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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Cited by 35 Publications

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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 NWrWXGN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXI[lQzPCCq M{jOdGdKPTB;Mke2JI5O MmDUNlU5PTJyNUi=
Myoblast MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXvZYE4OiCq MUjJR|UxRTFyM{Wgcm0> NF74NYEzPThzMEO3OS=>
IMRS Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInEUG44OiCq MV\JR|UxRTh5MzDuUS=> NX7QUoVPOjV6MUCzO|U>
SKNAS NVLYXXdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIGzNpY4OiCq MmPXTWM2OO,:nkGwNFAxKG6P M3rwb|I2QDFyM{e1
Rh28 NGrGbW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzzU5Q4OiCq Mm\6TWM2OD16NEWgcm0> MUCyOVgyODN5NR?=
Rh41 NHe5R5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvxO|IhcA>? NVv4Z4l[UUN3ME23NVg4KG6P MlLLNlU5OTB|N{W=
CW9019 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[ybVA4OiCq Mme1TWM2OD17OUGyJI5O NGT5XpIzPThzMEO3OS=>
Rh5 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO3NkBp M1jtfmlEPTExvK6xNFAxOCCwTR?= MmmzNlU5OTB|N{W=
Rh30 M33HeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknzO|IhcA>? NIjlfZRKSzVy78{eNVAxODBibl2= MmSwNlU5OTB|N{W=
778 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX23NkBp MoXXbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIf0[HYzPTB{OES2PS=>
449 M3zCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TWblczKGh? MX3pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NVzTVVdyOjVyMki0Olk>
LP3 M2PlZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVe3NkBp NUjsW4Z3cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Ml7PNlUxOjh2Nkm=
LP6 NHS2S|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLQO|IhcA>? Mlz5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml7UNlUxOjh2Nkm=
LP8 NH;WWJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjnO4c4OiCq M2rad4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NH35W5EzPTB{OES2PS=>
LPS141 M3K0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjEeYVLPzJiaB?= NFPUXmlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MYiyOVAzQDR4OR?=
778 MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M324NFMvOzNizszN NF;nU4kzPCCq MWjk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NGn4RpkzPTB{OES2PS=>
449 M3;CU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DVUFMvOzNizszN MYeyOEBp M1HjfoRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M3vHN|I2ODJ6NE[5
LP3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rpWVMvOzNizszN M{HKclI1KGh? Mke0[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NVPCbXNWOjVyMki0Olk>
LP6 NIfsNYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu0cWw{NjN|IN88US=> Mnv0NlQhcA>? MkDv[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NFvLeYEzPTB{OES2PS=>
LP8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz4cok{NjN|IN88US=> MWOyOEBp MlfX[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NV[1e5cxOjVyMki0Olk>
LPS141 MmjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;QdWRWOy5|MzFOwG0> NUXkRphrOjRiaB?= NX3xclI5\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NF3od5UzPTB{OES2PS=>
IMR5 M3PoNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK0fVFMOjRiaB?= MmLnSG1UVw>? MXnJR|UxRTF{NjDuUS=> MVKyOFA1PTF5OR?=
BE2C Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSyOEBp Ml7KSG1UVw>? MXPJR|UxRTF|NDDuUS=> Ml:zNlQxPDVzN{m=
1643 MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX4NlQhcA>? NELXO41FVVOR NYTZNlVbUUN3ME2xOFchdk1? MUiyOFA1PTF5OR?=
SKNSH NELLUJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHq5SVgzPCCq MUjEUXNQ M3nme2lEPTB;MUS4JI5O M2TJRVI1ODR3MUe5
SY5Y NYCwbJFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfEfZczPCCq NGi1N3RFVVOR MnrRTWM2OD1zNUSgcm0> MUmyOFA1PTF5OR?=
NGP NYTqUpFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHyOYVqOjRiaB?= NIXtN5RFVVOR NF\3e5FKSzVyPUG3OUBvVQ>? MXKyOFA1PTF5OR?=
KELLY NVr0Wod5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK5WnozPCCq NHPTb3JFVVOR M{HrdmlEPTB;MkKwJI5O MoDFNlQxPDVzN{m=
CHP134 M2fDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzSNlQhcA>? NIr2XFNFVVOR NID2WHVKSzVyPUK3N{BvVQ>? NEXSfFEzPDB2NUG3PS=>
NLF M1[2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPRdJoyOjRiaB?= MYnEUXNQ MXXJR|UxRTN{ODDuUS=> M4n2O|I1ODR3MUe5
LAN5 M{frfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD6[oEzPCCq MYTEUXNQ NF7SWVlKSzVyPUSyPUBvVQ>? MV2yOFA1PTF5OR?=
NB69 MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nvVFI1KGh? MX3EUXNQ NGfPenZKSzVyPUezPEBvVQ>? MWiyOFA1PTF5OR?=
SKNDZ Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWyOEBp M2\6RWROW09? NG\wfIxKSzVyPUiwNUBvVQ>? M3;xRlI1ODR3MUe5
NBSD M1r3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;YPWpxOjRiaB?= MV3EUXNQ MmL0TWM2OD1zOUCwJI5O MXqyOFA1PTF5OR?=
SKNF1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fiUlI1KGh? MmraSG1UVw>? MYrJR|UxRTN3MECgcm0> MoLENlQxPDVzN{m=
EBC1 NUXYNFQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPZXYgzPCCq MojUSG1UVw>? M3Pke2lEPTB;NkSwNEBvVQ>? M4fZOVI1ODR3MUe5
SKNAS MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6yOEBp MmTCSG1UVw>? MnHYTWM2OO,:nkGwNFAxKG6P NWDtdopJOjRyNEWxO|k>
NB16 MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnFTlB2OjRiaB?= MVrEUXNQ M2f2NGlEPTExvK6xNFAxOCCwTR?= MlnkNlQxPDVzN{m=
RPE1 M{\lSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTIeppXOjRiaB?= MYrEUXNQ MXfJR|Ux97zgMUCwNFAhdk1? NYjDZ|V4OjRyNEWxO|k>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP; 

PubMed: 29789630     


Effect of ribociclib on pRB and G1 cell cycle regulating protein expressions in C666-1 and HK1 cells. Cells were treated with ribociclib in 2 concentrations, one of them near their corresponding IC50, for 24 and 48 hours. Phosphorylation of Rb in all cell䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€𢡄⟼෕€䀷痗⟼෕౴⟼෕

29789630
Growth inhibition assay
Cell viability ; 

PubMed: 26390342     


Effects of palbociclib and ribociclib on viability of H157, H2170, H520 and H596 cells after 72 hours of drug treatment and IC50 values for inhibition of cell viability.

26390342
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]

- Collapse
  • 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]

- Collapse
  • 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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03834740 Recruiting Drug: Ribociclib|Drug: Everolimus Glioblastoma Multiforme|Glioma of Brain St. Joseph''s Hospital and Medical Center Phoenix|Ivy Brain Tumor Center|Barrow Neurological Institute December 21 2018 Early Phase 1
NCT03701334 Recruiting Drug: Ribociclib|Other: Endocrine Therapy Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3
NCT03613220 Recruiting Drug: ribociclib|Drug: letrozole HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis December 28 2018 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID