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Size | Price | Stock |
---|---|---|
500mg | $450 | Check With Us |
1g | $745 | Check With Us |
5g | $2010 | Check With Us |
Cat #: V3925 CAS #: 1374639-75-4 Purity ≥ 98%
Description: Ribociclib succinate (LEE011, NVP-LEE-011; LEE-011, NVP-LEE011; Kisqali), the succinate salt of Ribociclib, is a CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA for the treatment of breast cancer.
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Molecular Weight (MW) | 552.64 |
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Molecular Formula | C27H36N8O5 |
CAS No. | 1374639-75-4 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: ≥ 19 mg/mLr |
Water: N/Ar | |
Ethanol: N/A | |
Synonyms | LEE011 succinate; LEE-011 succinate; LEE 011 succinate; trade name: Kisqali |
Protocol | In Vitro | Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly 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. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in 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 |
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In Vivo | 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 a 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. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.8095 mL | 9.0475 mL | 18.0950 mL | 36.1899 mL |
5mM | 0.3619 mL | 1.8095 mL | 3.6190 mL | 7.2380 mL |
10mM | 0.1809 mL | 0.9047 mL | 1.8095 mL | 3.6190 mL |
20mM | 0.0905 mL | 0.4524 mL | 0.9047 mL | 1.8095 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.