Ribociclib (LEE011)

For research use only.

Catalog No.S7440

47 publications

Ribociclib (LEE011) Chemical Structure

CAS No. 1211441-98-3

Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

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Selleck's Ribociclib (LEE011) has been cited by 47 publications

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Biological Activity

Description Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. 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 [2]
(Cell-free assay)
CDK6 [2]
(Cell-free assay)
10 nM 39 nM
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 MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD0doNNOjRiaB?= MWDHTVUxRTJ5NjDuUS=> MVqyOVg2OjB3OB?=
Myoblast NFXSNWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzTfZc4OiCq MVvJR|UxRTFyM{Wgcm0> MVuyOVgyODN5NR?=
IMRS MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon3O|IhcA>? MnXNTWM2OD16N{Ogcm0> M3nkcVI2QDFyM{e1
SKNAS NVTneFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVq3NkBp Mnm0TWM2OO,:nkGwNFAxKG6P NF7YVYczPThzMEO3OS=>
Rh28 M16zS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rjV|czKGh? NXP1VVBxUUN3ME24OFUhdk1? M3XjfFI2QDFyM{e1
Rh41 M2rDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfKXFI2PzJiaB?= M3nyRmlEPTB;N{G4O{BvVQ>? M2PkcFI2QDFyM{e1
CW9019 NXXu[pZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXDXpU4OiCq MkTpTWM2OD17OUGyJI5O MWSyOVgyODN5NR?=
Rh5 NV7yb3NPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf6SlN7PzJiaB?= MoPBTWM2OO,:nkGwNFAxKG6P Mm\4NlU5OTB|N{W=
Rh30 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e3TVczKGh? MoLsTWM2OO,:nkGwNFAxKG6P NEjnZlEzPThzMEO3OS=>
778 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XjN|czKGh? MYnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmnINlUxOjh2Nkm=
449 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLuO|IhcA>? MoHQbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NGjQbVkzPTB{OES2PS=>
LP3 M2nJO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\Mc2M4OiCq NV;1[4d6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MlXJNlUxOjh2Nkm=
LP6 M1r1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37KVVczKGh? MlKzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NXHTNW5jOjVyMki0Olk>
LP8 M1vydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq3NkBp M1PCNolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXeyOVAzQDR4OR?=
LPS141 M37UPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFeyRmY4OiCq NGjVVYVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NXXaZoZ2OjVyMki0Olk>
778 M3;XSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jQVFMvOzNizszN NEW1[|QzPCCq NYf5TWdC\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MonXNlUxOjh2Nkm=
449 NFj3OIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTaRYJ2Oy5|MzFOwG0> MoHjNlQhcA>? M{m3PYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NXrieZl4OjVyMki0Olk>
LP3 NHKyOlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\MN{4{OyEQvF2= MkXUNlQhcA>? MXLk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NXn0eVFsOjVyMki0Olk>
LP6 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHtTnlOOy5|MzFOwG0> NY\VVHNGOjRiaB?= MX\k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MX[yOVAzQDR4OR?=
LP8 M2O0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HIdlMvOzNizszN M2HiXVI1KGh? NYDzNFF7\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NXPlOG1XOjVyMki0Olk>
LPS141 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TXfVMvOzNizszN M3HuTFI1KGh? NYHmflFW\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M4m0eVI2ODJ6NE[5
IMR5 M1:4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKyOEBp M3ztfGROW09? NGDzXlJKSzVyPUGyOkBvVQ>? M3rvXVI1ODR3MUe5
BE2C NX:0UWU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;4UINTOjRiaB?= NGnaSIZFVVOR NWTLVFllUUN3ME2xN|Qhdk1? M2r6PFI1ODR3MUe5
1643 Mn:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW3SlQzPCCq NV\QUpdOTE2VTx?= M3HZU2lEPTB;MUS3JI5O Mk\6NlQxPDVzN{m=
SKNSH MkHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PZVFI1KGh? NV3ueJJpTE2VTx?= M33xeWlEPTB;MUS4JI5O NUnJfopTOjRyNEWxO|k>
SY5Y MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DrPFI1KGh? MYPEUXNQ MXrJR|UxRTF3NDDuUS=> Mn7ZNlQxPDVzN{m=
NGP NIPE[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS2NlQhcA>? NE\yXoxFVVOR NF;xUZVKSzVyPUG3OUBvVQ>? NYXVWHMyOjRyNEWxO|k>
KELLY MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nvT|I1KGh? NUC4XIpPTE2VTx?= NV\NfJBEUUN3ME2yNlAhdk1? MWOyOFA1PTF5OR?=
CHP134 MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzmNlQhcA>? M{KwNWROW09? NWjkR4h{UUN3ME2yO|Mhdk1? Mn;JNlQxPDVzN{m=
NLF NHHPTlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rSVVI1KGh? M3TXcWROW09? NWHC[mNiUUN3ME2zNlghdk1? M{D0SlI1ODR3MUe5
LAN5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPoOIl7OjRiaB?= MUHEUXNQ NIf4Z4xKSzVyPUSyPUBvVQ>? MUeyOFA1PTF5OR?=
NB69 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrJbIJFOjRiaB?= NIXlV|RFVVOR M3rDTWlEPTB;N{O4JI5O NXL2PGJpOjRyNEWxO|k>
SKNDZ NX71NmdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrp[HUzPCCq NI\B[|BFVVOR NHHnNmxKSzVyPUiwNUBvVQ>? NWDXW5p4OjRyNEWxO|k>
NBSD MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\INlQhcA>? MUHEUXNQ M3zpe2lEPTB;MUmwNEBvVQ>? NHHGd5IzPDB2NUG3PS=>
SKNF1 NW\Ve4Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmyOEBp MUPEUXNQ M2T3bWlEPTB;M{WwNEBvVQ>? NY\mXodjOjRyNEWxO|k>
EBC1 M4LUc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTSNlQhcA>? MlzwSG1UVw>? MXvJR|UxRTZ2MECgcm0> MmfoNlQxPDVzN{m=
SKNAS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCyOEBp NWTTR3ZKTE2VTx?= MoT4TWM2OO,:nkGwNFAxKG6P NEezOVgzPDB2NUG3PS=>
NB16 NX7lUVQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT2NlQhcA>? M2C5TmROW09? NIXqSoZKSzVy78{eNVAxODBibl2= NIDDOmYzPDB2NUG3PS=>
RPE1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEntOYczPCCq NUjyVHNjTE2VTx?= MnzyTWM2OO,:nkGwNFAxKG6P MYqyOFA1PTF5OR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP; 

PubMed: 29789630     


Effect of ribociclib on pRB and G1 cell cycle regulating protein expressions in C666-1 and HK1 cells. Cells were treated with ribociclib in 2 concentrations, one of them near their corresponding IC50, for 24 and 48 hours. Phosphorylation of Rb in all cell䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€𢡄⟼෕€䀷痗⟼෕౴⟼෕

29789630
Growth inhibition assay
Cell viability ; 

PubMed: 26390342     


Effects of palbociclib and ribociclib on viability of H157, H2170, H520 and H596 cells after 72 hours of drug treatment and IC50 values for inhibition of cell viability.

26390342
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]

- Collapse
  • 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]

- Collapse
  • Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts.
  • 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
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04657679 Not yet recruiting Drug: Ribociclib Breast Cancer Georgetown University|Medstar Health Research Institute|Breast Cancer Research Foundation|Georgetown-Howard Universities Center for Clinical and Translational Science (GHUCCTS) December 2020 --
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma October 29 2020 Phase 1
NCT04417621 Recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Melanoma Novartis Pharmaceuticals|Novartis October 16 2020 Phase 2
NCT03834740 Recruiting Drug: Ribociclib|Drug: Everolimus Glioblastoma Multiforme|Glioma of Brain St. Joseph''s Hospital and Medical Center Phoenix|Ivy Brain Tumor Center|Barrow Neurological Institute December 21 2018 Early Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID