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Ribociclib succinate

Catalog No. T15732   CAS 1374639-75-4
Synonyms: LEE011 succinate

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 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 Chemical Structure
Ribociclib succinate, CAS 1374639-75-4
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 47.00
10 mg In stock $ 67.00
25 mg In stock $ 98.00
50 mg In stock $ 117.00
100 mg In stock $ 177.00
200 mg In stock $ 286.00
500 mg In stock $ 509.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 99.57%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 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 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 Tumor growth is obviously delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment. CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models [2].
Synonyms LEE011 succinate
Molecular Weight 552.63
Formula C27H36N8O5
CAS No. 1374639-75-4

Storage

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

Solubility Information

DMSO: 41 mg/mL (74.19 mM), sonification is recommended.

TargetMolReferences 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Approved Drug Library FDA-Approved Drug Library Clinical Compound Library FDA-Approved & Pharmacopeia Drug Library Drug-induced Liver Injury (DILI) Compound Library

Related Products

Related compounds with same targets
SCH900776 (S-isomer) Voruciclib hydrochloride CDK-IN-2 Bisindolylmaleimide X hydrochloride ZCL278 NSC23005 CDK4-IN-2 CP-10

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Keywords

Ribociclib succinate 1374639-75-4 Cell Cycle/Checkpoint CDK LEE 011 Ribociclib inhibit LEE011 LEE-011 Succinate LEE-011 Ribociclib Succinate LEE 011 Succinate Inhibitor LEE011 Succinate Cyclin dependent kinase LEE011 succinate inhibitor

 

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