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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Cited by 28 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 M3TWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLLNlQhcA>? NHzEfZBIUTVyPUK3OkBvVQ>? NH7aSZQzPTh3MkC1PC=>
Myoblast M1PtdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXe3NkBp MYLJR|UxRTFyM{Wgcm0> Mn;yNlU5OTB|N{W=
IMRS NEL5PVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XKdVczKGh? NXvxUmNTUUN3ME24O|Mhdk1? M{TOb|I2QDFyM{e1
SKNAS NVrqRotQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzPO|IhcA>? NYexS3JQUUN3MP-8olExODByIH7N NVHGNWs2OjV6MUCzO|U>
Rh28 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnSNG84OiCq NGLMWmZKSzVyPUi0OUBvVQ>? MVGyOVgyODN5NR?=
Rh41 NU\wPHEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDvNJNjPzJiaB?= M1;t[2lEPTB;N{G4O{BvVQ>? MWOyOVgyODN5NR?=
CW9019 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfGTW9yPzJiaB?= NXHGS25vUUN3ME25PVEzKG6P MUCyOVgyODN5NR?=
Rh5 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX0bZNFPzJiaB?= MoD2TWM2OO,:nkGwNFAxKG6P NXTZfVV7OjV6MUCzO|U>
Rh30 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW5e45[PzJiaB?= NUXReIppUUN3MP-8olExODByIH7N NITRcIwzPThzMEO3OS=>
778 NWT2TFVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG2O|IhcA>? NUnMdmlPcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NEfOcXozPTB{OES2PS=>
449 MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXe3NkBp NVP5Z2Y5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M1S1flI2ODJ6NE[5
LP3 NG\RSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjXO|IhcA>? M1nlV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MV2yOVAzQDR4OR?=
LP6 NFLKUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3WUlY4OiCq NWDUOWdNcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NV\lUVNsOjVyMki0Olk>
LP8 NVvkPGdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTJ[4tKPzJiaB?= NFPwSlNqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NUDQVINFOjVyMki0Olk>
LPS141 NFrpOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HsTFczKGh? M36yZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NIjZXGgzPTB{OES2PS=>
778 M1LZb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITOPVg{NjN|IN88US=> Mm\ONlQhcA>? MlHx[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M1X2WlI2ODJ6NE[5
449 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\QN{4{OyEQvF2= NHLUSWozPCCq MWHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MYqyOVAzQDR4OR?=
LP3 M{TiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm1PFVxOy5|MzFOwG0> MomxNlQhcA>? NYPTWIR2\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> Mk\TNlUxOjh2Nkm=
LP6 NH\oU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFWy[Xk{NjN|IN88US=> NGG2ZWwzPCCq NF7YcXhl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> Mk\GNlUxOjh2Nkm=
LP8 NWC2OoxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjNSYQ{NjN|IN88US=> MUSyOEBp Ml\D[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MoLyNlUxOjh2Nkm=
LPS141 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLkN{4{OyEQvF2= Ml\QNlQhcA>? MWfk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NXTiNW5mOjVyMki0Olk>
IMR5 M2nT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rHZVI1KGh? MWfEUXNQ MnzITWM2OD1zMk[gcm0> NIXCTFMzPDB2NUG3PS=>
BE2C NUfMZWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rjeVI1KGh? NH3vbItFVVOR NFL5[lRKSzVyPUGzOEBvVQ>? M{nzT|I1ODR3MUe5
1643 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLhboczPCCq MVfEUXNQ MlrMTWM2OD1zNEegcm0> NHr1bmkzPDB2NUG3PS=>
SKNSH MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLh[ZIzPCCq M3fGPGROW09? M3K1XmlEPTB;MUS4JI5O MUeyOFA1PTF5OR?=
SY5Y MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKyOEBp MXfEUXNQ MmXUTWM2OD1zNUSgcm0> MmjYNlQxPDVzN{m=
NGP MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPlNlQhcA>? NY\zPFh[TE2VTx?= MmnJTWM2OD1zN{Wgcm0> Ml;wNlQxPDVzN{m=
KELLY MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInnTJUzPCCq NGi2S5RFVVOR MUTJR|UxRTJ{MDDuUS=> M17LcFI1ODR3MUe5
CHP134 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHNPWYzPCCq MkfnSG1UVw>? M3zxW2lEPTB;MkezJI5O MWGyOFA1PTF5OR?=
NLF MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDnNlQhcA>? NIj5V|VFVVOR MYfJR|UxRTN{ODDuUS=> MYiyOFA1PTF5OR?=
LAN5 NVrydG9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmyOEBp MUfEUXNQ M4rWe2lEPTB;NEK5JI5O M2H5W|I1ODR3MUe5
NB69 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2yOEBp MX3EUXNQ MojMTWM2OD15M{igcm0> NIHhd4YzPDB2NUG3PS=>
SKNDZ MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrINlQhcA>? MnXxSG1UVw>? NHLBcWFKSzVyPUiwNUBvVQ>? NIrWPIkzPDB2NUG3PS=>
NBSD MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XWTVI1KGh? MkS0SG1UVw>? M1v1fmlEPTB;MUmwNEBvVQ>? M{HDNFI1ODR3MUe5
SKNF1 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDtc|dLOjRiaB?= NXjxc3A1TE2VTx?= Mor2TWM2OD1|NUCwJI5O M4HjcVI1ODR3MUe5
EBC1 NImwOVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfTNlQhcA>? M{fa[mROW09? NWX3WYhjUUN3ME22OFAxKG6P M1vERVI1ODR3MUe5
SKNAS NGPSWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmyOEBp NHrhc3pFVVOR MlTxTWM2OO,:nkGwNFAxKG6P MkjPNlQxPDVzN{m=
NB16 M3HqXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqyOEBp MUnEUXNQ M37VVmlEPTExvK6xNFAxOCCwTR?= NYnVNZRFOjRyNEWxO|k>
RPE1 NH3YflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3vZ|YzPCCq NU\XdYxyTE2VTx?= M2rG[mlEPTExvK6xNFAxOCCwTR?= MV6yOFA1PTF5OR?=

... 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.
  • 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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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