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 16 Publications

6 Customer Reviews

  • IB analysis of whole cell lysates derived from mouse CT26 or 4T1 tumor cell lines treated with or without the CDK4/6 inhibitor, ribociclib.

    Nature, 2017, 553(7686):91-95. Ribociclib (LEE011) purchased from Selleck.

  • Analysis of apoptosis in leukemia cells induced by LEE011. Annexin V staining of cells following 48-h treatment with LEE011 at 2 or 5 µM compared with DMSO controls. Following 5-µM LEE011 treatment, the K562 apoptotic cell percentage was 5.9 ± 0.75 vs. 1.2 ± 0.66% for the DMSO group, P = 0.001; in MV4-11 cells, the apoptotic cell percentage was 24.2 ± 3.06 vs. 0.53 ± 0.40% for the DMSO group, P = 0.005; in U937 cells, the apoptotic cell percentage was 9.9 ± 2.81 vs. 0.57 ± 0.42% for the DMSO group, P = 0.027; in HL-60 cells, the apoptotic cell percentage was 28.23 ± 6.01 vs. 0.9 ± 0.8% for the DMSO group, P = 0.015; in THP-1 cells, the apoptotic cell percentage was 1.76 ± 0.4 vs. 1.56 ± 0.45% for the DMSO group, P = 0.59; in CCRF cells, the apoptotic cell percentage was 13.77 ± 3.16 vs. 1.2 ± 0.36% for the DMSO group, P = 0.019; in NB4 cells, the apoptotic cell percentage was 12.1 ± 1.35 vs. 0.86 ± 0.25% for the DMSO group, P = 0.004; and in SHI-1 cells the apoptotic cell percentage was 12.6 ± 2.81 vs. 1.87 ± 0.75% for the DMSO group, P = 0.017. These analyses were repeated three times. *P < 0.05; **P < 0.01

    Cancer Cell Int, 2017, 17:35. Ribociclib (LEE011) purchased from Selleck.

  • The combination of a different mTOR inhibitor temsirolimus (4 μM) and a different CDK4/6 inhibitor ribociclib (4 μM) is also synergistic against GICs (***P < 0.0001; one-way ANOVA with post-hoc Tukey analysis).

    Clin Cancer Res, 2017, 23(22):6958-6968. Ribociclib (LEE011) purchased from Selleck.

  • The effects of the CDK inhibitor abemaciclib, palbociclib, and ribociclib on Trop2 ICD cleavage. CDK inhibitors decreased Trop2 ICD abundance after the second day of CDK inhibitor treatment.

    Cancer Res, 2016, 76(22):6723-6734. Ribociclib (LEE011) purchased from Selleck.

  • SJSA cells were treated with the alternate CDK4/6 inhibitors Ribociclib (LEE011) and Abemaciclib (LY2835219) for 30 h, alone or in combination with Nutlin at 20 µM for 6 h.

    Cell Death Dis, 2018, 9(9): 918. Ribociclib (LEE011) purchased from Selleck.

  • (B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.

    Transl Oncol, 2016, 9(3):197-202.. Ribociclib (LEE011) purchased from Selleck.

Purity & Quality Control

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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 NV2wNlQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37NWlI1KGh? NUPldFYxT0l3ME2yO|Yhdk1? M{nsVlI2QDV{MEW4
Myoblast NXTsWXhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi3NkBp M1n6cGlEPTB;MUCzOUBvVQ>? NFXqXW8zPThzMEO3OS=>
IMRS MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUH4fJY1PzJiaB?= MlnuTWM2OD16N{Ogcm0> NF7iRnczPThzMEO3OS=>
SKNAS MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYe3NkBp NVz0NWVsUUN3MP-8olExODByIH7N MojmNlU5OTB|N{W=
Rh28 MmjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETOS204OiCq M{n2PGlEPTB;OES1JI5O NI\MZlMzPThzMEO3OS=>
Rh41 M2P6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf1VII4OiCq MnfiTWM2OD15MUi3JI5O NYfwUI4zOjV6MUCzO|U>
CW9019 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTmO|IhcA>? MnfRTWM2OD17OUGyJI5O NFqyOlgzPThzMEO3OS=>
Rh5 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLLfpM4OiCq MlnhTWM2OO,:nkGwNFAxKG6P MUWyOVgyODN5NR?=
Rh30 M4i3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjKTIlPPzJiaB?= NHTIfXdKSzVy78{eNVAxODBibl2= MY[yOVgyODN5NR?=
778 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fOXFczKGh? MonHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUeyOVAzQDR4OR?=
449 NFLYc5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO4O|IhcA>? M3vYWolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M{LoRVI2ODJ6NE[5
LP3 NFm1O3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXK3NkBp NXn3PZRDcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mn\DNlUxOjh2Nkm=
LP6 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO3NkBp M{XRUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHryXXMzPTB{OES2PS=>
LP8 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\oSFczKGh? M1vOVolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWrSUXVwOjVyMki0Olk>
LPS141 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjLT3M4OiCq MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NVPMR3kzOjVyMki0Olk>
778 NWG2NpFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGzMlM{KM7:TR?= M1zzUFI1KGh? NUjlPYlw\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MVyyOVAzQDR4OR?=
449 NXm4dIxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXyzMlM{KM7:TR?= MX6yOEBp NEiyb5Rl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NHj3UY8zPTB{OES2PS=>
LP3 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;IXFM{NjN|IN88US=> NUH3V2M2OjRiaB?= MX7k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M3;lRVI2ODJ6NE[5
LP6 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3SboY{NjN|IN88US=> MnHCNlQhcA>? NWGyT21X\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MmnqNlUxOjh2Nkm=
LP8 NYPlcphJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPKNJY{NjN|IN88US=> M2GzWlI1KGh? NVq3ephs\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NXHtSIxjOjVyMki0Olk>
LPS141 NXXFcWJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\PNVMvOzNizszN M1XXNlI1KGh? Ml;z[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MmL1NlUxOjh2Nkm=
IMR5 MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33zd|I1KGh? M2TKeGROW09? MkfjTWM2OD1zMk[gcm0> MUmyOFA1PTF5OR?=
BE2C Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37HblI1KGh? M1vRfWROW09? M3PKWmlEPTB;MUO0JI5O MljpNlQxPDVzN{m=
1643 NGrVUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:0NlQhcA>? MWHEUXNQ NVjrTGJ4UUN3ME2xOFchdk1? NUDORYtROjRyNEWxO|k>
SKNSH M3PjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrmNlQhcA>? NGPUWHRFVVOR NVr5NFVbUUN3ME2xOFghdk1? M3:0XFI1ODR3MUe5
SY5Y MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViyOEBp MkH0SG1UVw>? MULJR|UxRTF3NDDuUS=> M3\tWlI1ODR3MUe5
NGP NXnONJR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPCfFczPCCq M{jOcWROW09? M334Z2lEPTB;MUe1JI5O MUCyOFA1PTF5OR?=
KELLY M4jpWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDTPFQzPCCq MWLEUXNQ M4HzTmlEPTB;MkKwJI5O MXGyOFA1PTF5OR?=
CHP134 NHnPUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnTO2UzPCCq MYfEUXNQ MnX0TWM2OD1{N{Ogcm0> NX;TOpFwOjRyNEWxO|k>
NLF NG\ZPGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknxNlQhcA>? MUDEUXNQ MWrJR|UxRTN{ODDuUS=> M2rR[|I1ODR3MUe5
LAN5 M1LlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTYNlQhcA>? MUPEUXNQ MoHuTWM2OD12Mkmgcm0> M4XPV|I1ODR3MUe5
NB69 M3TDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmyOEBp MY\EUXNQ MXHJR|UxRTd|ODDuUS=> MlfPNlQxPDVzN{m=
SKNDZ MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCzeJJ[OjRiaB?= M1jmOGROW09? MVvJR|UxRThyMTDuUS=> NYC1V5ZyOjRyNEWxO|k>
NBSD NWfQOFNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\SNlQhcA>? M3zJRmROW09? M1LQXGlEPTB;MUmwNEBvVQ>? M{\jT|I1ODR3MUe5
SKNF1 M1LDcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MViyOEBp M{S1ZWROW09? MUTJR|UxRTN3MECgcm0> NHu4PXgzPDB2NUG3PS=>
EBC1 NU\XcY1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[1WFdGOjRiaB?= MXjEUXNQ MWrJR|UxRTZ2MECgcm0> MnmxNlQxPDVzN{m=
SKNAS MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fxUFI1KGh? MnfDSG1UVw>? NHrzdZBKSzVy78{eNVAxODBibl2= NUPyOZpYOjRyNEWxO|k>
NB16 NEi4R4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXYNlQhcA>? NIT2blVFVVOR MULJR|Ux97zgMUCwNFAhdk1? MnjZNlQxPDVzN{m=
RPE1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSzbZFLOjRiaB?= NXPWXVk4TE2VTx?= NUi3NYcxUUN3MP-8olExODByIH7N M2q4WFI1ODR3MUe5

... 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]

+ Expand
  • 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]

+ Expand
  • 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