Ribociclib (LEE011)

For research use only.

Catalog No.S7440

42 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 42 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 M1LhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF63bY8zPCCq MX;HTVUxRTJ5NjDuUS=> MXmyOVg2OjB3OB?=
Myoblast MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHu0SGY4OiCq NYXReI0yUUN3ME2xNFM2KG6P NFnPfIMzPThzMEO3OS=>
IMRS MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHxTohOPzJiaB?= NHzSNFNKSzVyPUi3N{BvVQ>? MVKyOVgyODN5NR?=
SKNAS NIXVN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHUO|IhcA>? NYXH[FFzUUN3MP-8olExODByIH7N MW[yOVgyODN5NR?=
Rh28 NHrPZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jzVFczKGh? Mnm0TWM2OD16NEWgcm0> NULmXVd4OjV6MUCzO|U>
Rh41 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYK3NkBp MWTJR|UxRTdzOEegcm0> M3jRN|I2QDFyM{e1
CW9019 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPWSFRrPzJiaB?= NVP5[ZZ3UUN3ME25PVEzKG6P M12ySlI2QDFyM{e1
Rh5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljhO|IhcA>? NX[yTXpkUUN3MP-8olExODByIH7N NWD5Vm13OjV6MUCzO|U>
Rh30 Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vrWFczKGh? NWDGWFBpUUN3MP-8olExODByIH7N NUHCPY5iOjV6MUCzO|U>
778 MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzRXolkPzJiaB?= MnnJbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyOVAzQDR4OR?=
449 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe3NkBp MonmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXGyOVAzQDR4OR?=
LP3 NHy0XGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP6T5U4OiCq MoHlbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHPR[lMzPTB{OES2PS=>
LP6 NG\JUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjFO|IhcA>? NF;IR41qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MYWyOVAzQDR4OR?=
LP8 M2nod2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG3NkBp M1myc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NIDR[FAzPTB{OES2PS=>
LPS141 M4f4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO3NkBp MYTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MnuwNlUxOjh2Nkm=
778 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjyN{4{OyEQvF2= M4m3XFI1KGh? M1KyU4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MlPjNlUxOjh2Nkm=
449 M3;6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\SeFMvOzNizszN MUmyOEBp MmHz[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NUn1XXRnOjVyMki0Olk>
LP3 NYC2fnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnGU40{NjN|IN88US=> NHvmeJozPCCq Mknx[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NWn1NZk4OjVyMki0Olk>
LP6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWzMlM{KM7:TR?= Mni4NlQhcA>? NYXoe3pJ\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NIDzd2szPTB{OES2PS=>
LP8 MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHqTXk{NjN|IN88US=> MXuyOEBp MYTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M1vQUVI2ODJ6NE[5
LPS141 M1\4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7MN{4{OyEQvF2= NHnpcoczPCCq M335OYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NGf3N2szPTB{OES2PS=>
IMR5 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jEc|I1KGh? M4O2WGROW09? NVXn[IhQUUN3ME2xNlYhdk1? Ml;NNlQxPDVzN{m=
BE2C NHTYUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiyOEBp Mn\DSG1UVw>? NGrlWoVKSzVyPUGzOEBvVQ>? MX2yOFA1PTF5OR?=
1643 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYeyOEBp MXnEUXNQ MmnwTWM2OD1zNEegcm0> NY\1U2hLOjRyNEWxO|k>
SKNSH MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f4V|I1KGh? MmnhSG1UVw>? M{Dv[2lEPTB;MUS4JI5O M3y5W|I1ODR3MUe5
SY5Y MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nFb|I1KGh? Moj1SG1UVw>? NW\BXXJjUUN3ME2xOVQhdk1? NGPEWVgzPDB2NUG3PS=>
NGP M4WxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\NSlI1KGh? M2nXW2ROW09? NVzDcVFOUUN3ME2xO|Uhdk1? NVvWbWpDOjRyNEWxO|k>
KELLY NFe5VVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz3XXQzPCCq NXK5TXc6TE2VTx?= Ml\1TWM2OD1{MkCgcm0> NVLydIRoOjRyNEWxO|k>
CHP134 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3GTm8zPCCq MXXEUXNQ M1;VO2lEPTB;MkezJI5O Mn3lNlQxPDVzN{m=
NLF NYPHOJFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X0VVI1KGh? MnL5SG1UVw>? MlzxTWM2OD1|Mkigcm0> MkjYNlQxPDVzN{m=
LAN5 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWyOEBp NH3XTVdFVVOR NU[3c|R4UUN3ME20Nlkhdk1? NHHPRYczPDB2NUG3PS=>
NB69 NIn3bIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jVT|I1KGh? MUDEUXNQ Mn7rTWM2OD15M{igcm0> NEfC[IUzPDB2NUG3PS=>
SKNDZ NYfKNFIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGyOEBp MXLEUXNQ NH\NVlNKSzVyPUiwNUBvVQ>? NEOyNXczPDB2NUG3PS=>
NBSD NH7DSopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TObVI1KGh? MmfnSG1UVw>? MVzJR|UxRTF7MECgcm0> NH\NVYgzPDB2NUG3PS=>
SKNF1 MmrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKyOEBp NHfPXllFVVOR MoHHTWM2OD1|NUCwJI5O MUCyOFA1PTF5OR?=
EBC1 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3aNlQhcA>? NUfmfogzTE2VTx?= M{THdGlEPTB;NkSwNEBvVQ>? MY[yOFA1PTF5OR?=
SKNAS NHfkbYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqyOEBp MlPKSG1UVw>? M2jle2lEPTExvK6xNFAxOCCwTR?= MVuyOFA1PTF5OR?=
NB16 NF7Z[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\DNlQhcA>? MWXEUXNQ MUnJR|Ux97zgMUCwNFAhdk1? MoXENlQxPDVzN{m=
RPE1 M1LaWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\IUGd6OjRiaB?= MlnlSG1UVw>? NFLBRXVKSzVy78{eNVAxODBibl2= MlXPNlQxPDVzN{m=

... 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
NCT04315233 Not yet recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma August 2020 Phase 1
NCT04417621 Not yet recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Melanoma Novartis Pharmaceuticals|Novartis July 30 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
NCT03701334 Recruiting Drug: Ribociclib|Other: Endocrine Therapy Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID