SG1UVw>? MXjJR|UxRTF7MECgcm0> MVWyOFA1PTF5OR?=
SKNF1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDLNlQhcA>? MX3EUXNQ M1\0TGlEPTB;M{WwNEBvVQ>? M{nBNlI1ODR3MUe5
EBC1 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDQNlQhcA>? MmXOSG1UVw>? M3TTN2lEPTB;NkSwNEBvVQ>? NXTyV4R6OjRyNEWxO|k>
SKNAS MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjxPZAzPCCq MYfEUXNQ MlSyTWM2OO,:nkGwNFAxKG6P MVWyOFA1PTF5OR?=
NB16 NFLWcYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPrbo8zPCCq MXPEUXNQ M3O5RWlEPTExvK6xNFAxOCCwTR?= NEPCcIkzPDB2NUG3PS=>
RPE1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWftbI1jOjRiaB?= M{Wxb2ROW09? NYPLdGtJUUN3MP-8olExODByIH7N M13STlI1ODR3MUe5

... 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
NCT03822468 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2019 Phase 2
NCT03822468 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2019 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03839823 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis February 28 2019 Phase 2
NCT03839823 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis February 28 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID