LEE011 (succinate hydrate)
- Product Name
- LEE011 (succinate hydrate)
- CAS No.
- 1374639-79-8
- Chemical Name
- LEE011 (succinate hydrate)
- Synonyms
- Ribociclib succite hydrate;LEE011 (succinate hydrate);Ribociclib Succinate hydrat;Ribociclib (succinate hydrate);Ribociclib (LEE011) succinate hydrate;RIBOCICLIB SUCCINATE HYDRATE (LEE011 SUCCINATE HYDRATE)
- CBNumber
- CB12682009
- Molecular Formula
- C27H36N8O5
- Formula Weight
- 552.64
- MOL File
- 1374639-79-8.mol
LEE011 (succinate hydrate) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 19 mg/mL (33.30 mM)
- form
- Powder
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- CS-2278
- Product name
- Ribociclibsuccinatehydrate
- Purity
- 99.96%
- Packaging
- 5mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- CS-2278
- Product name
- Ribociclibsuccinatehydrate
- Purity
- 99.96%
- Packaging
- 10mg
- Price
- $84
- Updated
- 2021/12/16
- Product number
- CS-2278
- Product name
- Ribociclibsuccinatehydrate
- Purity
- 99.96%
- Packaging
- 50mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- CS-2278
- Product name
- Ribociclibsuccinatehydrate
- Purity
- 99.96%
- Packaging
- 100mg
- Price
- $216
- Updated
- 2021/12/16
- Product number
- CD31003701
- Product name
- LEE011succinatehydrate
- Purity
- 98+%
- Packaging
- 50mg
- Price
- $315
- Updated
- 2021/12/16
LEE011 (succinate hydrate) Chemical Properties,Usage,Production
Description
LEE011 succinate hydrate is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
in vitro
In Vitro:Treating a panel of 17 neuroblastoma cell lines with LEE011 (Ribociclib) across a four-log dose range (10 to 10,000 nM). Treatment with LEE011 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. LEE011 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 LEE011 concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].
in vivo
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 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[2].
References
References:[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. [2]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
LEE011 (succinate hydrate) Preparation Products And Raw materials
Raw materials
Preparation Products
LEE011 (succinate hydrate) Suppliers
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View Lastest Price from LEE011 (succinate hydrate) manufacturers
- Product
- Ribociclib Succinate 1374639-79-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-08-09
- Product
- LEE011 (succinate hydrate) 1374639-79-8
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 1000kg
- Release date
- 2019-08-31