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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2 Customer Reviews

  • (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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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 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTyc4ozPCCq M{\h[GdKPTB;Mke2JI5O NFjTdFgzPTh3MkC1PC=>
Myoblast NIf3cYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G5TVczKGh? NFzEV4JKSzVyPUGwN|Uhdk1? NGmwW|kzPThzMEO3OS=>
IMRS NEXZe4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jOV|czKGh? M1fYVGlEPTB;OEezJI5O M2DMR|I2QDFyM{e1
SKNAS M3z6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XVUFczKGh? NFnDeoxKSzVy78{eNVAxODBibl2= M3vFPVI2QDFyM{e1
Rh28 NHjReHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfpcYNUPzJiaB?= MVvJR|UxRTh2NTDuUS=> MkPyNlU5OTB|N{W=
Rh41 NFXIdmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37Qc|czKGh? MY\JR|UxRTdzOEegcm0> NWHXdm1MOjV6MUCzO|U>
CW9019 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLvO|IhcA>? M1TmOWlEPTB;OUmxNkBvVQ>? NE\nN4szPThzMEO3OS=>
Rh5 NGnoW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPiO|IhcA>? M1jrV2lEPTExvK6xNFAxOCCwTR?= MlXPNlU5OTB|N{W=
Rh30 NXT6XY9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV23NkBp NUPPXGQ{UUN3MP-8olExODByIH7N NWLTVnZQOjV6MUCzO|U>
778 M3LuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P5bVczKGh? MlXpbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1jubVI2ODJ6NE[5
449 M3fyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG3NkBp NF3QbWJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NH:4dWUzPTB{OES2PS=>
LP3 M4DySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLaO|IhcA>? M3LnU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MlnLNlUxOjh2Nkm=
LP6 NYXuTnNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\hWXpqPzJiaB?= NUm4OGZ5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NXnqU403OjVyMki0Olk>
LP8 NH\hWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC3NkBp NX\lZlREcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MYeyOVAzQDR4OR?=
LPS141 M2HFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:3NkBp NFvmRndqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NF\PPZkzPTB{OES2PS=>
778 NGXy[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvBb|NuOy5|MzFOwG0> MVGyOEBp MkHp[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NW[wWmNTOjVyMki0Olk>
449 M1q0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCzMlM{KM7:TR?= M1;6[|I1KGh? M13wT4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NXHtc4dqOjVyMki0Olk>
LP3 M1nsdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS1e2ZqOy5|MzFOwG0> MVGyOEBp M1fTNIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M2i1XVI2ODJ6NE[5
LP6 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfzZ2E{NjN|IN88US=> M2r4[FI1KGh? MVTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MoHYNlUxOjh2Nkm=
LP8 NV7mbopRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv5U4E{NjN|IN88US=> MWGyOEBp NHfrXG1l\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MlmzNlUxOjh2Nkm=
LPS141 MlP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPueFA{NjN|IN88US=> MlXHNlQhcA>? NXjyOlZM\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MXWyOVAzQDR4OR?=
IMR5 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTUfnYzPCCq M33CVmROW09? NV\jO5RVUUN3ME2xNlYhdk1? Mlr2NlQxPDVzN{m=
BE2C MkPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i0XVI1KGh? NInv[|FFVVOR NF\UOHNKSzVyPUGzOEBvVQ>? MWSyOFA1PTF5OR?=
1643 NHX6WY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:1PWQzPCCq M4SzN2ROW09? NFrWd4dKSzVyPUG0O{BvVQ>? M2K1VFI1ODR3MUe5
SKNSH Mk\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe2e|B6OjRiaB?= NUjZfGtqTE2VTx?= NFzBflNKSzVyPUG0PEBvVQ>? NIPZNHYzPDB2NUG3PS=>
SY5Y MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljYNlQhcA>? NF7L[GFFVVOR M2q2bmlEPTB;MUW0JI5O M4nOSFI1ODR3MUe5
NGP M{DzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqyOEBp Mk\DSG1UVw>? NHqyUXhKSzVyPUG3OUBvVQ>? MmjLNlQxPDVzN{m=
KELLY NFfaRmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fCbFI1KGh? NX;YPZNCTE2VTx?= NGC1SmZKSzVyPUKyNEBvVQ>? NWHyTmpbOjRyNEWxO|k>
CHP134 NETXNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3pNlQhcA>? Mk[wSG1UVw>? M4DrOmlEPTB;MkezJI5O MV2yOFA1PTF5OR?=
NLF NF7qT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO0NlQhcA>? MojoSG1UVw>? M{TKSWlEPTB;M{K4JI5O MoX4NlQxPDVzN{m=
LAN5 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[3cJRYOjRiaB?= NIHOeGFFVVOR M1K5OWlEPTB;NEK5JI5O MUGyOFA1PTF5OR?=
NB69 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHJNlQhcA>? NUGzd5lXTE2VTx?= M2rxfWlEPTB;N{O4JI5O M336XFI1ODR3MUe5
SKNDZ M4PyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrOd5MxOjRiaB?= M1jYVGROW09? MoH5TWM2OD16MEGgcm0> MWGyOFA1PTF5OR?=
NBSD NWDGd|dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSyOEBp MkG2SG1UVw>? M33UWmlEPTB;MUmwNEBvVQ>? MXuyOFA1PTF5OR?=
SKNF1 NGmz[4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G4dVI1KGh? NHHVOI9FVVOR NYXrS5R[UUN3ME2zOVAxKG6P MYCyOFA1PTF5OR?=
EBC1 NXfBW4JRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLjXJIzPCCq M2HqOmROW09? MkXuTWM2OD14NECwJI5O MVSyOFA1PTF5OR?=
SKNAS M4rueWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXJVWZiOjRiaB?= MkC0SG1UVw>? MWjJR|Ux97zgMUCwNFAhdk1? M2nrTVI1ODR3MUe5
NB16 M323fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\BNWVUOjRiaB?= MmrQSG1UVw>? MWDJR|Ux97zgMUCwNFAhdk1? M37zb|I1ODR3MUe5
RPE1 M{fzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v3XFI1KGh? MVzEUXNQ Ml\QTWM2OO,:nkGwNFAxKG6P NVPlRoQ4OjRyNEWxO|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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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
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