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Size | Price | Stock |
---|---|---|
1g | $420 | Check With Us |
2g | $680 | Check With Us |
5g | $1200 | Check With Us |
Cat #: V3924 CAS #: 1211443-80-9 Purity ≥ 98%
Description: Ribociclib HCl (formerly also known as LEE-011, NVP-LEE011; Kisqali), the hydrochloride salt of Ribociclib, is an orally bioavailable CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA to treat postmenopausal women with a type of advanced breast cancer.
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Molecular Weight (MW) | 471.01 |
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Molecular Formula | C23H31ClN8O |
CAS No. | 1211443-80-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: >10 mMr |
Water: N/Ar | |
Ethanol: N/A | |
Synonyms | NVP-LEE011; LEE011; LEE-011; LEE011 HCl; LEE-011 HCl; LEE 011 HCl; 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 | 2.1231 mL | 10.6155 mL | 21.2310 mL | 42.4619 mL |
5mM | 0.4246 mL | 2.1231 mL | 4.2462 mL | 8.4924 mL |
10mM | 0.2123 mL | 1.0615 mL | 2.1231 mL | 4.2462 mL |
20mM | 0.1062 mL | 0.5308 mL | 1.0615 mL | 2.1231 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.