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CDK&Aurora kinase

Ribociclib (LEE011) (1211441-98-3)

LEE011 is an orally available, and highly specific CDK4/6 inhibitor with IC50s of 10 nM and 39 nM, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 1211441-98-3 Category

Ribociclib (LEE011) (1211441-98-3) Description

Ribociclib Free Base, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.

Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle

 

Ribociclib (LEE011) (1211441-98-3) Specifications

Product Name Ribociclib (LEE011)
Synonyms LEE011; LEE-011. LEE 011; Ribociclib.
Chemical Names 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
Purity ≥98% (HPLC)
CAS Number 1211441-98-3
Molecular Formula C23H30N8O
Molecular Weight 434.54
Monoisotopic Mass 434.25426  g/mol
MDL number MFCD27976795
InChIKey RHXHGRAEPCAFML-UHFFFAOYSA-N
InChi Code InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)
SMILES O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C
Form Powder
Color Yellow solid
Solubility  Soluble in DMSO (~10 mg/ml)
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application An orally available, and highly specific CDK4/6 inhibitor

 


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