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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3 Customer Reviews

  • 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.

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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 NIHvWodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH3NlQhcA>? NEPC[XdIUTVyPUK3OkBvVQ>? MmSzNlU5PTJyNUi=
Myoblast M{DIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy3NkBp MVvJR|UxRTFyM{Wgcm0> NIT0eXUzPThzMEO3OS=>
IMRS NULrdWNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXaO|IhcA>? MWjJR|UxRTh5MzDuUS=> NEC4T2czPThzMEO3OS=>
SKNAS M4Pmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TsT|czKGh? MU\JR|Ux97zgMUCwNFAhdk1? NIDmfJkzPThzMEO3OS=>
Rh28 NXXQTm5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS3O|IhcA>? M1i2TWlEPTB;OES1JI5O NVrLe4hMOjV6MUCzO|U>
Rh41 MlPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnaZXRsPzJiaB?= MWXJR|UxRTdzOEegcm0> NYn1Wmd7OjV6MUCzO|U>
CW9019 M{XNNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\T[FczKGh? NFP4PVlKSzVyPUm5NVIhdk1? NFvhNoQzPThzMEO3OS=>
Rh5 NUPJXm9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TRZ|czKGh? MYjJR|Ux97zgMUCwNFAhdk1? NGr1fYUzPThzMEO3OS=>
Rh30 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ReZFqPzJiaB?= M2HTR2lEPTExvK6xNFAxOCCwTR?= MVmyOVgyODN5NR?=
778 NIDwZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\FPYdGPzJiaB?= M4niUIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M4\jNVI2ODJ6NE[5
449 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUS3NkBp M1z1W4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NVPNXWt4OjVyMki0Olk>
LP3 M3HWW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm3NkBp NEjEWG1qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MYGyOVAzQDR4OR?=
LP6 NHTXRnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTsXGZ7PzJiaB?= NHLnOXlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M4C0dlI2ODJ6NE[5
LP8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLZO|IhcA>? MYXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MkPpNlUxOjh2Nkm=
LPS141 NHjMTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fUXFczKGh? M2mxN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXOyOVAzQDR4OR?=
778 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmzMlM{KM7:TR?= MmrUNlQhcA>? MnTZ[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M{GyO|I2ODJ6NE[5
449 NIHQWpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSzMlM{KM7:TR?= M{\udFI1KGh? NWDQWmkx\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MnGxNlUxOjh2Nkm=
LP3 NEXZdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrtN{4{OyEQvF2= Mmj5NlQhcA>? MkHF[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NHrxUXkzPTB{OES2PS=>
LP6 MkfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkX1N{4{OyEQvF2= NXv0VXdWOjRiaB?= NU\r[m9i\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NVXXeHNtOjVyMki0Olk>
LP8 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[zMlM{KM7:TR?= Mn7lNlQhcA>? NGrDNmdl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NVPrbnJOOjVyMki0Olk>
LPS141 NWO2fop6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\1N{4{OyEQvF2= M1vrc|I1KGh? MVPk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MUeyOVAzQDR4OR?=
IMR5 NVnQN452T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLWNlQhcA>? Mn;lSG1UVw>? MmPtTWM2OD1zMk[gcm0> MW[yOFA1PTF5OR?=
BE2C MkPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXnNlQhcA>? Mn3GSG1UVw>? NWrlNHhnUUN3ME2xN|Qhdk1? MnHrNlQxPDVzN{m=
1643 NVv1dmxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP6R5VYOjRiaB?= MVnEUXNQ NWCzPYgxUUN3ME2xOFchdk1? NX61[2JUOjRyNEWxO|k>
SKNSH NYXOdGV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOyOEBp M2HGdGROW09? NWTZdHZpUUN3ME2xOFghdk1? MVuyOFA1PTF5OR?=
SY5Y MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DUS|I1KGh? MWLEUXNQ M4TKT2lEPTB;MUW0JI5O MljoNlQxPDVzN{m=
NGP MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqyOEBp M3zHNmROW09? MULJR|UxRTF5NTDuUS=> MX6yOFA1PTF5OR?=
KELLY NHP1VFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvheXhwOjRiaB?= NH3SSGhFVVOR NYHYWIg2UUN3ME2yNlAhdk1? MV6yOFA1PTF5OR?=
CHP134 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWOyOEBp MYjEUXNQ Mnn1TWM2OD1{N{Ogcm0> MWOyOFA1PTF5OR?=
NLF MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiyOEBp M{LLS2ROW09? NEPWPGtKSzVyPUOyPEBvVQ>? NIL6RXAzPDB2NUG3PS=>
LAN5 NELp[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS1NlQhcA>? MV7EUXNQ NHHXWVlKSzVyPUSyPUBvVQ>? M3TEeVI1ODR3MUe5
NB69 NUS5dlJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz4S2RpOjRiaB?= NW[ye3dETE2VTx?= M3HUO2lEPTB;N{O4JI5O M1rhOFI1ODR3MUe5
SKNDZ NFzBUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULldFBmOjRiaB?= NWHJR3NWTE2VTx?= NFrUOWhKSzVyPUiwNUBvVQ>? MXSyOFA1PTF5OR?=
NBSD NUT5OlVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:yOEBp NXXYWph3TE2VTx?= MWXJR|UxRTF7MECgcm0> NFjSWVAzPDB2NUG3PS=>
SKNF1 M1LsWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTYOZIzPCCq NXLQc5F{TE2VTx?= MUjJR|UxRTN3MECgcm0> NF7KXoszPDB2NUG3PS=>
EBC1 NGHFU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfWWlkzPCCq MnzJSG1UVw>? NHHQZoZKSzVyPU[0NFAhdk1? MkXGNlQxPDVzN{m=
SKNAS MlTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[yOEBp M{LUZmROW09? NH7tOYNKSzVy78{eNVAxODBibl2= M1fvZlI1ODR3MUe5
NB16 NUfRdWdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfIVZkzPCCq NXTyXlgyTE2VTx?= NV6xWo9nUUN3MP-8olExODByIH7N MnHwNlQxPDVzN{m=
RPE1 M3iyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDZNlQhcA>? M{HwV2ROW09? MmX6TWM2OO,:nkGwNFAxKG6P MYCyOFA1PTF5OR?=

... 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