Ribociclib (LEE011)

Catalog No.S7440

For research use only.

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

Ribociclib (LEE011) Chemical Structure

CAS No. 1211441-98-3

Selleck's Ribociclib (LEE011) has been cited by 63 publications

Purity & Quality Control

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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 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLqfHdkOjRiaB?= M3;rc2dKPTB;Mke2JI5O NFzKTHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi1NlA2QCd-MkW4OVIxPTh:L3G+
Myoblast MnPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHGOHpHPzJiaB?= NYTIWZZuUUN3ME2xNFM2KG6P MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO|U9N2F-
IMRS MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPVc|FvPzJiaB?= NEL3cotKSzVyPUi3N{BvVQ>? MmrBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO|UoRjJ3OEGwN|c2RC:jPh?=
SKNAS MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4i1TlczKGh? NX;JdFJ2UUN3MP-8olExODByIH7N NGfURm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
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CW9019 NFewXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\nO|IhcA>? NFvsNJlKSzVyPUm5NVIhdk1? M3ftR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN|c2Lz5{NUixNFM4PTxxYU6=
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Rh30 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nVV|czKGh? MYrJR|Ux97zgMUCwNFAhdk1? NHu0boc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
778 M1HKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi3NkBp NW[4RXlmcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M3zLXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
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NCI-H1299 MnLOR5l1d3SxeHnjbZR6KGG|c3H5 NEHBbpA4OiCqcoO= M1;nVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KMUK5PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA2NjR4IN88UU4> MmrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
T47D MlPoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkSzO|IhcHK| MkDwS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWFQ4TCClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gOk4zOjdizszNMi=> NEDjVJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+
T47D M2XCZmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHnoSY84OiCqcoO= MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDZwMkOg{txONg>? M{HmVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
H1299 NEnpTm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1foXlczKGi{cx?= NHzmfVRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJOTJ7OTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPy54M{eg{txONg>? Mnn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUG5O|koRjJ6NkWxPVc6RC:jPh?=
KOPN8 NHPpb41CeG:ydH;zbZMh[XO|YYm= NXfK[4k5OC53IIXN MW[zJIhzew>? NH7P[mVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKGGodHXyJFMhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NGrtS2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO|k4PSd-Mkm0NFc6PzV:L3G+
KOPN8 MV7BdI9xfG:|aYOgZZN{[Xl? MnT5NE42KHWP MWSyOEBpenN? NWfN[nNiUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLU3BPQCClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4Yh[2ynYY\l[EBRSVKSIHzleoVtKGG2IECuOUB2VSCycnWteJJm[XSnZDD3bZRpKE6DQzDmc5IhOSCqcjDhcoQhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M3Gzc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO|k4PTxxYU6=
Hep3B NW\CcFRIS2WubDDjfYNt\SCjc4PhfS=> NWrlSWRKOjRiaILz NIHsdGlE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ\XB|QjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com= NYmxfVNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2 NULPVGRrS2WubDDjfYNt\SCjc4PhfS=> NITydmQzPCCqcoO= Moq2R4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 M2jkdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
A549 NYnJNYl1S2WubDDjfYNt\SCjc4PhfS=> NFTlbpkzPCCqcoO= MoDuR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? NF\3WGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
NCI-H460 M360UmNmdGxiY4njcIUh[XO|YYm= NXz0bYppOjRiaILz MonHR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gUmNKNUh2NkCgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5 NFnkcJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
T47D NY\1XGFCS2WubDDjfYNt\SCjc4PhfS=> M1jqWFI1KGi{cx?= MlGzR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? NHjze2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
MDA-MB-231 MXPD[YxtKGO7Y3zlJIF{e2G7 M1;Md|I1KGi{cx?= MXnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNE9IOSCyaHHz[UBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDiZZNm\CCobH;3JIN6fG:vZYTyfS=> NFviW4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
Fluc-labeled 4T1 MkXmRY51cXS3bX;yJIF{e2G7 MUixN|AhdWdxa3e= NXvJN281OThiZHH5dy=> NYrB[G0zSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgSox2[y2uYXLlcIVlKDSWMTDj[YxteyCrbYDsZY51\WRiaX6gRoFt[i:lIH3veZNmKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckB1fW2xcjD3[YlocHRiYYSgNVMxKG2pL3vnMEBqeCCjZH3pcol{fGW{ZXSg[IFqdHliZn;yJFE5KGSjeYOgcYVie3W{ZXSgZYZ1\XJiODD0c{AzPSCmYYnz NHy3VJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
T47D NXPlS|g3S2WubDDjfYNt\SCjc4PhfS=> M3TMfFI1KGi{cx?= Ml[4TY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6 NEW0Rm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+
Assay
Methods Test Index PMID
Western blot pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP 29789630
Growth inhibition assay 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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts.
  • Dosages: ~200 mg/kg daily
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 7 mg/mL
(16.1 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 434.54
Formula

C23H30N8O

CAS No. 1211441-98-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04657679 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) May 20 2021 --
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma May 3 2021 Phase 1
NCT04417621 Recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Melanoma Novartis Pharmaceuticals|Novartis October 30 2020 Phase 2
NCT05141240 Completed Drug: Ribiciclib|Drug: Palbociclib|Drug: Abemaciclib Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis April 15 2020 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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