Medchemexpress LLC Lerociclib dihydrochloride | 2097938-59-3 | 98.5% | 547.52 | 10 MG

Supplier:  Medchemexpress LLC HY112272A10MG

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

• Produces a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC50 of approximately 20 nM.
• Causes a dose-dependent increase of cells in the G1 phase and exhibits complete inhibition of RB phosphorylation.
• Produces robust inhibition of proliferation in various tumor cell lines including breast, melanoma, leukemia, and lymphoma with EC50 concentrations as low as 23 nM.
• Elicits tumor regression in HER2+ breast cancer models.
• Shows tumor growth inhibition in MCF7 xenograft models, with Lerociclib being significantly more efficacious than palbociclib at 50 mg/kg.
• Demonstrates high efficacy in the ER+ ZR-75-1 breast cancer xenograft model and NSCLC tumor model.

Catalog No. 50-004-38565