Ribociclib (LEE011)

For research use only.

Catalog No.S7440

39 publications

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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Selleck's Ribociclib (LEE011) has been cited by 39 publications

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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 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\5T3U6OjRiaB?= MWPHTVUxRTJ5NjDuUS=> NE\qV5AzPTh3MkC1PC=>
Myoblast NILCRWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnHO|IhcA>? M4PtbmlEPTB;MUCzOUBvVQ>? M{DpRVI2QDFyM{e1
IMRS NEexO|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jiPVczKGh? MULJR|UxRTh5MzDuUS=> MYCyOVgyODN5NR?=
SKNAS NVm2S5R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTzO|IhcA>? NWLDTGxQUUN3MP-8olExODByIH7N NX63NpNTOjV6MUCzO|U>
Rh28 M3rK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX1VHQ4OiCq M1vSW2lEPTB;OES1JI5O M3vYVFI2QDFyM{e1
Rh41 NXvoXYViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPQO|IhcA>? MnjNTWM2OD15MUi3JI5O NF7xdm0zPThzMEO3OS=>
CW9019 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPKO|IhcA>? NXTERpk5UUN3ME25PVEzKG6P NYrOUFZPOjV6MUCzO|U>
Rh5 MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVG3NkBp M4[5[WlEPTExvK6xNFAxOCCwTR?= NGPUe|IzPThzMEO3OS=>
Rh30 NF60UWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P4TFczKGh? MoO3TWM2OO,:nkGwNFAxKG6P MnfCNlU5OTB|N{W=
778 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXrV4xlPzJiaB?= M1vPTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NXznSZVZOjVyMki0Olk>
449 M3zlbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmwepdKPzJiaB?= NEjm[pZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NHvqOIUzPTB{OES2PS=>
LP3 M33JR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXGOFFqPzJiaB?= M3v4TYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWrreYs6OjVyMki0Olk>
LP6 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PDeVczKGh? M3y1NYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXSyOVAzQDR4OR?=
LP8 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\rTo44OiCq NVz0e|JUcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NWrvWYhnOjVyMki0Olk>
LPS141 NHHvNm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfGO|IhcA>? NVvqelc{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M4Dje|I2ODJ6NE[5
778 NHvMdotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nINlMvOzNizszN NFf0dJMzPCCq M3rzNIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NXf5R4RXOjVyMki0Olk>
449 NID4fVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqzMlM{KM7:TR?= MYeyOEBp NEOxVpBl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NGnFdJYzPTB{OES2PS=>
LP3 NX7jOGE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDLenE1Oy5|MzFOwG0> NGjmcHozPCCq NI\KdGll\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MnXSNlUxOjh2Nkm=
LP6 NIXT[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGzMlM{KM7:TR?= MXKyOEBp MVjk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MmG2NlUxOjh2Nkm=
LP8 MlPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqzMlM{KM7:TR?= NGLtSlYzPCCq NHvIWldl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MUiyOVAzQDR4OR?=
LPS141 M4jCS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\GN{4{OyEQvF2= M3q1WlI1KGh? MYPk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NEfB[4IzPTB{OES2PS=>
IMR5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS0NlQhcA>? M{XHdGROW09? Ml31TWM2OD1zMk[gcm0> MVOyOFA1PTF5OR?=
BE2C NHL3dpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W3blI1KGh? MYLEUXNQ MVrJR|UxRTF|NDDuUS=> NVrzTYxYOjRyNEWxO|k>
1643 M1XXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHCeG4zPCCq MoLpSG1UVw>? MWXJR|UxRTF2NzDuUS=> MXuyOFA1PTF5OR?=
SKNSH NH\wdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWiyOEBp NFLIbldFVVOR Ml3BTWM2OD1zNEigcm0> M{XMPFI1ODR3MUe5
SY5Y NUKwOGZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuyOEBp M2jSXmROW09? NVO1T|ViUUN3ME2xOVQhdk1? NVT6fnQ2OjRyNEWxO|k>
NGP M17NbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nHU|I1KGh? MkTlSG1UVw>? NYDTRWhrUUN3ME2xO|Uhdk1? MYKyOFA1PTF5OR?=
KELLY MnLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKyOEBp MnjTSG1UVw>? M2LWc2lEPTB;MkKwJI5O NWjRWWNiOjRyNEWxO|k>
CHP134 M{nHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\5O|I1KGh? M4fod2ROW09? M36xN2lEPTB;MkezJI5O M4DzclI1ODR3MUe5
NLF M373RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[yOEBp MYnEUXNQ MnruTWM2OD1|Mkigcm0> MX:yOFA1PTF5OR?=
LAN5 Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4CzfFI1KGh? MkHrSG1UVw>? NEXQTm5KSzVyPUSyPUBvVQ>? MoHQNlQxPDVzN{m=
NB69 M{LWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DCeFI1KGh? Mmj2SG1UVw>? Ml\WTWM2OD15M{igcm0> MmPCNlQxPDVzN{m=
SKNDZ MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL3eWozPCCq NWroNowxTE2VTx?= NYP5cpViUUN3ME24NFEhdk1? MkD5NlQxPDVzN{m=
NBSD MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWwenczPCCq NFv6PYNFVVOR MYfJR|UxRTF7MECgcm0> M2fieFI1ODR3MUe5
SKNF1 MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\DRotYOjRiaB?= M1\nbmROW09? MYnJR|UxRTN3MECgcm0> M1zKSFI1ODR3MUe5
EBC1 NUWzNoh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknKNlQhcA>? M1e4UGROW09? MmXCTWM2OD14NECwJI5O M1rTR|I1ODR3MUe5
SKNAS NYrv[|dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[5WpE2OjRiaB?= NVP1T25YTE2VTx?= NU\SVWJ1UUN3MP-8olExODByIH7N NF\CUngzPDB2NUG3PS=>
NB16 NGPyflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O0SFI1KGh? NXP1eY5oTE2VTx?= M4\HUmlEPTExvK6xNFAxOCCwTR?= NWTzUGFwOjRyNEWxO|k>
RPE1 NVm2bWk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7rNlQhcA>? NUP5O|BkTE2VTx?= M3WzbGlEPTExvK6xNFAxOCCwTR?= M1u2dVI1ODR3MUe5

... 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(NC3=NC=C(C=C3)N4CCNCC4)N=C2[N]1C5CCCC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04315233 Not yet recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma August 2020 Phase 1
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
NCT03701334 Recruiting Drug: Ribociclib|Other: Endocrine Therapy Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3
NCT03613220 Recruiting Drug: ribociclib|Drug: letrozole HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis December 28 2018 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID