Ribociclib (LEE011)

For research use only.

Catalog No.S7440

42 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 42 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 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnKdphmOjRiaB?= NWXydY9QT0l3ME2yO|Yhdk1? MVOyOVg2OjB3OB?=
Myoblast NYfZWnFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjCdJVHPzJiaB?= MnvqTWM2OD1zMEO1JI5O MlPINlU5OTB|N{W=
IMRS Mo[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGwO|IhcA>? MVfJR|UxRTh5MzDuUS=> NF;MZlczPThzMEO3OS=>
SKNAS MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK3NmlDPzJiaB?= NF3ISIZKSzVy78{eNVAxODBibl2= NXrkOolVOjV6MUCzO|U>
Rh28 NHjtRppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LFcVczKGh? MkPNTWM2OD16NEWgcm0> NWHtXW5lOjV6MUCzO|U>
Rh41 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVW3NkBp MoraTWM2OD15MUi3JI5O Mn70NlU5OTB|N{W=
CW9019 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PnVVczKGh? MmLpTWM2OD17OUGyJI5O MkTwNlU5OTB|N{W=
Rh5 NVr3WGl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWG3NkBp M4WyZWlEPTExvK6xNFAxOCCwTR?= M3XZNlI2QDFyM{e1
Rh30 NUjXc2N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;FdphJPzJiaB?= MXrJR|Ux97zgMUCwNFAhdk1? M1\nZVI2QDFyM{e1
778 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7xU5o4OiCq M2PRUolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MYKyOVAzQDR4OR?=
449 M2n1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlm3O|IhcA>? MojEbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M3jJdFI2ODJ6NE[5
LP3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TUXFczKGh? MXXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MX[yOVAzQDR4OR?=
LP6 NYPG[XY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILXOYo4OiCq MVfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MV2yOVAzQDR4OR?=
LP8 NVj6cGdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHG[2c4OiCq MWfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUOyWmFpOjVyMki0Olk>
LPS141 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHiO|IhcA>? Ml3obY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MWKyOVAzQDR4OR?=
778 M3zYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PrXFMvOzNizszN M{\jclI1KGh? NX3Pbotv\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NIXTWHozPTB{OES2PS=>
449 NF3GUHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSzMlM{KM7:TR?= NYDZclRROjRiaB?= NIfrWHVl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MUCyOVAzQDR4OR?=
LP3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q2RVMvOzNizszN NGrjZVgzPCCq NHLFTHhl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MoCzNlUxOjh2Nkm=
LP6 NYfOSIxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknlN{4{OyEQvF2= NEX6OHozPCCq MX3k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NUC5WoVWOjVyMki0Olk>
LP8 M2PYcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXDN{4{OyEQvF2= MVuyOEBp MXfk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NVPUcYNQOjVyMki0Olk>
LPS141 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjvb4xPOy5|MzFOwG0> NULIc|JEOjRiaB?= MoGy[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M2WwN|I2ODJ6NE[5
IMR5 NFfXVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rCWFI1KGh? Mn7rSG1UVw>? MofDTWM2OD1zMk[gcm0> MYeyOFA1PTF5OR?=
BE2C M{Ppb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPzO4lUOjRiaB?= MmK0SG1UVw>? MYLJR|UxRTF|NDDuUS=> M2rhXVI1ODR3MUe5
1643 M1PBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\sNlQhcA>? NEC0bmdFVVOR NXf4b2FpUUN3ME2xOFchdk1? NF2yWpIzPDB2NUG3PS=>
SKNSH M4izd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPHZoFJOjRiaB?= NU\4S3pQTE2VTx?= M{LURmlEPTB;MUS4JI5O M1HuO|I1ODR3MUe5
SY5Y NV\2W4lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmGzNlQhcA>? MoTZSG1UVw>? NGnTdJhKSzVyPUG1OEBvVQ>? NXHlVIlPOjRyNEWxO|k>
NGP M4PF[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITLPGkzPCCq M3\WfmROW09? NYCzOJVKUUN3ME2xO|Uhdk1? Ml70NlQxPDVzN{m=
KELLY M1rqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\u[pozPCCq M{XCUGROW09? MYnJR|UxRTJ{MDDuUS=> MUeyOFA1PTF5OR?=
CHP134 M331N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3SRoYzPCCq NGO5b3RFVVOR MoHSTWM2OD1{N{Ogcm0> MUWyOFA1PTF5OR?=
NLF MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTUNlQhcA>? NIHrfXFFVVOR MXXJR|UxRTN{ODDuUS=> NGjLfoUzPDB2NUG3PS=>
LAN5 NWDhdY1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDkeHBEOjRiaB?= MYjEUXNQ NFrkfXJKSzVyPUSyPUBvVQ>? NVHIfZBpOjRyNEWxO|k>
NB69 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;zXFI1KGh? NF62dIJFVVOR NWPkfXc6UUN3ME23N|ghdk1? MkHFNlQxPDVzN{m=
SKNDZ NIm1RYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCyOEBp NY[0TW9xTE2VTx?= M37uUmlEPTB;OECxJI5O NVLLPZdzOjRyNEWxO|k>
NBSD NILoO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrwNlQhcA>? NEHo[JVFVVOR MVvJR|UxRTF7MECgcm0> MXuyOFA1PTF5OR?=
SKNF1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvuSoozPCCq M1n6W2ROW09? MnfTTWM2OD1|NUCwJI5O M4jORlI1ODR3MUe5
EBC1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCyOEBp MXTEUXNQ MU\JR|UxRTZ2MECgcm0> MWCyOFA1PTF5OR?=
SKNAS NWL0XYV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7lOJczPCCq MVHEUXNQ M1\2T2lEPTExvK6xNFAxOCCwTR?= M3TNPFI1ODR3MUe5
NB16 MnfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjsNlQhcA>? NGDoRWJFVVOR MlLhTWM2OO,:nkGwNFAxKG6P MYqyOFA1PTF5OR?=
RPE1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjBbYF6OjRiaB?= MYDEUXNQ MV;JR|Ux97zgMUCwNFAhdk1? M2TJZlI1ODR3MUe5

... 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