Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

CDK5-p35:287 nM, JNK3:389 nM, GSK-3β:192 nM, PIM2:3400 nM, CDK5-p25:355 nM, HIPK2:31 nM, FLT3:3960 nM, CDK2-CyclinE:504 nM, CDK4:2 nM, CDK6:10 nM, CDK1-cyclinB1:1627 nM, FLT3 (D835Y):403 nM, CDK7-CyclinH-MAT1:3910 nM, DRAK1:659 nM, DYRK2:61 nM, PIM1:50 nM, CK2:117 nM, CDK9-CyclinT1:57 nM

In subcutaneous and intracranial glioma models (U87 mg), MsOH treatment results in LY2835219 inhibiting tumor growth in a dose-dependent manner.

In retinoblastoma, LY2835219 inhibits cancer cell growth by specifically targeting and inhibiting CDK4 and CDK6, leading to cell cycle arrest at the G1 phase and suppression of DNA synthesis.

Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.

LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.