2167898-24-8
Chemical Structure
Ribociclib-d8
Synonym(s): LEE011-d8
- CAS No.: 2167898-24-8
- Formula:C23H22D8N8O
- Molecular Weight:442.59
IUPAC Name: N-(4-(4-fluorophenyl)-5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-6-(propan-2-yl-1,1,1,3,3,3-d6)pyrimidin-2-yl)-N-methylmethanesulfonamide
InChIKey: RHXHGRAEPCAFML-PMCMNDOISA-N
SMILES: CN(C)C(C(N(C1CCCC1)C2=N3)=CC2=CN=C3NC4=CC=C(N5C([2H])([2H])C([2H])([2H])NC([2H])([2H])C5([2H])[2H])C=N4)=O
Biological Activity: Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) 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[2].
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Ribociclib-d8 | 99.00% | Ribociclib-d8 is the deuterium labeled Ribociclib. Ribociclib (LEE01) 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. | ||||||||||||||||||||
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Ribociclib (Standard) | 99.76% | Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. Ribociclib (LEE01) 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. | ||||||||||||||||||||
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Ribociclib-d6 | 99.9% | Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). Ribociclib 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. | ||||||||||||||||||||
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Ribociclib | 99.94% | RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex. | ||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. 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. [Content Brief]
