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Ribociclib succinate hydrate

Catalog No. T15731 CAS 1374639-79-8

Synonyms: LEE011 succinate hydrate

Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.

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Ribociclib succinate hydrate Chemical Structure

Ribociclib succinate hydrate, CAS 1374639-79-8

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Biological Description

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Description	Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
Targets&IC50	CDK4:10 nM, CDK6:39 nM
In vitro	Ribociclib succinate hydrate treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition causes a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively. Treatment with Ribociclib obviously 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. Treating a panel of 17 neuroblastoma cell lines with Ribociclib across a four-log dose range (10 to 10,000 nM) [2].
In vivo	Treatment with Ribociclib (LEE011; 200 mg/kg) or vehicle control for 21 days significantly delayed tumor growth in CB17 immunodeficient mice bearing BE2C or NB-1643 (MYCN amplified, sensitive in vitro) xenografts, with both groups showing a marked growth inhibition (p<0.0001); however, tumor growth resumed after the treatment period. This study also included EBC1 (non-amplified, resistant in vitro) xenografts in the treatment regimen. The daily dosing of Ribociclib was well tolerated across all xenograft models, with no observed weight loss or signs of toxicity [2].

Synonyms	LEE011 succinate hydrate
Molecular Weight	570.651
Formula	C27H38N8O6
CAS No.	1374639-79-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 19 mg/mL (33.30 mM)

References and Literature

1. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. 2. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.

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Indisulam Kobophenol A Roniciclib XL413 CDK9-IN-1 XL413 hydrochloride CDK7-IN-25 Avotaciclib

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Keywords

Ribociclib succinate hydrate 1374639-79-8 Cell Cycle/Checkpoint CDK LEE011 succinate hydrate LEE011 succinate Hydrate Ribociclib succinate Hydrate inhibitor inhibit

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