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

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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 NGnNZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrpemRxOjRiaB?= M2D3SWdKPTB;Mke2JI5O NF7McVczPTh3MkC1PC=>
Myoblast NIfMbnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1y2U|czKGh? MnrpTWM2OD1zMEO1JI5O M{fTflI2QDFyM{e1
IMRS NFTOVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVO3NkBp NV3wTXNTUUN3ME24O|Mhdk1? MX:yOVgyODN5NR?=
SKNAS NVr0N29wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXVZWw4OiCq NWntW3p2UUN3MP-8olExODByIH7N NH:xeYczPThzMEO3OS=>
Rh28 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKyO|IhcA>? MXrJR|UxRTh2NTDuUS=> NV7BOY9POjV6MUCzO|U>
Rh41 NEPQOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4WzNFczKGh? NV;EZYFrUUN3ME23NVg4KG6P NWjRV4dQOjV6MUCzO|U>
CW9019 M2nZc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITaRlU4OiCq M3XaRWlEPTB;OUmxNkBvVQ>? NEnNcnMzPThzMEO3OS=>
Rh5 NEPzVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe3NkBp MVzJR|Ux97zgMUCwNFAhdk1? NUfOepdZOjV6MUCzO|U>
Rh30 M2fsOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr4[3ByPzJiaB?= NF7CUnFKSzVy78{eNVAxODBibl2= NVf0XHZlOjV6MUCzO|U>
778 NF\KV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPWO3pTPzJiaB?= MkHXbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NF3YSHMzPTB{OES2PS=>
449 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTMO|IhcA>? NUXOdZBLcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NGqySFUzPTB{OES2PS=>
LP3 M1fnemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X3flczKGh? MXXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NHex[VQzPTB{OES2PS=>
LP6 NYXFSHNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLhO|IhcA>? NFzJbmlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MXiyOVAzQDR4OR?=
LP8 NVuzdZVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD2fnpOPzJiaB?= M1fhV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NGTNeWUzPTB{OES2PS=>
LPS141 NGjOSZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3PO|IhcA>? NEKzOoxqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M1HBPFI2ODJ6NE[5
778 NWTjToViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmzMlM{KM7:TR?= M1;WTFI1KGh? NXzLZ2M2\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MnnsNlUxOjh2Nkm=
449 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUizMlM{KM7:TR?= NVjQUos4OjRiaB?= Mnr1[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MnvNNlUxOjh2Nkm=
LP3 NX;tSm0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK2N3g{NjN|IN88US=> MWOyOEBp M4jXTYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NHnNV2kzPTB{OES2PS=>
LP6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i5c|MvOzNizszN MlnLNlQhcA>? Mo\6[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MmL0NlUxOjh2Nkm=
LP8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jYclMvOzNizszN M2\FT|I1KGh? Mlqz[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NID2TpQzPTB{OES2PS=>
LPS141 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHxN{4{OyEQvF2= MlK1NlQhcA>? MXfk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MmfsNlUxOjh2Nkm=
IMR5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLQUpdyOjRiaB?= MW\EUXNQ MnPnTWM2OD1zMk[gcm0> MnzXNlQxPDVzN{m=
BE2C NHi3OJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TGWlI1KGh? M1fH[mROW09? NUXWSlB6UUN3ME2xN|Qhdk1? MYeyOFA1PTF5OR?=
1643 NHf1R2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mni4NlQhcA>? NVfpNFBrTE2VTx?= Mn:0TWM2OD1zNEegcm0> MYSyOFA1PTF5OR?=
SKNSH MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPtRo8zPCCq M1iweWROW09? M1;6UWlEPTB;MUS4JI5O MknENlQxPDVzN{m=
SY5Y MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn2NlQhcA>? Mlf2SG1UVw>? M4noTmlEPTB;MUW0JI5O MnLWNlQxPDVzN{m=
NGP NU\5cWh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXeyOEBp NYnEcINZTE2VTx?= NH74bm5KSzVyPUG3OUBvVQ>? NYOx[I9COjRyNEWxO|k>
KELLY M2rUSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1njPVI1KGh? Ml\vSG1UVw>? M3HJNWlEPTB;MkKwJI5O MVuyOFA1PTF5OR?=
CHP134 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\sNlQhcA>? M{TNbGROW09? NFjOR5JKSzVyPUK3N{BvVQ>? MUOyOFA1PTF5OR?=
NLF NXfKbJpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DQW|I1KGh? NWDlcnVzTE2VTx?= MV7JR|UxRTN{ODDuUS=> Moi5NlQxPDVzN{m=
LAN5 NUTsc2RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrqWIx1OjRiaB?= MVPEUXNQ MkXLTWM2OD12Mkmgcm0> M3PIT|I1ODR3MUe5
NB69 M1rVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XtXlI1KGh? NUPCRoVRTE2VTx?= MnPlTWM2OD15M{igcm0> M1jmPVI1ODR3MUe5
SKNDZ M175XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmyOEBp MV;EUXNQ MXnJR|UxRThyMTDuUS=> M1PrflI1ODR3MUe5
NBSD Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3YWm01OjRiaB?= MoDQSG1UVw>? M1jlOWlEPTB;MUmwNEBvVQ>? NG\4SXMzPDB2NUG3PS=>
SKNF1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;SNlI1KGh? NEnp[GlFVVOR MXzJR|UxRTN3MECgcm0> NUXUSm06OjRyNEWxO|k>
EBC1 NFLwellIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XVbVI1KGh? MnjUSG1UVw>? M1P5N2lEPTB;NkSwNEBvVQ>? M{\0OlI1ODR3MUe5
SKNAS M3[zV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTOOmZSOjRiaB?= NIjGSmdFVVOR M3HydmlEPTExvK6xNFAxOCCwTR?= M{H1TFI1ODR3MUe5
NB16 M2jkVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD2TZJDOjRiaB?= M2DkTmROW09? NWP6d|FpUUN3MP-8olExODByIH7N NXjQdnVSOjRyNEWxO|k>
RPE1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HK[FI1KGh? NVf6eIgzTE2VTx?= MXPJR|Ux97zgMUCwNFAhdk1? NVqwZpl2OjRyNEWxO|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
+ 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
+ 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
NCT02657928 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 2016 Phase 2
NCT02780128 Recruiting Neuroblastoma|Cancer Yael P Mosse|Novartis Pharmaceuticals|Foundation Medicine|Childrens Hospital of Philadelphia July 2016 Phase 1
NCT02734615 Recruiting Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 2016 Phase 1
NCT02732119 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis June 2016 Phase 1|Phase 2
NCT02703571 Recruiting Solid Tumors|Pancreatic Cancer|Colorectal Cancer Novartis Pharmaceuticals|Novartis June 2016 Phase 1|Phase 2
NCT02813135 Recruiting Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France June 2016 Phase 1|Phase 2

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID