Ribociclib (LEE011)

Catalog No.S7440

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

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Ribociclib (LEE011) Chemical Structure

Ribociclib (LEE011) Chemical Structure
Molecular Weight: 434.54

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Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
DFSP105MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2[1XFI1KGh?M3vTfmdKPTB;Mke2JI5OMoHqNlU5PTJyNUi=
MyoblastNYrnWZFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnvEO|IhcA>?NWjzNGtVUUN3ME2xNFM2KG6PM4\3bFI2QDFyM{e1
IMRSMYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NHPqeXE4OiCqMWXJR|UxRTh5MzDuUS=>NUf2ZWpiOjV6MUCzO|U>
SKNASMl;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWrtPHFlPzJiaB?=M2qzc2lEPTExvK6xNFAxOCCwTR?=MmKxNlU5OTB|N{W=
Rh28Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUTQNpo3PzJiaB?=NITCdY5KSzVyPUi0OUBvVQ>?MXiyOVgyODN5NR?=
Rh41NUPscW1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3vsVVczKGh?NHrNSmxKSzVyPUexPFchdk1?M{DwfVI2QDFyM{e1
CW9019MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWnZe3M2PzJiaB?=NHfhZmJKSzVyPUm5NVIhdk1?M1;IWVI2QDFyM{e1
Rh5MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVLVOZNDPzJiaB?=MmXHTWM2OO,:nkGwNFAxKG6PMWeyOVgyODN5NR?=
Rh30NEjMOHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYm3NkBpNHfXb4pKSzVy78{eNVAxODBibl2=MnTpNlU5OTB|N{W=
778M1fEd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1G4bVczKGh?NVXXWmdbcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?NFnYZo8zPTB{OES2PS=>
449M{\UeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NY\CSWt3PzJiaB?=MkCybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=>NEHTWXczPTB{OES2PS=>
LP3MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{i4VlczKGh?MYnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5M4K3OVI2ODJ6NE[5
LP6M13oeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M33CbVczKGh?NFLnRZhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6M2O5fVI2ODJ6NE[5
LP8MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2G2ZVczKGh?M3\PeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk>MYGyOVAzQDR4OR?=
LPS141M2nOUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFfmRpA4OiCqMoK4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=>MYGyOVAzQDR4OR?=
778MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWmzMlM{KM7:TR?=MXeyOEBpMVTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?=NXvHTFJTOjVyMki0Olk>
449M2TCeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFmyVmo{NjN|IN88US=>NVjwN254OjRiaB?=NF\sU|Zl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>MUeyOVAzQDR4OR?=
LP3MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3XKTFMvOzNizszNMYmyOEBpNEXITYtl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>M2nrelI2ODJ6NE[5
LP6MmPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFXKcHg{NjN|IN88US=>MVyyOEBpM33pSoRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPlMXiyOVAzQDR4OR?=
LP8M4nqbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NH3pc5o{NjN|IN88US=>MUSyOEBpMlS2[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W=NVnFNW1lOjVyMki0Olk>
LPS141MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlP3N{4{OyEQvF2=NIe2Sm8zPCCqMYnk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?=MVSyOVAzQDR4OR?=
IMR5MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGHyTIwzPCCqMoXNSG1UVw>?MlSwTWM2OD1zMk[gcm0>NYq1So5[OjRyNEWxO|k>
BE2CM1XRTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUL3W4Z{OjRiaB?=M1P2Z2ROW09?MVvJR|UxRTF|NDDuUS=>NXGyRXp3OjRyNEWxO|k>
1643NIPxVlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3LWc|I1KGh?NXTJU2dsTE2VTx?=M2nS[2lEPTB;MUS3JI5OMViyOFA1PTF5OR?=
SKNSHMl3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVG4UpVjOjRiaB?=M37QfWROW09?M3u1bWlEPTB;MUS4JI5OM3rQOFI1ODR3MUe5
SY5YMWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYGyOEBpMl;JSG1UVw>?MWnJR|UxRTF3NDDuUS=>NULucWt6OjRyNEWxO|k>
NGPNUOzTmlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFTFdXgzPCCqNEfGUYZFVVORNFrnenlKSzVyPUG3OUBvVQ>?NXXEPYw{OjRyNEWxO|k>
KELLYMYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Ml[yNlQhcA>?NVfpOFk4TE2VTx?=M1nVcmlEPTB;MkKwJI5ONUfYVWJXOjRyNEWxO|k>
CHP134MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXmyOEBpNVHwRXhUTE2VTx?=Mn;GTWM2OD1{N{Ogcm0>NX\Xc3liOjRyNEWxO|k>
NLFMkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHKwbYwzPCCqMl\aSG1UVw>?MmC2TWM2OD1|Mkigcm0>NHLGTXUzPDB2NUG3PS=>
LAN5Mn31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUXCeFhIOjRiaB?=NI\YU2ZFVVORNEXwbWdKSzVyPUSyPUBvVQ>?M4Xae|I1ODR3MUe5
NB69NHnDSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoLKNlQhcA>?MlqzSG1UVw>?NE[4bnNKSzVyPUezPEBvVQ>?NF62fZMzPDB2NUG3PS=>
SKNDZNHvCRXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M135VFI1KGh?M36xWmROW09?M2LzbWlEPTB;OECxJI5OM1jsRVI1ODR3MUe5
NBSDNYLPfW9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2nPeVI1KGh?MlHOSG1UVw>?NFXEdo5KSzVyPUG5NFAhdk1?M1z2bVI1ODR3MUe5
SKNF1MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVqyOEBpNVfUN5RGTE2VTx?=M{PTfmlEPTB;M{WwNEBvVQ>?MVGyOFA1PTF5OR?=
EBC1NVz0Z|BOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUWxXW9oOjRiaB?=M13DPWROW09?NGXhZY1KSzVyPU[0NFAhdk1?MlrlNlQxPDVzN{m=
SKNASMVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFHLcXAzPCCqMkHjSG1UVw>?NEj5U5pKSzVy78{eNVAxODBibl2=M3nGZ|I1ODR3MUe5
NB16NGHYR|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWLJRVZlOjRiaB?=NFjCdZVFVVORMWDJR|Ux97zgMUCwNFAhdk1?M4WxTVI1ODR3MUe5
RPE1NE\tTodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MojsNlQhcA>?MkDWSG1UVw>?NXnJTIlpUUN3MP-8olExODByIH7NM121Z|I1ODR3MUe5

... 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]
Features Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.

Protocol(Only for Reference)

Cell Assay:

[1]

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.

Animal Study:

[1]

Animal Models Mice bearing BE2C, NB-1643, or EBC1 xenografts.
Formulation 0.5% methylcellulose
Dosages ~200 mg/kg daily
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02657928 Not yet recruiting Estrogen Receptor Positive|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine  ...more Estrogen Receptor Positive|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma Mayo Clinic|National Cancer Institute (NCI) June 2016 Phase 2
NCT02732119 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis June 2016 Phase 1|Phase 2
NCT02703571 Not yet 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 Cance  ...more Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France June 2016 Phase 1|Phase 2
NCT02734615 Recruiting Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis May 2016 Phase 1

view more

Chemical Information

Download Ribociclib (LEE011) SDF
Molecular Weight (MW) 434.54
Formula

C23H30N8O

CAS No. 1211441-98-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 7 mg/mL (16.1 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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