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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4 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.

    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.

  • (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.

    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.

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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 NGLrOZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvXRpozPCCq MV3HTVUxRTJ5NjDuUS=> MY[yOVg2OjB3OB?=
Myoblast M1LUOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXqxcnUxPzJiaB?= M1rvfWlEPTB;MUCzOUBvVQ>? MoXqNlU5OTB|N{W=
IMRS MmDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXQ[HM4OiCq NI\3TIJKSzVyPUi3N{BvVQ>? NYXSNGV3OjV6MUCzO|U>
SKNAS MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDhO|IhcA>? MkSzTWM2OO,:nkGwNFAxKG6P Mm\KNlU5OTB|N{W=
Rh28 NIi3cYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXyxUnVXPzJiaB?= MUnJR|UxRTh2NTDuUS=> M1rCNlI2QDFyM{e1
Rh41 NWqyZWIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYm3NkBp NFjUVG5KSzVyPUexPFchdk1? M2j2c|I2QDFyM{e1
CW9019 Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKxZpBCPzJiaB?= MonYTWM2OD17OUGyJI5O NV;yb5B{OjV6MUCzO|U>
Rh5 NEPyV5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6zO|IhcA>? MYTJR|Ux97zgMUCwNFAhdk1? NHX3VVEzPThzMEO3OS=>
Rh30 M1:0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;RO|IhcA>? MUnJR|Ux97zgMUCwNFAhdk1? M3TyTFI2QDFyM{e1
778 MmXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M371XVczKGh? NYXmOolQcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MonWNlUxOjh2Nkm=
449 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF36WII4OiCq NYj6dFdCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MXmyOVAzQDR4OR?=
LP3 NVPF[WJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[zR|czKGh? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NH;4PY0zPTB{OES2PS=>
LP6 NH70XIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUCyeIZkPzJiaB?= NUPYPGpXcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MmiwNlUxOjh2Nkm=
LP8 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LXS|czKGh? NUL5dnBXcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NIfqcFYzPTB{OES2PS=>
LPS141 NVn5Zm9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknuO|IhcA>? MXfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2q5UFI2ODJ6NE[5
778 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD3N{4{OyEQvF2= MVKyOEBp MWfk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NVThUIFNOjVyMki0Olk>
449 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL4N{4{OyEQvF2= M{LEPVI1KGh? NFHITJpl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M3fsNlI2ODJ6NE[5
LP3 NYfER3VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHDN{4{OyEQvF2= MYiyOEBp MYHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NV\2SHJ4OjVyMki0Olk>
LP6 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLySpNOOy5|MzFOwG0> MVSyOEBp MlXQ[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MYGyOVAzQDR4OR?=
LP8 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:zMlM{KM7:TR?= NXGzXZJ5OjRiaB?= NYTDOZlu\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MXiyOVAzQDR4OR?=
LPS141 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn4N{4{OyEQvF2= M17zPFI1KGh? MkXJ[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NFfqPZIzPTB{OES2PS=>
IMR5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[yOEBp MVXEUXNQ M1PsZWlEPTB;MUK2JI5O M2TIelI1ODR3MUe5
BE2C NHrie2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz4NlQhcA>? NH\RUVZFVVOR NH\mOZFKSzVyPUGzOEBvVQ>? MnPwNlQxPDVzN{m=
1643 M3LYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfVNlQhcA>? NFPxOnJFVVOR Mo[zTWM2OD1zNEegcm0> NWXaRppFOjRyNEWxO|k>
SKNSH NHfjT49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\wfoJ[OjRiaB?= MUPEUXNQ MlLwTWM2OD1zNEigcm0> Mle3NlQxPDVzN{m=
SY5Y MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:yeGMzPCCq M3OybmROW09? NUHuUmFIUUN3ME2xOVQhdk1? MlTZNlQxPDVzN{m=
NGP MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\oNlI1KGh? NWG5eXpCTE2VTx?= NH3EclFKSzVyPUG3OUBvVQ>? NUnJPXFEOjRyNEWxO|k>
KELLY MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrPNlQhcA>? NFvHWXVFVVOR NILRU5VKSzVyPUKyNEBvVQ>? NWHGUYlbOjRyNEWxO|k>
CHP134 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\V[3ZMOjRiaB?= NGHYVY9FVVOR Mn3iTWM2OD1{N{Ogcm0> NF\6O4kzPDB2NUG3PS=>
NLF M2L0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2mwWlI1KGh? MYDEUXNQ M3q1UmlEPTB;M{K4JI5O NHrSS2czPDB2NUG3PS=>
LAN5 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ZNm0zPCCq M4WwW2ROW09? M1LQdGlEPTB;NEK5JI5O MlH5NlQxPDVzN{m=
NB69 NGTSXpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSyOEBp NWPjNYNbTE2VTx?= NXOzdm9RUUN3ME23N|ghdk1? MWKyOFA1PTF5OR?=
SKNDZ M{\WRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm5U|lNOjRiaB?= NGfpWmFFVVOR MkjJTWM2OD16MEGgcm0> MmnHNlQxPDVzN{m=
NBSD NUfrSWJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn30NlQhcA>? MnzESG1UVw>? NGfBRZlKSzVyPUG5NFAhdk1? NXzubI9MOjRyNEWxO|k>
SKNF1 M3fPWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f4TlI1KGh? M2HLOmROW09? MojETWM2OD1|NUCwJI5O MlX1NlQxPDVzN{m=
EBC1 NHKxeYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LBW|I1KGh? M1;jVGROW09? MWfJR|UxRTZ2MECgcm0> NUfFZ2JbOjRyNEWxO|k>
SKNAS NHLrXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKyOEBp MWLEUXNQ M3z4ZWlEPTExvK6xNFAxOCCwTR?= NVHv[48{OjRyNEWxO|k>
NB16 NVOzcYpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\DNlQhcA>? MknCSG1UVw>? MWjJR|Ux97zgMUCwNFAhdk1? M4nyeVI1ODR3MUe5
RPE1 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITjRpozPCCq MVzEUXNQ NFX3Xm1KSzVy78{eNVAxODBibl2= MUiyOFA1PTF5OR?=

... Click to View More Cell Line Experimental Data

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 Conditions Sponsor/Collaborators Start Date Phases
NCT02657343 Recruiting Breast Cancer Dana-Farber Cancer Institute|Novartis March 9 2016 Phase 1|Phase 2
NCT02422615 Active not recruiting Advanced Breast Cancer Novartis Pharmaceuticals|Novartis June 9 2015 Phase 3
NCT03114527 Recruiting Soft Tissue Sarcoma Fox Chase Cancer Center August 8 2017 Phase 2
NCT02657928 Active not recruiting Estrogen Receptor Positive|Postmenopausal|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma Mayo Clinic|National Cancer Institute (NCI) July 8 2016 Phase 2
NCT01857193 Active not recruiting Breast Cancer Novartis Pharmaceuticals|Novartis September 6 2013 Phase 1
NCT03237390 Recruiting Advanced Malignant Solid Neoplasm|Metastatic Malignant Solid Neoplasm Mayo Clinic|National Cancer Institute (NCI) January 4 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID