Ribociclib (LEE011)

For research use only.

Catalog No.S7440

49 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 49 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

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
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NCI-H1299 Mn3iR5l1d3SxeHnjbZR6KGG|c3H5 NEHuTJo4OiCqcoO= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gOU41PiEQvF2u NXnBVZVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D M3j5R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\vO|IhcHK| MUTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDUOFdFKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTC2MlIzPyEQvF2u NHP1dFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+
T47D MW\DfZRwfG:6aXPpeJkh[XO|YYm= Ml;IO|IhcHK| MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDZwMkOg{txONg>? M1XMPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
H1299 MnzJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYq3NkBpenN? Mor4S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFEzQTliY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgR2NMQCCjc4PhfUwhUUN3MDC9JFcvPjN5IN88UU4> NF;BeXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+
KOPN8 M2nndmFxd3C2b4Ppd{Bie3OjeR?= NWPpOnlOOC53IIXN NWTsVndpOyCqcoO= NG\sSlNKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKGGodHXyJFMhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
KOPN8 MVPBdI9xfG:|aYOgZZN{[Xl? NH;4eXoxNjVidV2= MnXQNlQhcHK| NGnUdmhKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKHC{ZT30doVifGWmIIfpeIghVkGFIH\vdkAyKGi{IHHu[EBu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M37B[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO|k4PTxxYU6=
Hep3B MlywR4VtdCCleXPs[UBie3OjeR?= NGezVZUzPCCqcoO= MW\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
HepG2 Mn70R4VtdCCleXPs[UBie3OjeR?= MnTENlQhcHK| MmK2R4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 M2XLWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
A549 NHrtPJVE\WyuIHP5Z4xmKGG|c3H5 Ml;xNlQhcHK| MmjDR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? MkDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
NCI-H460 MWfD[YxtKGO7Y3zlJIF{e2G7 MV[yOEBpenN? M{nWSmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG5EUS2KNE[wJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNE9IOSCyaHHz[UBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDiZZNm\CCobH;3JIN6fG:vZYTyfS=> NWXCbWdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D NYfWU|g1S2WubDDjfYNt\SCjc4PhfS=> Mmi2NlQhcHK| M33icmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJHQ1P0RiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
MDA-MB-231 MlG5R4VtdCCleXPs[UBie3OjeR?= NFfobnIzPCCqcoO= NWftSYQ3S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? NFG1cGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
Fluc-labeled 4T1 NXHQWnVHSW62aYT1cY9zKGG|c3H5 M2m0WFE{OCCvZz;r[y=> NHTtdJUyQCCmYYnz M1OzU2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF\seYMudGGkZXzl[EA1XDFiY3XscJMhcW2ybHHueIVlKGmwIFLhcIIw[yCvb4Xz[UBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6geJVud3Jid3Xp[4h1KGG2IEGzNEBu\y:tZzygbZAh[WSvaX7pd5RmemWmIHThbYx6KG[xcjCxPEBl[Xm|IH3lZZN2emWmIHHmeIVzKDhidH:gNlUh\GG7cx?= NHPkO5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
T47D M2PyPWNmdGxiY4njcIUh[XO|YYm= NWfKPFZ3OjRiaILz MkLPTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6 MmnwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUG5O|koRjJ6NkWxPVc6RC:jPh?=

... 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04657679 Not yet 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) December 2020 --
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma October 29 2020 Phase 1
NCT04417621 Recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Melanoma Novartis Pharmaceuticals|Novartis October 16 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

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

Tel: +1-832-582-8158 Ext:3

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID