Ribociclib (LEE011)

Catalog No.S7440

Ribociclib (LEE011) Chemical Structure

Molecular Weight(MW): 434.54

1 Customer Review

  • (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

Choose Selective CDK Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M4TWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqyOEBp MV;HTVUxRTJ5NjDuUS=> NV;RPGxVOjV6NUKwOVg>
Myoblast NI[zcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LGdlczKGh? MofuTWM2OD1zMEO1JI5O NHrhO2wzPThzMEO3OS=>
IMRS M1m4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnSS5E4OiCq MX3JR|UxRTh5MzDuUS=> MlewNlU5OTB|N{W=
SKNAS MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;RVlczKGh? NXTn[m46UUN3MP-8olExODByIH7N NIrOToEzPThzMEO3OS=>
Rh28 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXaO|IhcA>? NWK1TWhIUUN3ME24OFUhdk1? NGT3dJozPThzMEO3OS=>
Rh41 NWH6OlhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnGO|IhcA>? NYTN[I15UUN3ME23NVg4KG6P NU\GbYlsOjV6MUCzO|U>
CW9019 NXXISGo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1i2XFczKGh? NIPjZWVKSzVyPUm5NVIhdk1? MWmyOVgyODN5NR?=
Rh5 NV;uW2F{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUe3NkBp MW\JR|Ux97zgMUCwNFAhdk1? M1z0T|I2QDFyM{e1
Rh30 MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUC3NkBp NVG5SFdEUUN3MP-8olExODByIH7N MofQNlU5OTB|N{W=
778 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPFcoxnPzJiaB?= Mm\KbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MVeyOVAzQDR4OR?=
449 M2TSV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPwO2M4OiCq M1jpSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NVXvXYxXOjVyMki0Olk>
LP3 NHnBbpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfwN4c4OiCq NHPleIdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NYX6RnZiOjVyMki0Olk>
LP6 NULUNVk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKzO|IhcA>? NVXKNFhvcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NEDQT|IzPTB{OES2PS=>
LP8 M{H1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\GXXYzPzJiaB?= M1v6b4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHXCdJMzPTB{OES2PS=>
LPS141 M3\mWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLjO|IhcA>? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2fsRVI2ODJ6NE[5
778 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe3cZFYOy5|MzFOwG0> M2K1WVI1KGh? MWfk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= Mo[5NlUxOjh2Nkm=
449 NFW2Ro5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ZN{4{OyEQvF2= M4ex[FI1KGh? MoDu[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MWKyOVAzQDR4OR?=
LP3 NF7oO4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3hemNNOy5|MzFOwG0> MUWyOEBp MV7k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M1TVdFI2ODJ6NE[5
LP6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInSe3o{NjN|IN88US=> M{PofVI1KGh? M371coRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MoHENlUxOjh2Nkm=
LP8 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\IW|MvOzNizszN M{G4S|I1KGh? NGnSdnVl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MkLPNlUxOjh2Nkm=
LPS141 M4rGW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn23N{4{OyEQvF2= NHnRSY0zPCCq MVLk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MYCyOVAzQDR4OR?=
IMR5 MoPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXiyOEBp NFm5WFZFVVOR NV3OPJhKUUN3ME2xNlYhdk1? MlfuNlQxPDVzN{m=
BE2C NHnrW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXSNlQhcA>? NX;tV|RSTE2VTx?= MUDJR|UxRTF|NDDuUS=> M1;DT|I1ODR3MUe5
1643 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PibFI1KGh? MmrrSG1UVw>? MXLJR|UxRTF2NzDuUS=> M{jWblI1ODR3MUe5
SKNSH NHvUUpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHJUVhROjRiaB?= M4Dk[mROW09? NYX6dYM3UUN3ME2xOFghdk1? NY\R[FR{OjRyNEWxO|k>
SY5Y MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnYVYkzPCCq M{T4XGROW09? NGS3TmhKSzVyPUG1OEBvVQ>? MlPONlQxPDVzN{m=
NGP M1HL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MleyNlQhcA>? MYrEUXNQ NHrkdIxKSzVyPUG3OUBvVQ>? MXSyOFA1PTF5OR?=
KELLY NVHQdJp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHGSnVTOjRiaB?= M1HsN2ROW09? NGrFcXdKSzVyPUKyNEBvVQ>? NHL1TIIzPDB2NUG3PS=>
CHP134 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP6enF7OjRiaB?= M3HTZ2ROW09? M2q2NWlEPTB;MkezJI5O M4XYdlI1ODR3MUe5
NLF Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzVS4IzPCCq NUP2V29lTE2VTx?= MVTJR|UxRTN{ODDuUS=> MV[yOFA1PTF5OR?=
LAN5 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzYR5YzPCCq NWHuSHpCTE2VTx?= NWHMe5V{UUN3ME20Nlkhdk1? NHLhbWwzPDB2NUG3PS=>
NB69 NHW5WIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVeyOEBp NGPU[VFFVVOR NWPJbJRlUUN3ME23N|ghdk1? NUj4eWZCOjRyNEWxO|k>
SKNDZ M{XYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETOPJIzPCCq MVvEUXNQ MV7JR|UxRThyMTDuUS=> MV[yOFA1PTF5OR?=
NBSD MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLNWVhkOjRiaB?= M{n3cGROW09? NE\IcpRKSzVyPUG5NFAhdk1? MmPINlQxPDVzN{m=
SKNF1 M160T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTpPJMzPCCq MnnzSG1UVw>? M1j6XWlEPTB;M{WwNEBvVQ>? NEXyOJAzPDB2NUG3PS=>
EBC1 MnfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LtXFI1KGh? MUPEUXNQ NID5S2ZKSzVyPU[0NFAhdk1? M1PSeVI1ODR3MUe5
SKNAS NGjzeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;qelI1KGh? NHq3VmJFVVOR MV;JR|Ux97zgMUCwNFAhdk1? MnX1NlQxPDVzN{m=
NB16 NXHvPFdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3vTpYzPCCq MYDEUXNQ M3jCSWlEPTExvK6xNFAxOCCwTR?= NWGyeYVMOjRyNEWxO|k>
RPE1 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfZSYs4OjRiaB?= Mo\OSG1UVw>? MnLwTWM2OO,:nkGwNFAxKG6P NWG2PVR5OjRyNEWxO|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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID