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. 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 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnHNlQhcA>? MlLRS2k2OD1{N{[gcm0> NH;GT2gzPTh3MkC1PC=>
Myoblast MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfseY84OiCq NVn0[IZxUUN3ME2xNFM2KG6P M{LOe|I2QDFyM{e1
IMRS MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;zXWVmPzJiaB?= MVfJR|UxRTh5MzDuUS=> MofRNlU5OTB|N{W=
SKNAS NUj3OHh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYC3NkBp NF;HZZBKSzVy78{eNVAxODBibl2= MUOyOVgyODN5NR?=
Rh28 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWG3NkBp NFfpc|hKSzVyPUi0OUBvVQ>? NFvnO4czPThzMEO3OS=>
Rh41 NFfRbJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFS0d4M4OiCq NFvwcIxKSzVyPUexPFchdk1? NYLEWZhEOjV6MUCzO|U>
CW9019 NV;IN2Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvtVYg{PzJiaB?= NETSfW1KSzVyPUm5NVIhdk1? NY\pVYFXOjV6MUCzO|U>
Rh5 NFXS[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\QWlczKGh? MojVTWM2OO,:nkGwNFAxKG6P NXvJeo9pOjV6MUCzO|U>
Rh30 M{TmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjnO|IhcA>? NVzQcIZrUUN3MP-8olExODByIH7N NXjT[nFrOjV6MUCzO|U>
778 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\TO|IhcA>? NV;IUWZHcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYHqclNJOjVyMki0Olk>
449 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkK2O|IhcA>? NXfnZ2REcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MlXaNlUxOjh2Nkm=
LP3 NW[4RXpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3IO|IhcA>? NXy2WndocW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NGrpOXgzPTB{OES2PS=>
LP6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW3WmI4OiCq NH7iOopqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M2\u[VI2ODJ6NE[5
LP8 M3XpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:3NkBp M2CweolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MnflNlUxOjh2Nkm=
LPS141 NFLHcXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fSc|czKGh? NIfNdFVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NEO0N|kzPTB{OES2PS=>
778 NV6xO41oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HRUlMvOzNizszN NYjpflM{OjRiaB?= MXnk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NFL3UGQzPTB{OES2PS=>
449 MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvwc3BOOy5|MzFOwG0> NVvsRmVSOjRiaB?= MVTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NUHnb3FYOjVyMki0Olk>
LP3 NIfNfWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TEZVMvOzNizszN NHLtOW0zPCCq NIHqOZVl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NUTU[olDOjVyMki0Olk>
LP6 NVfUR5F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jJ[FMvOzNizszN MmPWNlQhcA>? M{DUUIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MorlNlUxOjh2Nkm=
LP8 M2P5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOzMlM{KM7:TR?= NY[0e5BsOjRiaB?= M1Xre4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MV6yOVAzQDR4OR?=
LPS141 MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnYN{4{OyEQvF2= NIjuVYozPCCq M4LVbIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NIT5enozPTB{OES2PS=>
IMR5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jq[|I1KGh? NHXmWINFVVOR M{jwemlEPTB;MUK2JI5O NYLJbXNPOjRyNEWxO|k>
BE2C M{X3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiyOEBp NYHaWpZ5TE2VTx?= M4TJT2lEPTB;MUO0JI5O MkHoNlQxPDVzN{m=
1643 NXrZRpcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUSze5RNOjRiaB?= NV;ubll2TE2VTx?= M{W0NGlEPTB;MUS3JI5O NV\4NnpoOjRyNEWxO|k>
SKNSH NYjGZ417T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSyOEBp M{PhRWROW09? M4LKPGlEPTB;MUS4JI5O M1HOdlI1ODR3MUe5
SY5Y NHK5NZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSyOEBp MlTlSG1UVw>? NHmxdWNKSzVyPUG1OEBvVQ>? M1\CRlI1ODR3MUe5
NGP NXnSN2tOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSyOEBp NFPBZo9FVVOR NXXaVGF4UUN3ME2xO|Uhdk1? MlXLNlQxPDVzN{m=
KELLY MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOyOEBp MUXEUXNQ Ml\NTWM2OD1{MkCgcm0> MVmyOFA1PTF5OR?=
CHP134 NIjpZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu2NlQhcA>? MVjEUXNQ NGLhWlZKSzVyPUK3N{BvVQ>? Mo\KNlQxPDVzN{m=
NLF MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3hTlNiOjRiaB?= Mly1SG1UVw>? M4\DT2lEPTB;M{K4JI5O NXHsU2piOjRyNEWxO|k>
LAN5 MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\0fnZxOjRiaB?= Mm\PSG1UVw>? NGPWNmVKSzVyPUSyPUBvVQ>? M3;XN|I1ODR3MUe5
NB69 NXTxXVdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO5NolqOjRiaB?= MnW2SG1UVw>? MkjUTWM2OD15M{igcm0> MnzwNlQxPDVzN{m=
SKNDZ NXvvWldwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M130NFI1KGh? MV;EUXNQ M2\3c2lEPTB;OECxJI5O MmrmNlQxPDVzN{m=
NBSD M37iemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe2dZh1OjRiaB?= NHzib2RFVVOR MkDHTWM2OD1zOUCwJI5O M2HXeVI1ODR3MUe5
SKNF1 Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jaVFI1KGh? NUDhO21UTE2VTx?= M2HDUWlEPTB;M{WwNEBvVQ>? M1PVZlI1ODR3MUe5
EBC1 NVGySlhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYeyOEBp NGjTSZhFVVOR NE\OV25KSzVyPU[0NFAhdk1? NGjieG4zPDB2NUG3PS=>
SKNAS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzCPZpvOjRiaB?= M4XOO2ROW09? NWL5UWRYUUN3MP-8olExODByIH7N NYjQNWg6OjRyNEWxO|k>
NB16 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL5c4duOjRiaB?= M{TxOmROW09? MUHJR|Ux97zgMUCwNFAhdk1? NV;OdIlnOjRyNEWxO|k>
RPE1 M1LoNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\RfFI1KGh? Mn3aSG1UVw>? NHXScGlKSzVy78{eNVAxODBibl2= MljNNlQxPDVzN{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
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