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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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 MmP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjsNHQzPCCq MX7HTVUxRTJ5NjDuUS=> M2fqXFI2QDV{MEW4
Myoblast NHzENlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\tO|IhcA>? NIDxcFRKSzVyPUGwN|Uhdk1? M36yVVI2QDFyM{e1
IMRS NEXnV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXmSlc4OiCq NYj6S2h6UUN3ME24O|Mhdk1? NH73TYczPThzMEO3OS=>
SKNAS M3LZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTPO|IhcA>? M13UfWlEPTExvK6xNFAxOCCwTR?= M3vER|I2QDFyM{e1
Rh28 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ntWlczKGh? NEPScYpKSzVyPUi0OUBvVQ>? MUSyOVgyODN5NR?=
Rh41 NXH2UnVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnVXoQ4OiCq MUHJR|UxRTdzOEegcm0> NVrNemhNOjV6MUCzO|U>
CW9019 NWrCeYdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M170SFczKGh? NGTye5lKSzVyPUm5NVIhdk1? MoHvNlU5OTB|N{W=
Rh5 NI\2dJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzySGE4OiCq MYXJR|Ux97zgMUCwNFAhdk1? NYTsO41{OjV6MUCzO|U>
Rh30 M3LzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;vTlczKGh? MXLJR|Ux97zgMUCwNFAhdk1? MWWyOVgyODN5NR?=
778 NXX1fHpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljJO|IhcA>? M37QSolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mn7BNlUxOjh2Nkm=
449 NYf0So5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnZOIZuPzJiaB?= MnnBbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NETadpczPTB{OES2PS=>
LP3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXHNoI4OiCq Mn7ybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MofGNlUxOjh2Nkm=
LP6 M4POXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHQO|IhcA>? MmnMbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MlH5NlUxOjh2Nkm=
LP8 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfkO|IhcA>? NGDDXpVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NF\kZYgzPTB{OES2PS=>
LPS141 Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjMO|IhcA>? M4fNeolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVyyOVAzQDR4OR?=
778 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLJ[Gg{NjN|IN88US=> NGf0PGwzPCCq NYr0[W9z\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NIW3SpczPTB{OES2PS=>
449 NEfVXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6zMlM{KM7:TR?= NVLGSmxxOjRiaB?= NWjhNlAx\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> MWmyOVAzQDR4OR?=
LP3 M4HlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHzZlJJOy5|MzFOwG0> NGT0VmozPCCq Ml7X[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MXSyOVAzQDR4OR?=
LP6 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz6dW5WOy5|MzFOwG0> MXeyOEBp M2jaTYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NVy3bJY5OjVyMki0Olk>
LP8 NXHTV5hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzLb44{NjN|IN88US=> M{XaUFI1KGh? MWHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MoHHNlUxOjh2Nkm=
LPS141 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXoN{4{OyEQvF2= NFrMVWszPCCq NGDab5Zl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> Mly0NlUxOjh2Nkm=
IMR5 NHi2dVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmxWJMzPCCq M3f6[2ROW09? M3vRVGlEPTB;MUK2JI5O M4fPb|I1ODR3MUe5
BE2C NYH3d|FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXiyOEBp M4fZW2ROW09? MlH4TWM2OD1zM{Sgcm0> Mn;VNlQxPDVzN{m=
1643 NFvWVGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:yOEBp NFfaV3BFVVOR NYnmTmxjUUN3ME2xOFchdk1? Mkj5NlQxPDVzN{m=
SKNSH NUPWN3dKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\Od|d[OjRiaB?= MUfEUXNQ M33BdWlEPTB;MUS4JI5O M1PKZVI1ODR3MUe5
SY5Y MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGyOEBp MlLVSG1UVw>? NILjTZpKSzVyPUG1OEBvVQ>? NIHkd|YzPDB2NUG3PS=>
NGP Mnf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f2SVI1KGh? NYDwPFFRTE2VTx?= MVPJR|UxRTF5NTDuUS=> MWSyOFA1PTF5OR?=
KELLY MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XlSVI1KGh? M1XWWWROW09? Mle5TWM2OD1{MkCgcm0> MoHJNlQxPDVzN{m=
CHP134 NV7zb2pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TWXVI1KGh? MXHEUXNQ NGH6OHVKSzVyPUK3N{BvVQ>? MViyOFA1PTF5OR?=
NLF MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXJNlQhcA>? NX73OphlTE2VTx?= MWLJR|UxRTN{ODDuUS=> MV6yOFA1PTF5OR?=
LAN5 MoP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDSfIUzPCCq NGXXTGRFVVOR Mmn5TWM2OD12Mkmgcm0> MmrZNlQxPDVzN{m=
NB69 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu4d|czPCCq MkLSSG1UVw>? MoH1TWM2OD15M{igcm0> NFzmNGczPDB2NUG3PS=>
SKNDZ MlW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTuTWxxOjRiaB?= MXvEUXNQ NXfMbm1RUUN3ME24NFEhdk1? NUHqXXRwOjRyNEWxO|k>
NBSD NV3CZnBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiyOEBp MYjEUXNQ MU\JR|UxRTF7MECgcm0> M4LjOFI1ODR3MUe5
SKNF1 M1zRb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\DNlQhcA>? MoriSG1UVw>? Mm\DTWM2OD1|NUCwJI5O NXnGW|V7OjRyNEWxO|k>
EBC1 MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvafo0zPCCq M{n2XmROW09? NEewPGpKSzVyPU[0NFAhdk1? NWTVVo5QOjRyNEWxO|k>
SKNAS NYP5dHhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2yOEBp MW\EUXNQ NFLxUXVKSzVy78{eNVAxODBibl2= MUKyOFA1PTF5OR?=
NB16 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqyOEBp M4H6SGROW09? NF23eVZKSzVy78{eNVAxODBibl2= MYKyOFA1PTF5OR?=
RPE1 NI\He5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\1N|I1KGh? NWCweYF7TE2VTx?= NWjEWYtCUUN3MP-8olExODByIH7N NWnoe4NbOjRyNEWxO|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