General
Preferred name
Ribociclib
Synonyms
LEE-011, NVP-LEE011 ()
LEE011 ()
LEE011 succinate ()
Ribociclib succinate hydrate ()
LEE011 (succinate hydrate) ()
LEE 011 ()
RIBOCICLIB SUCCINATE ()
Ribociclib hydrochloride ()
LEE011 (hydrochloride) ()
LEE011 (succinate) ()
LEE011 hydrochloride ()
LEE011 succinate, Kisqali ()
Ribociclib (LEE011) ()
RIBOCICLIBLEE-011LEE-011A-1277A-1277LEE011N,N-Dimethyl 7-cyclopentyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamideN,N-DIMETHYL 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YLPYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXAMIDE ()
LEE-011 ()
LEE-011A ()
LEE011A ()
NVP-LEE011 ()
LEE-011 SUCCINATE ()
Ribociclib succinate component of kisqali femara co-pack ()
Kisqali ()
LEE011-BBA ()
Birociclib ()
LEE-011-BBA ()
P&D ID
PD010313
CAS
1211441-98-3
1374639-75-4
1211443-80-9
Tags
available
drug
Approved by
EMA
FDA
First approval
2017
Drug indication
Breast cancer
breast carcinoma
Hormone receptor positive and HER2-negative advanced or metastatic breast cancer
Lymphoma
Solid tumour/cancer
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA Inhibition of cyclin-dependent kinase 4 and 6 (CDK4/6) may provide protection against oncogenic processes in specific tissue types. For example, CDK4 is not required for normal mammary tissue development based on knockout mouse studies, but it is needed for growth of Ras-induced mammary tumors, suggesting a potential therapeutic window for treatment with lower toxicity.; Ribociclib was reported to be a most selective CDK4/6 inhibitor and to have dose dependent antitumor activity in a number of preclinical models. It inhibited growth of tumor cells by arresting the cells at the G1 checkpoint, which prevents the tumor cells from proliferating.
ABSORPTION Ribociclib is orally bioavailable, highly selective inhibitor of CDK4/6 kinases with inhibitory IC50 concentrations in the low nanomolar range. ; Following oral dosing, ribociclib was rapidly absorbed with median Tmax ranging from 1 to 5 hours. Plasma concentrations increased approximately 2- to 3-fold from Cycle 1 Day 1 to Cycle 1 Day 18/21 due to accumulation, with steady state reached by approximately Day 8 on the basis of trough concentrations after repeated daily dosing. Dose-proportionality analyses demonstrated that exposure to ribociclib increased with dose, with both Cmax and area under the curve (AUC) increasing slightly more than proportional to dose, over the dose range 50–1,200 mg/day
DESCRIPTION Ribociclib is a selective, orally available inhibitor of the cyclin-dependent kinases CDK4 and CDK6 . (GtoPdb)
DESCRIPTION RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1][1].
PRICE 72
DESCRIPTION Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
PRICE 69
DESCRIPTION Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
DESCRIPTION Kisqali (ribociclib) is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably. (PKIDB)
DESCRIPTION High affinity HDAC4 negative allosteric modulator; also binds S100A9; antiangiogenic (Tocris Bioactive Compound Library)
DESCRIPTION Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM). (TargetMol Bioactive Compound Library)
DESCRIPTION Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex. (TargetMol Bioactive Compound Library)
Cell lines
13
Organisms
0
Compound Sets
31
AdooQ Bioactive Compound Library
A13549
Axon Medchem Screening Library
2273
Cayman Chemical Bioactives
17666
36414
CDK inhibitor database (CDKiDB)
ChEMBL Approved Drugs
CHEMBL3545110
CHEMBL3707266
ChEMBL Drugs
CHEMBL3545110
CHEMBL3707266
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB11730
DrugBank Approved Drugs
DB11730
DrugCentral
5218
DrugCentral Approved Drugs
5218
DrugMAP
DMMX75K
DM9CIUW
DrugMAP Approved Drugs
DM9CIUW
EU-OPENSCREEN Bioactive Compound Library
EOS101280
EUbOPEN Chemogenomics Library
EUB0000686
Guide to Pharmacology
7383
LINCS compound set
10395-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL3545110
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL3545110
MedChem Express Bioactive Compound Library
HY-15777
HY-15777B
HY-15777A
NCATS Inxight Approved Drugs
TK8ERE8P56
NIH Approved Oncology Drugs
440809902
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
lee011
ribociclib-succinate
ribociclib-hydrochloride
TargetMol Bioactive Compound Library
T6199
T15732
Tocris Bioactive Compound Library
7050
External IDs
56
Properties
(calculated by RDKit )
Molecular Weight
434.25
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
3
cLogP
2.8
TPSA
91.21
Fraction CSP3
0.48
Chiral centers
0.0
Largest ring
6.0
QED
0.64
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
CDK4,CDK6
Target
CDK
CDK4
CDK6
VEGFR4
VEGFR6
CDK4, CDK6
CDK4/6 inhibitor
Primary Target
Cyclin-dependent Kinase
Pathway
Cell Cycle/DNA Damage
Cell Cycle/Checkpoint
Angiogenesis
Tyrosine Kinase/Adaptors
MOA
Inhibitor
CDK inhibitor
CDK4 Inhibitors
CDK6 Inhibitors
Jak3 Inhibitors
Member status
virtual
Indication
breast cancer
Recommended Cell Concentration
1 uM
Source data