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Ribociclib succinate

Catalog No. T15732Cas No. 1374639-75-4
Alias LEE011 succinate

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex.

Ribociclib succinate

Ribociclib succinate

Purity: 99.90%
Catalog No. T15732Alias LEE011 succinateCas No. 1374639-75-4
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex.
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$47In Stock
10 mg$67In Stock
25 mg$98In Stock
50 mg$117In Stock
100 mg$177In Stock
200 mg$286In Stock
500 mg$509In Stock
1 mL x 10 mM (in DMSO)$58In Stock
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Purity:99.90%
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Product Introduction

Bioactivity
Description
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency 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 significantly delayed during 21 days of Ribociclib (LEE011; 200 mg/kg) treatment in mice with BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment. CB17 immunodeficient mice with BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts received daily treatment with Ribociclib or vehicle control, with no observed weight loss or toxicity signs in any models [2].
AliasLEE011 succinate
Chemical Properties
Molecular Weight552.63
FormulaC27H36N8O5
Cas No.1374639-75-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 9 mg/mL (16.29 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8095 mL9.0476 mL18.0953 mL90.4764 mL
5 mM0.3619 mL1.8095 mL3.6191 mL18.0953 mL
10 mM0.1810 mL0.9048 mL1.8095 mL9.0476 mL

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