A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor (nm IC50) that inhibits retinoblastoma protein phosphorylation

LEE011 – 500 µg

Brand:
Cayman
CAS:
1211441-98-3
Storage:
-20
UN-No:
Non-Hazardous - /

LEE011 is a cyclin-dependent kinase (CDK) inhibitor that targets cyclin D1/CDK4 and cyclin D3/CDK6 at nanomolar concentrations.{28690,28691,28692} It inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth.{28692} LEE011 has been shown to reduce proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis (mean IC50 = 306 nM in sensitive lines).{28692}  

 

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Description

A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor (nm IC50) that inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth; reduces proliferation of several human neuroblastoma-derived cell lines (mean IC50 = 306 nM)

Formal name: 7-​cyclopentyl-​N,​N-​dimethyl-​2-​[[5-​(1-​piperazinyl)​-​2-​pyridinyl]​amino]​-7H-​pyrrolo[2,​3-​d]​pyrimidine-​6-​carboxamide

Synonyms:  Ribociclib

Molecular weight: 434.5

CAS: 1211441-98-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling

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