Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41 mg/mL (74.19 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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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