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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4 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 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.

  • (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 M3jMcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7vb3RlOjRiaB?= NGPubnZIUTVyPUK3OkBvVQ>? Mo\kNlU5PTJyNUi=
Myoblast NV7TUVVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHwXpBRPzJiaB?= NIrqVphKSzVyPUGwN|Uhdk1? M3LjdlI2QDFyM{e1
IMRS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M336elczKGh? M1P1OGlEPTB;OEezJI5O NVjj[HlnOjV6MUCzO|U>
SKNAS M4f5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi3NkBp NXjXS4ZzUUN3MP-8olExODByIH7N NH:5WlMzPThzMEO3OS=>
Rh28 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO3NkBp NFHTWItKSzVyPUi0OUBvVQ>? M3nCTVI2QDFyM{e1
Rh41 NFPCSYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjrbFA4OiCq MXjJR|UxRTdzOEegcm0> NGHISYgzPThzMEO3OS=>
CW9019 NU[wXmpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrvbXk4OiCq NYWyU4N{UUN3ME25PVEzKG6P NEG2OmkzPThzMEO3OS=>
Rh5 NXG1VYdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PXRVczKGh? M1PIemlEPTExvK6xNFAxOCCwTR?= MUSyOVgyODN5NR?=
Rh30 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\VfFczKGh? NHW1S2xKSzVy78{eNVAxODBibl2= NFjke2ozPThzMEO3OS=>
778 M1\XNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW2UZY4OiCq M{nXNolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M4fhc|I2ODJ6NE[5
449 NE\kNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\0O|IhcA>? Mn3MbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFL2NGYzPTB{OES2PS=>
LP3 M3uydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV65cWlPPzJiaB?= M1nzb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mof1NlUxOjh2Nkm=
LP6 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDiO|IhcA>? NFf1N3ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MYiyOVAzQDR4OR?=
LP8 NWDPZY85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml25O|IhcA>? MlPjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFrLRpEzPTB{OES2PS=>
LPS141 NWS1[nBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3GO|IhcA>? MUXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGWzfJQzPTB{OES2PS=>
778 MkTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITZ[VQ{NjN|IN88US=> MonVNlQhcA>? M4q3PIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NEe2ZnQzPTB{OES2PS=>
449 M4jpUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOzMlM{KM7:TR?= NVPXXIRnOjRiaB?= NGXtd3Fl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M3LaeVI2ODJ6NE[5
LP3 NF71d3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nuPFMvOzNizszN Mlr3NlQhcA>? MWLk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NIPlelgzPTB{OES2PS=>
LP6 NVHTXnd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXCN{4{OyEQvF2= MUKyOEBp NXXlPW9V\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MWiyOVAzQDR4OR?=
LP8 NVP5do1tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCzMlM{KM7:TR?= MYSyOEBp NX73UoJj\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M1zmbVI2ODJ6NE[5
LPS141 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTCN{4{OyEQvF2= NIXV[GEzPCCq MUjk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MWWyOVAzQDR4OR?=
IMR5 NHfRXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWyOEBp NVHwbIJKTE2VTx?= MoTrTWM2OD1zMk[gcm0> MY[yOFA1PTF5OR?=
BE2C NEXZWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnINlQhcA>? NXGycpF[TE2VTx?= MULJR|UxRTF|NDDuUS=> NI\KZ2ozPDB2NUG3PS=>
1643 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfvRpQ2OjRiaB?= NI\1UmZFVVOR M4TUXmlEPTB;MUS3JI5O MXOyOFA1PTF5OR?=
SKNSH Mm\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;EfpR[OjRiaB?= Mnq5SG1UVw>? M2D4PGlEPTB;MUS4JI5O NXHTWlZyOjRyNEWxO|k>
SY5Y M2HFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILTcpQzPCCq NFvk[IVFVVOR MljxTWM2OD1zNUSgcm0> NXTpWpJnOjRyNEWxO|k>
NGP M37SNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3yT4UzPCCq NHTMNJJFVVOR MUHJR|UxRTF5NTDuUS=> MXeyOFA1PTF5OR?=
KELLY MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH5RoxkOjRiaB?= NFz4c3BFVVOR MWTJR|UxRTJ{MDDuUS=> MWeyOFA1PTF5OR?=
CHP134 NYC0WlNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTiR3RWOjRiaB?= NVqyc|N{TE2VTx?= MUTJR|UxRTJ5MzDuUS=> NGD1epczPDB2NUG3PS=>
NLF Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnPNlQhcA>? NGq3O5VFVVOR M4XTN2lEPTB;M{K4JI5O NWizdFFnOjRyNEWxO|k>
LAN5 NELldVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDiNlQhcA>? M3P4OGROW09? M{\yT2lEPTB;NEK5JI5O M1;SeVI1ODR3MUe5
NB69 M1XsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;LUlI1KGh? NEnVO4pFVVOR NUi3b4Z5UUN3ME23N|ghdk1? NGHDNpYzPDB2NUG3PS=>
SKNDZ NXLCdFZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTDNlQhcA>? NH7nc3VFVVOR MmLpTWM2OD16MEGgcm0> MUGyOFA1PTF5OR?=
NBSD MlvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[yOEBp MlfRSG1UVw>? MlHlTWM2OD1zOUCwJI5O NFrNN3AzPDB2NUG3PS=>
SKNF1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOyOEBp M1z2cmROW09? MmXSTWM2OD1|NUCwJI5O NIjrSHIzPDB2NUG3PS=>
EBC1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPOfox7OjRiaB?= MYLEUXNQ NVjpeoxLUUN3ME22OFAxKG6P MWGyOFA1PTF5OR?=
SKNAS NXzuWodST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXy3RYx7OjRiaB?= M2O5cWROW09? MW\JR|Ux97zgMUCwNFAhdk1? NITBXnczPDB2NUG3PS=>
NB16 Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zUNFI1KGh? Ml3kSG1UVw>? NVLYVlN4UUN3MP-8olExODByIH7N NH\nO5UzPDB2NUG3PS=>
RPE1 NVjhXHdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvyPZhPOjRiaB?= M{\zbWROW09? NFPRcJZKSzVy78{eNVAxODBibl2= MoTXNlQxPDVzN{m=

... 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