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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3 Customer Reviews

  • 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. Ribociclib (LEE011) purchased from Selleck.

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Choose Selective CDK Inhibitors

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 NXPRdFZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvFN4YzPCCq NVG0[G9TT0l3ME2yO|Yhdk1? Mny2NlU5PTJyNUi=
Myoblast MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Pz[|czKGh? M3\QfGlEPTB;MUCzOUBvVQ>? M3nxV|I2QDFyM{e1
IMRS M1POV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXK3NkBp M3faVGlEPTB;OEezJI5O MmWxNlU5OTB|N{W=
SKNAS Mn;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y3SlczKGh? NGT5U2ZKSzVy78{eNVAxODBibl2= M2jYVlI2QDFyM{e1
Rh28 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe3NkBp M1LNbGlEPTB;OES1JI5O NYe5Wm1tOjV6MUCzO|U>
Rh41 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TvOVczKGh? NXHlOVlVUUN3ME23NVg4KG6P NIDwbJIzPThzMEO3OS=>
CW9019 NUO1[WhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLvWWg4OiCq M{fjZ2lEPTB;OUmxNkBvVQ>? NWXqPVhDOjV6MUCzO|U>
Rh5 NXT6cox4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\6UIJ1PzJiaB?= MWjJR|Ux97zgMUCwNFAhdk1? NFfhbYEzPThzMEO3OS=>
Rh30 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rjWlczKGh? NY[2NIJiUUN3MP-8olExODByIH7N M2PGdVI2QDFyM{e1
778 MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK5Tnk4OiCq NV;OPYlOcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M2i1ZVI2ODJ6NE[5
449 Mn7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfMT4k4OiCq NUD4O3BTcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M3KxdlI2ODJ6NE[5
LP3 NVWyTlRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjRbVU4OiCq MlmxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MkLlNlUxOjh2Nkm=
LP6 NHLPdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWyO|IhcA>? NVfsO21QcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mon0NlUxOjh2Nkm=
LP8 M{LEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLNS4Y4OiCq MoXQbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1LLW|I2ODJ6NE[5
LPS141 NULkUHF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\XVG04OiCq M1PESYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NVzHfnZqOjVyMki0Olk>
778 NV;SW|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HY[|MvOzNizszN MYWyOEBp NWrDPGg4\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NInwWo0zPTB{OES2PS=>
449 NUHLOIpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzQPYNXOy5|MzFOwG0> MoHKNlQhcA>? NUL1eZBw\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NX;He3lnOjVyMki0Olk>
LP3 NWDqbpJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nydlMvOzNizszN M2[wZlI1KGh? NHTsWVBl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NWLIW29DOjVyMki0Olk>
LP6 Ml[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnsV5A{NjN|IN88US=> M4DFe|I1KGh? MnrY[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M3zheVI2ODJ6NE[5
LP8 M1fjd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi3dlU{NjN|IN88US=> MXyyOEBp MmTD[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MmPINlUxOjh2Nkm=
LPS141 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDwNYo{NjN|IN88US=> NVzVTnE3OjRiaB?= NGrlR2Fl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M2TiOFI2ODJ6NE[5
IMR5 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33idlI1KGh? NHnyW5lFVVOR MWTJR|UxRTF{NjDuUS=> M4K5N|I1ODR3MUe5
BE2C NVLYPXJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfENoR{OjRiaB?= NWj4cmpYTE2VTx?= MoPrTWM2OD1zM{Sgcm0> NID2ToUzPDB2NUG3PS=>
1643 NYPEVHdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDXNlQhcA>? Mnv4SG1UVw>? M1j0[WlEPTB;MUS3JI5O MWeyOFA1PTF5OR?=
SKNSH MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7yPGQzPCCq M3jNPGROW09? MVrJR|UxRTF2ODDuUS=> MVuyOFA1PTF5OR?=
SY5Y M4LkOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVyyOEBp M33zUmROW09? Mkf3TWM2OD1zNUSgcm0> NELIbXczPDB2NUG3PS=>
NGP NUfKWnhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPyWolHOjRiaB?= M1jjRWROW09? MW\JR|UxRTF5NTDuUS=> NGG4WJczPDB2NUG3PS=>
KELLY Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vJRlI1KGh? MX3EUXNQ MYTJR|UxRTJ{MDDuUS=> NXvwT3VUOjRyNEWxO|k>
CHP134 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKyOEBp NIO0R4VFVVOR MmHtTWM2OD1{N{Ogcm0> MVuyOFA1PTF5OR?=
NLF MoTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXUe5VIOjRiaB?= MofDSG1UVw>? MU\JR|UxRTN{ODDuUS=> M17ucFI1ODR3MUe5
LAN5 NV3QUI1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz4XHRJOjRiaB?= NH;DO3dFVVOR MXLJR|UxRTR{OTDuUS=> MoX6NlQxPDVzN{m=
NB69 NFHEOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVyyT3VIOjRiaB?= NWC2VYJ7TE2VTx?= NV;qdJR2UUN3ME23N|ghdk1? MUSyOFA1PTF5OR?=
SKNDZ NGf5WohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvUNlQhcA>? M2rCU2ROW09? NHn2R4NKSzVyPUiwNUBvVQ>? NYLWSGd2OjRyNEWxO|k>
NBSD NXf3e25XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrv[ZZ6OjRiaB?= MX7EUXNQ MU\JR|UxRTF7MECgcm0> M1\Jc|I1ODR3MUe5
SKNF1 M1zDfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOyOEBp NVrwNXlzTE2VTx?= NFPBZWZKSzVyPUO1NFAhdk1? NVWxVZAyOjRyNEWxO|k>
EBC1 MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV2wXlVROjRiaB?= NHK0bJlFVVOR Mnz2TWM2OD14NECwJI5O M3vBRlI1ODR3MUe5
SKNAS NHHK[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvnWZozPCCq MoXsSG1UVw>? MYHJR|Ux97zgMUCwNFAhdk1? M3;RO|I1ODR3MUe5
NB16 NHnjPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWeyOEBp NYrQR4hrTE2VTx?= MULJR|Ux97zgMUCwNFAhdk1? Mni3NlQxPDVzN{m=
RPE1 NWW1[VU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz2NlQhcA>? NV\neWx[TE2VTx?= MX3JR|Ux97zgMUCwNFAhdk1? NXHxR|ZlOjRyNEWxO|k>

... 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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02941926 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis November 30, 2016 Phase 3
NCT02388620 Completed Normal Hepatic Function|Impaired Hepatic Function Novartis Pharmaceuticals|Novartis March 25, 2015 Phase 1
NCT01872260 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 22, 2013 Phase 1
NCT01237236 Active, not recruiting Advanced Solid Tumor|Lymphomas Novartis Pharmaceuticals|Novartis December 21, 2010 Phase 1
NCT03008408 Not yet recruiting Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma M.D. Anderson Cancer Center|Novartis April 2017 Phase 2
NCT02754011 Recruiting Breast Cancer UNICANCER|Novartis January 2017 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID