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 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr6NlQhcA>? NUThPGVNT0l3ME2yO|Yhdk1? MlPnNlU5PTJyNUi=
Myoblast MlnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG3NkBp NYDNdmJNUUN3ME2xNFM2KG6P NGXrWWYzPThzMEO3OS=>
IMRS M4XtO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK3NkBp NEnSN2hKSzVyPUi3N{BvVQ>? NYfneJg2OjV6MUCzO|U>
SKNAS MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;GSo1DPzJiaB?= MVTJR|Ux97zgMUCwNFAhdk1? MmH3NlU5OTB|N{W=
Rh28 M{[4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfpbm1KPzJiaB?= NEXrfYxKSzVyPUi0OUBvVQ>? MWSyOVgyODN5NR?=
Rh41 MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDuV284OiCq M2Tu[2lEPTB;N{G4O{BvVQ>? NVvWRXVwOjV6MUCzO|U>
CW9019 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVu3NkBp Mm\KTWM2OD17OUGyJI5O M{jodlI2QDFyM{e1
Rh5 NGjoTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PjRlczKGh? NXL1SGRtUUN3MP-8olExODByIH7N MlnxNlU5OTB|N{W=
Rh30 NGfhXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX21S2NJPzJiaB?= MWjJR|Ux97zgMUCwNFAhdk1? MXGyOVgyODN5NR?=
778 M2XTcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLHO|IhcA>? MnHjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnvmNlUxOjh2Nkm=
449 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWC3NkBp Mnj2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUmyOVAzQDR4OR?=
LP3 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGyOGdGPzJiaB?= MoLGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MYWyOVAzQDR4OR?=
LP6 NXzyRopiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jlNFczKGh? M3PaUolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MWSyOVAzQDR4OR?=
LP8 NUP6S2hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPlO|IhcA>? M3jqPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NYjnPYN2OjVyMki0Olk>
LPS141 NYrn[YU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDOU4I4OiCq NYfkO|ZkcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M{HyfVI2ODJ6NE[5
778 Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPlUZo{NjN|IN88US=> M3yydFI1KGh? MWrk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NIPMUIszPTB{OES2PS=>
449 MmLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PpelMvOzNizszN NEC0clYzPCCq NIHNXlNl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> Mmf1NlUxOjh2Nkm=
LP3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\KclMvOzNizszN MWmyOEBp NETQZXZl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M1zvWFI2ODJ6NE[5
LP6 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{GxdlMvOzNizszN NFX0W3UzPCCq MVHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NXLtUZNOOjVyMki0Olk>
LP8 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXWN{4{OyEQvF2= NV7JUHVtOjRiaB?= MXzk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NVLqNXlCOjVyMki0Olk>
LPS141 MofWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe3c2c{NjN|IN88US=> M1\6[FI1KGh? MkC0[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NFWzdoEzPTB{OES2PS=>
IMR5 MkfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSyOEBp NYKyXIwzTE2VTx?= MYjJR|UxRTF{NjDuUS=> M3KzXVI1ODR3MUe5
BE2C MlHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYeyOEBp NEPDUI9FVVOR Moi2TWM2OD1zM{Sgcm0> MWCyOFA1PTF5OR?=
1643 NH7ibGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHp[5VCOjRiaB?= MVrEUXNQ NELNNGpKSzVyPUG0O{BvVQ>? M1HQW|I1ODR3MUe5
SKNSH NWHmfoVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H2flI1KGh? MnS1SG1UVw>? MWDJR|UxRTF2ODDuUS=> NHn0NYwzPDB2NUG3PS=>
SY5Y NHvUOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDLdFAzPCCq MXfEUXNQ MkjVTWM2OD1zNUSgcm0> NGnJOXEzPDB2NUG3PS=>
NGP M1na[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3HTGgzPCCq NFTNbWxFVVOR NEj5XYlKSzVyPUG3OUBvVQ>? NWThS2E1OjRyNEWxO|k>
KELLY NF74XZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPLNlQhcA>? NE[4TItFVVOR M33l[mlEPTB;MkKwJI5O MWWyOFA1PTF5OR?=
CHP134 NXmwdnBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfLNYgzPCCq M2naVGROW09? NIDPTHNKSzVyPUK3N{BvVQ>? M2K0N|I1ODR3MUe5
NLF NGXzN2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIWxSYIzPCCq M1ThWmROW09? M1HHNGlEPTB;M{K4JI5O NEjjWIszPDB2NUG3PS=>
LAN5 NGHpUY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rPRlI1KGh? MkK1SG1UVw>? NXu2R3NVUUN3ME20Nlkhdk1? NWfLWHRHOjRyNEWxO|k>
NB69 M3O2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17jN|I1KGh? MUXEUXNQ NVnubJFGUUN3ME23N|ghdk1? NHzR[IwzPDB2NUG3PS=>
SKNDZ NYPnS2txT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TDT|I1KGh? MXjEUXNQ NX\4co9qUUN3ME24NFEhdk1? NFTnfY8zPDB2NUG3PS=>
NBSD MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nsOVI1KGh? MWTEUXNQ MVfJR|UxRTF7MECgcm0> NYrr[FJWOjRyNEWxO|k>
SKNF1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGyOEBp NXjmVYk{TE2VTx?= M{LqVGlEPTB;M{WwNEBvVQ>? MVWyOFA1PTF5OR?=
EBC1 NUL4V4luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[yOEBp NIHQRnpFVVOR NWnVdYl2UUN3ME22OFAxKG6P MnHvNlQxPDVzN{m=
SKNAS MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nBUVI1KGh? M2XYNWROW09? NEHZb3JKSzVy78{eNVAxODBibl2= NGKz[3AzPDB2NUG3PS=>
NB16 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojSNlQhcA>? M2f2fmROW09? Mo\ITWM2OO,:nkGwNFAxKG6P MUOyOFA1PTF5OR?=
RPE1 MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX60fI1[OjRiaB?= NXridVBPTE2VTx?= MYfJR|Ux97zgMUCwNFAhdk1? M3z5[lI1ODR3MUe5

... 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