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 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnXWHJHOjRiaB?= M1rpdmdKPTB;Mke2JI5O NFixelAzPTh3MkC1PC=>
Myoblast M33EWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jSSFczKGh? MWXJR|UxRTFyM{Wgcm0> NGP6bYUzPThzMEO3OS=>
IMRS MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSxUZU4OiCq MnnOTWM2OD16N{Ogcm0> MmTnNlU5OTB|N{W=
SKNAS MkTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn3e4E4OiCq MnzzTWM2OO,:nkGwNFAxKG6P MXWyOVgyODN5NR?=
Rh28 NVzwRXg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XnZVczKGh? Ml;oTWM2OD16NEWgcm0> MYmyOVgyODN5NR?=
Rh41 NH3YfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXJO|IhcA>? M4PYdGlEPTB;N{G4O{BvVQ>? MXOyOVgyODN5NR?=
CW9019 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVO3NkBp MUHJR|UxRTl7MUKgcm0> M13MdFI2QDFyM{e1
Rh5 MlXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWC3NkBp NUjiWWxQUUN3MP-8olExODByIH7N MkDKNlU5OTB|N{W=
Rh30 M1zNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUe3NkBp MljNTWM2OO,:nkGwNFAxKG6P M3jJfFI2QDFyM{e1
778 NH31NIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nDeFczKGh? Ml\DbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIjRdlQzPTB{OES2PS=>
449 M2r6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm3NkBp M4W4VolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M1jTfFI2ODJ6NE[5
LP3 M3n3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNWFczKGh? NW\udGVjcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NIHENWMzPTB{OES2PS=>
LP6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO3NkBp M4PzZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NXTxNlV{OjVyMki0Olk>
LP8 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHmOI04OiCq MmT1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIrUdVQzPTB{OES2PS=>
LPS141 NIHQRXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG0TFk4OiCq MoTpbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1rR[FI2ODJ6NE[5
778 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17k[VMvOzNizszN M3HlS|I1KGh? MorH[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M4\0SVI2ODJ6NE[5
449 NIXhPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTiT|k5Oy5|MzFOwG0> MWqyOEBp NGPYWI5l\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MUKyOVAzQDR4OR?=
LP3 NWXQUXA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3i4VVMvOzNizszN NXLzcIM6OjRiaB?= NWrXNGxU\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M2H6RlI2ODJ6NE[5
LP6 NF;IUphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS5N{4{OyEQvF2= NIrTNoQzPCCq MYHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M2DJfVI2ODJ6NE[5
LP8 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWzMlM{KM7:TR?= NVvK[WQzOjRiaB?= NVTwcWd3\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MW[yOVAzQDR4OR?=
LPS141 MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XrZlMvOzNizszN Mlv0NlQhcA>? NHqx[|Zl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NFPLRo0zPTB{OES2PS=>
IMR5 NHv1OppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViyOEBp NIHJNINFVVOR MVPJR|UxRTF{NjDuUS=> MkTNNlQxPDVzN{m=
BE2C M4T3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\WNpQzPCCq MlK5SG1UVw>? M{HO[WlEPTB;MUO0JI5O MXiyOFA1PTF5OR?=
1643 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;IN2gzPCCq NFXoPFlFVVOR NFvXT49KSzVyPUG0O{BvVQ>? MlOzNlQxPDVzN{m=
SKNSH M{\3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3OUJE2OjRiaB?= NULhbHg3TE2VTx?= MlnvTWM2OD1zNEigcm0> M2nOS|I1ODR3MUe5
SY5Y NGP1[4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\vNlQhcA>? M4PSPWROW09? M1PDcmlEPTB;MUW0JI5O NI\2W5ozPDB2NUG3PS=>
NGP MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2yOEBp MmfWSG1UVw>? M1XFXGlEPTB;MUe1JI5O NXqz[FFoOjRyNEWxO|k>
KELLY NHfLWXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{KyUVI1KGh? MYjEUXNQ NFX4U|JKSzVyPUKyNEBvVQ>? MWCyOFA1PTF5OR?=
CHP134 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSyOEBp NHnNSpNFVVOR NWTWPVdHUUN3ME2yO|Mhdk1? MUOyOFA1PTF5OR?=
NLF MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPYeJQzPCCq MV;EUXNQ MXXJR|UxRTN{ODDuUS=> NVuzOlJDOjRyNEWxO|k>
LAN5 MofJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfHNlQhcA>? NXrBZXNuTE2VTx?= MXPJR|UxRTR{OTDuUS=> M3Xt[VI1ODR3MUe5
NB69 NWjISW9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[1PVI1KGh? MnvvSG1UVw>? M2\tT2lEPTB;N{O4JI5O NYTpdY9lOjRyNEWxO|k>
SKNDZ Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zHVlI1KGh? NICwZldFVVOR NVrGfWxQUUN3ME24NFEhdk1? Mnn6NlQxPDVzN{m=
NBSD MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2yOEBp MXjEUXNQ NHrmNo5KSzVyPUG5NFAhdk1? Mo[5NlQxPDVzN{m=
SKNF1 NVjLW5hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyNlQhcA>? NYriUGdyTE2VTx?= MUHJR|UxRTN3MECgcm0> M2j1dVI1ODR3MUe5
EBC1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HkWVI1KGh? NFewc2FFVVOR MmjpTWM2OD14NECwJI5O M2r5fVI1ODR3MUe5
SKNAS M1T4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKyOEBp NWrH[pp7TE2VTx?= Mn\wTWM2OO,:nkGwNFAxKG6P NXXhTYVsOjRyNEWxO|k>
NB16 M{HhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\5SlI1KGh? M4O1O2ROW09? MkXNTWM2OO,:nkGwNFAxKG6P M1zQWVI1ODR3MUe5
RPE1 NHy2ZZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\DNVI1KGh? MkS5SG1UVw>? MnO2TWM2OO,:nkGwNFAxKG6P Mn3hNlQxPDVzN{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
NCT02941926 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis November 30, 2016 Phase 3
NCT02388620 Completed Normal Hepatic Function|Impaired Hepatic Function Novartis Pharmaceuticals|Novartis March 25, 2015 Phase 1
NCT01872260 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 22, 2013 Phase 1
NCT01237236 Active, not recruiting Advanced Solid Tumor|Lymphomas Novartis Pharmaceuticals|Novartis December 21, 2010 Phase 1
NCT03008408 Not yet recruiting Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma M.D. Anderson Cancer Center|Novartis April 2017 Phase 2
NCT02754011 Recruiting Breast Cancer UNICANCER|Novartis January 2017 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID