Ribociclib succinate

CAS No. 1374639-75-4

Ribociclib succinate ( LEE011 succinate )

Catalog No. M22128 CAS No. 1374639-75-4

Ribociclib 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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 27 In Stock
5MG 42 In Stock
10MG 60 In Stock
25MG 88 In Stock
50MG 105 In Stock
100MG 159 In Stock
200MG 257 In Stock
500MG 458 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Ribociclib succinate
  • Note
    Research use only, not for human use.
  • Brief Description
    Ribociclib 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.
  • Description
    Ribociclib 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. 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) .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.
  • Synonyms
    LEE011 succinate
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK4;CDK6
  • Research Area
    Cancer
  • Indication
    Advanced Breast Cancer

Chemical Information

  • CAS Number
    1374639-75-4
  • Formula Weight
    552.63
  • Molecular Formula
    C27H36N8O5
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:41 mg/mL (74.19 mM; Need ultrasonic)
  • SMILES
    OC(=O)CCC(O)=O.CN(C)C(=O)c1cc2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n1C1CCCC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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