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LEE 011
- Ribociclib
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H30N8O
- MW: 434.54
Description
Orally bioavailable and highly selective small-molecule inhibitor of CDK4/6 (mean IC50 value 307 nM in sensitive neuroblastoma-derived cell lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. LEE 011 treatment of BE2C and IMR5 neuroblastoma cell lines with demonstrated sensitivity to CDK4/6 inhibition resulted in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle.
More Information
| Parent CAS No. | 1211441-98-3 |
|---|---|
| Chemical Name | 7-cyclopentyl-N,N-dimethyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide |
| SMILES | C1(NC2=NC=C(N3CCNCC3)C=C2)=NC=C2C=C(C(N(C)C)=O)N(C3CCCC3)C2=N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28) |
| InChiKey | RHXHGRAEPCAFML-UHFFFAOYSA-N |
| CID | 44631912 |
| Short Description | CDK4/6 inhibitor |
References
- J.R. Infante et al. Abstract A276: Phase 1 multicenter, open label, dose-escalation study of LEE011, an oral inhibitor of cyclin-dependent kinase 4/6, in patients with advanced solid tumors or lymphomas. Mol. Cancer Ther. 2013, 12, A276.
- K. Samson. LEE011 CDK Inhibitor showing early promise in drug-resistant cancers. Oncology Times 2014, 36, 39-40.
- J. Rader et al. Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin. Cancer Res. 2013, 19, 6173-6182.
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