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Ribociclib hydrochloride

Catalog No. T15730 CAS 1211443-80-9

Synonyms: LEE011 hydrochloride

Ribociclib hydrochloride is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It is over 1,000-fold less potent against the cyclin B/CDK1 complex.

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Ribociclib hydrochloride Chemical Structure

Ribociclib hydrochloride, CAS 1211443-80-9

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2 mg	5 days	$ 39.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ribociclib hydrochloride is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It is over 1,000-fold less potent against the cyclin B/CDK1 complex.
Targets&IC50	CDK4:10 nM, CDK6:39 nM
In vitro	Ribociclib hydrochloride 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. 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 (200 mg/kg) daily for 21 days significantly delays tumor growth in CB17 immunodeficient mice bearing BE2C or NB-1643 (MYCN amplified, sensitive in vitro) xenografts, with notable effects observed through the treatment period (p<0.0001 for both). However, tumor growth resumes after cessation of treatment. The regimen, also applied to EBC1 (non-amplified, resistant in vitro) xenografts for comparison, demonstrates a favorable safety profile across all xenograft models, indicated by the absence of weight loss or toxicity signs [2].

Synonyms	LEE011 hydrochloride
Molecular Weight	471
Formula	C23H31ClN8O
CAS No.	1211443-80-9

Storage

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

Solubility Information

H2O: 10 mg/mL (21.23 mM), Sonification is recommended.

DMSO: 7.69 mg/mL (16.33 mM), Sonification is recommended.

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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ribociclib hydrochloride 1211443-80-9 Cell Cycle/Checkpoint CDK LEE-011 Hydrochloride LEE011 hydrochloride LEE011 Hydrochloride Ribociclib Hydrochloride LEE 011 Hydrochloride inhibitor inhibit

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