Cas No.: | 1628256-23-4 |
Chemical Name: | Lerociclib |
Synonyms: | G1T 38 |
SMILES: | C1(CNC(=O)C2N1C1C(C=2)=CN=C(NC2=NC=C(N3CCN(C(C)C)CC3)C=C2)N=1)1CCCCC1 |
Formula: | C26H34N8O |
M.Wt: | 474.613 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively; shows weak inhibitory effect on CDK9/cyclin T (IC50=28 nM) and CDK5/p35 (IC50=832 nM), >1,000-fold selectivity over CDK1/2/7; decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines; demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model. |