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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2 Customer Reviews

  • (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 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfTXIkzPCCq NHXwWGxIUTVyPUK3OkBvVQ>? NUG2WGQxOjV6NUKwOVg>
Myoblast NFTCNpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7LTFA4OiCq NGj4OmRKSzVyPUGwN|Uhdk1? MWeyOVgyODN5NR?=
IMRS MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH0PXU4OiCq MUXJR|UxRTh5MzDuUS=> NVyyfoZQOjV6MUCzO|U>
SKNAS MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVK3NkBp M2TpV2lEPTExvK6xNFAxOCCwTR?= NH2wfI8zPThzMEO3OS=>
Rh28 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLweIJQPzJiaB?= MWrJR|UxRTh2NTDuUS=> MX:yOVgyODN5NR?=
Rh41 NYfSe4tqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vSVlczKGh? NHK4R2xKSzVyPUexPFchdk1? Mnu1NlU5OTB|N{W=
CW9019 NUnQOFZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnMbmxuPzJiaB?= NE\ZcVNKSzVyPUm5NVIhdk1? M1\XTFI2QDFyM{e1
Rh5 M1fiNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3joTFczKGh? M1rucWlEPTExvK6xNFAxOCCwTR?= NIfwSoczPThzMEO3OS=>
Rh30 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS4Rll{PzJiaB?= NYTpdVMyUUN3MP-8olExODByIH7N NGDzR5EzPThzMEO3OS=>
778 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HjcVczKGh? MkS5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyOVAzQDR4OR?=
449 Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETnVJA4OiCq MkLHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MlXHNlUxOjh2Nkm=
LP3 NX;5N2poT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HKeFczKGh? Mo\5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUGyOVAzQDR4OR?=
LP6 NFnnUodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW5O|IhcA>? MYjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGLUUYYzPTB{OES2PS=>
LP8 M1rpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;YO|IhcA>? NHLEU5lqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWT3NlNkOjVyMki0Olk>
LPS141 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHsO|IhcA>? M3LRbolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MYqyOVAzQDR4OR?=
778 M3TEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PaV|MvOzNizszN M1zSOVI1KGh? NGjIRWll\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NISyUW0zPTB{OES2PS=>
449 M33PbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrxU4ZMOy5|MzFOwG0> M4\LSVI1KGh? NWf6T4lD\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M4fJdlI2ODJ6NE[5
LP3 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLNN{4{OyEQvF2= M1LZZlI1KGh? MknN[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M2rYdlI2ODJ6NE[5
LP6 M3;nR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf0fIxXOy5|MzFOwG0> M4fXPVI1KGh? M{fwfYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NYTmNldIOjVyMki0Olk>
LP8 NVryU4VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCzMlM{KM7:TR?= NIHNXlIzPCCq MXrk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NXrSXnc6OjVyMki0Olk>
LPS141 NWDqTVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOzMlM{KM7:TR?= Mo\uNlQhcA>? M{CyR4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M2H4XFI2ODJ6NE[5
IMR5 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWyOEBp MULEUXNQ MWHJR|UxRTF{NjDuUS=> M4LTd|I1ODR3MUe5
BE2C M2npO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInhNnIzPCCq MlPNSG1UVw>? MXnJR|UxRTF|NDDuUS=> MWiyOFA1PTF5OR?=
1643 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrseYZOOjRiaB?= NGXpXGlFVVOR MnzrTWM2OD1zNEegcm0> NYPteZBDOjRyNEWxO|k>
SKNSH NEHQTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P0RlI1KGh? MXzEUXNQ M3TuOGlEPTB;MUS4JI5O M{PiclI1ODR3MUe5
SY5Y NYjmUJRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml23NlQhcA>? M4TnZWROW09? M1Szc2lEPTB;MUW0JI5O M4HMNFI1ODR3MUe5
NGP MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTYNlQhcA>? MVHEUXNQ MoXpTWM2OD1zN{Wgcm0> NFLsUFgzPDB2NUG3PS=>
KELLY M2XNWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmyOEBp NFXofXhFVVOR MVLJR|UxRTJ{MDDuUS=> NVnEVWF4OjRyNEWxO|k>
CHP134 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P1R|I1KGh? NEXKWVFFVVOR NG\NeWJKSzVyPUK3N{BvVQ>? NGTFdHgzPDB2NUG3PS=>
NLF NFjQZnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K4NVI1KGh? MmnVSG1UVw>? MXTJR|UxRTN{ODDuUS=> MYWyOFA1PTF5OR?=
LAN5 MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjnXopsOjRiaB?= MYrEUXNQ MXvJR|UxRTR{OTDuUS=> MVKyOFA1PTF5OR?=
NB69 NFXRPG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ONlQhcA>? MUPEUXNQ MXLJR|UxRTd|ODDuUS=> Mm\INlQxPDVzN{m=
SKNDZ NWHsfppjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\3[oxZOjRiaB?= Mn:0SG1UVw>? Mo\NTWM2OD16MEGgcm0> NIrifYczPDB2NUG3PS=>
NBSD NGLBfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfkc4lsOjRiaB?= NHniOGZFVVOR MlPPTWM2OD1zOUCwJI5O MVeyOFA1PTF5OR?=
SKNF1 NUS1WWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHyNlQhcA>? NFHMSW9FVVOR MmfCTWM2OD1|NUCwJI5O MlX3NlQxPDVzN{m=
EBC1 NVrTWHByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nEbFI1KGh? NHPCZWFFVVOR NGixfpFKSzVyPU[0NFAhdk1? M1O5[FI1ODR3MUe5
SKNAS NWT4eHhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXyyOEBp MlnJSG1UVw>? M2rsS2lEPTExvK6xNFAxOCCwTR?= MWqyOFA1PTF5OR?=
NB16 M2flZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofUNlQhcA>? M{\zTmROW09? M4jFfWlEPTExvK6xNFAxOCCwTR?= Mk\DNlQxPDVzN{m=
RPE1 Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDVNlQhcA>? MYLEUXNQ NFnwNlZKSzVy78{eNVAxODBibl2= Mme4NlQxPDVzN{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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:

* 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