Ribociclib succinate

SKU: orb1308130

Description

Ribociclib succinate (LEE011 succinate) is a potent and selective inhibitor of CDK4 and CDK6, with IC50 values of 10 nM and 39 nM, respectively, while showing minimal activity against CDK1. It is widely used in cancer research, particularly for studying cell cycle arrest in breast cancer models, both in vitro and in vivo.

Research Area

Cell Biology

Key Properties

• CAS Number: 1374639-75-4
• MW: 552.63
• Purity: 99.90%
• Formula: C₂₇H₃₆N₈O₅
• SMILES: OC(=O)CCC(O)=O.CN(C)C(=O)c1cc2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n1C1CCCC1
• Target: CDK
• Solubility: DMSO:9 mg/mL (16.29 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (0.9 mM)

Bioactivity

• Target IC50:
  CDK4:10 nM|CDK6:39 nM
• 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 .
• 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) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, LEE 011, LEE011 Succinate, LEE011 succinate, LEE-011 Succinate, LEE 011 Succinate, LEE011, LEE-011, inhibit, CDK6, CDK4, CDK, Cyclin dependent kinase, Ribociclib, Ribociclib succinate, Ribociclib Succinate

Compound Identifiers

PubChem CID

57334219