Ribociclib (LEE011)

Catalog No.S7440

Ribociclib (LEE011) Chemical Structure

Molecular Weight(MW): 434.54

1 Customer Review

  • (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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M1nOUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D4O|I1KGh? MnrtS2k2OD1{N{[gcm0> NGjF[okzPTh3MkC1PC=>
Myoblast MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rSZ|czKGh? MXnJR|UxRTFyM{Wgcm0> NXzDeGxpOjV6MUCzO|U>
IMRS Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3xZ484OiCq NVvUdYROUUN3ME24O|Mhdk1? M2rOTFI2QDFyM{e1
SKNAS NUnPZ5R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInXTGw4OiCq NEPi[FFKSzVy78{eNVAxODBibl2= NYXmUWhKOjV6MUCzO|U>
Rh28 M3e4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIWyZZM4OiCq NH\TTIRKSzVyPUi0OUBvVQ>? NGHxd2szPThzMEO3OS=>
Rh41 NGrHfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe3NkBp MWPJR|UxRTdzOEegcm0> MXiyOVgyODN5NR?=
CW9019 NWW4TGZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzXZYU4PzJiaB?= MVPJR|UxRTl7MUKgcm0> NGDpUnkzPThzMEO3OS=>
Rh5 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHEO|IhcA>? M{P5ZmlEPTExvK6xNFAxOCCwTR?= MUmyOVgyODN5NR?=
Rh30 NWm5VHVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXq3NkBp NVjOT4lKUUN3MP-8olExODByIH7N NVL6WZhTOjV6MUCzO|U>
778 M2LDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHZO|IhcA>? MWjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MoqzNlUxOjh2Nkm=
449 NGjMUZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[zR3NTPzJiaB?= MVjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWjrOYFiOjVyMki0Olk>
LP3 M1r4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrrO|IhcA>? M1nweIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MUCyOVAzQDR4OR?=
LP6 NUD0[JhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PEVlczKGh? MoHJbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MViyOVAzQDR4OR?=
LP8 NH3JS5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmyUGI4OiCq MYHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NEHubIIzPTB{OES2PS=>
LPS141 NGCyfYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[3NkBp NUTNUJJDcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NF\jeZUzPTB{OES2PS=>
778 NGftbpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSzMlM{KM7:TR?= MoT1NlQhcA>? MV;k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NW\NUVJoOjVyMki0Olk>
449 MnvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX3eoVJOy5|MzFOwG0> NEP4WoYzPCCq MXrk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NWLCVIZ5OjVyMki0Olk>
LP3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHTXolPOy5|MzFOwG0> M37Md|I1KGh? NUnLeJJO\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MmfLNlUxOjh2Nkm=
LP6 NFXRWm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfYZWxbOy5|MzFOwG0> MWGyOEBp M4C1OoRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MWiyOVAzQDR4OR?=
LP8 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTIfIx7Oy5|MzFOwG0> M37rbVI1KGh? MV\k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= Ml:yNlUxOjh2Nkm=
LPS141 NUO0WXBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH3V|Q{NjN|IN88US=> MkXzNlQhcA>? NFHERYpl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MY[yOVAzQDR4OR?=
IMR5 NGTqZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWzNlQhcA>? NFPmenJFVVOR MmLKTWM2OD1zMk[gcm0> Mnj6NlQxPDVzN{m=
BE2C MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nQTFI1KGh? M1\vOmROW09? NHnkfXdKSzVyPUGzOEBvVQ>? M4TlSVI1ODR3MUe5
1643 NUTQSJFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnnZpk2OjRiaB?= NYXkXI5jTE2VTx?= NEfudXZKSzVyPUG0O{BvVQ>? NGTxZ24zPDB2NUG3PS=>
SKNSH MmTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fuWFI1KGh? M4nhZ2ROW09? M1nV[2lEPTB;MUS4JI5O MmrZNlQxPDVzN{m=
SY5Y Moe3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXWNlQhcA>? M2PVO2ROW09? Mmj5TWM2OD1zNUSgcm0> M2O0d|I1ODR3MUe5
NGP M1zjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWyOEBp NVfLWY9pTE2VTx?= NYK4OGlwUUN3ME2xO|Uhdk1? MkmyNlQxPDVzN{m=
KELLY NVLL[4xvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzkfFVjOjRiaB?= MUXEUXNQ M4nHPWlEPTB;MkKwJI5O NIPCUpMzPDB2NUG3PS=>
CHP134 M2Kzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XSO|I1KGh? MYfEUXNQ M3GwWWlEPTB;MkezJI5O M2LzOVI1ODR3MUe5
NLF NWDjUoxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf3WXozPCCq MV7EUXNQ MX3JR|UxRTN{ODDuUS=> NEfIS|AzPDB2NUG3PS=>
LAN5 M{\W[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[wWVI1KGh? M3OzbGROW09? M1XUbmlEPTB;NEK5JI5O NX\PWmVvOjRyNEWxO|k>
NB69 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPTNHpROjRiaB?= MV3EUXNQ M1\vfGlEPTB;N{O4JI5O NIC2XlUzPDB2NUG3PS=>
SKNDZ M3jROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKyOEBp MlHmSG1UVw>? Mm\0TWM2OD16MEGgcm0> NUjTW4t1OjRyNEWxO|k>
NBSD M1\Cc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;ZdW4zPCCq NHHMblFFVVOR NUH2XWFHUUN3ME2xPVAxKG6P M{nsSFI1ODR3MUe5
SKNF1 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X2XlI1KGh? M2D0RWROW09? NYDVVGdSUUN3ME2zOVAxKG6P MUiyOFA1PTF5OR?=
EBC1 MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXeyOEBp MnuwSG1UVw>? M4LlZWlEPTB;NkSwNEBvVQ>? NFvU[I4zPDB2NUG3PS=>
SKNAS M{Txe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\jNlQhcA>? MnO2SG1UVw>? NYnIXno3UUN3MP-8olExODByIH7N NFLtVGwzPDB2NUG3PS=>
NB16 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7nTVAxOjRiaB?= Mm\aSG1UVw>? MUDJR|Ux97zgMUCwNFAhdk1? M4TkelI1ODR3MUe5
RPE1 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XoOlI1KGh? NFq4ZY1FVVOR NYfESXd3UUN3MP-8olExODByIH7N M2DNOVI1ODR3MUe5

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID