LY2835219 is a potent and selective CDK4/6 dual inhibitor with potential antineoplastic activity. CDK4/6 dual inhibitor LY2835219 has been shown in vitro to be a selective ATP-competitive inhibitor of CDK4/6 that inhibits phosphorylation of the Rb tumor suppressor protein and thereby induces G1 cell cycle arrest. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. LY2835219 is being investigated in a phase I clinical trial and in a clinical trial for the treatment of mantle cell lymphoma.
Cancer Cell. 2018 Aug 16;pii: S1535-6108(18)30318-0.
Identification of Therapeutic Targets in Rhabdomyosarcoma through Integrated Genomic, Epigenomic, and Proteomic Analyses.
LY2835219 purchased from AbMole
|Source||Cancer Cell (2018). Figure 5. abemaciclib (Abmole Bioscience, Houston, USA)|
|Results||Mice treated with IRN + VCR had stable disease (SD), whereas mice treated with either palbociclib + trametinib or abemaciclib + trametinib exhibited progressive disease.|
|Source||Invest New Drugs (2014). Figure 2. LY2835219|
|Cell Lines||MCF10A cells|
|Results||LY2835219 induced a G1 arrest in Rb-proficient MDA-MB-231 breast cancer cells, whereas no such effect was seen in Rb-deficient MDA-MB-468 breast cancer cells at compound concentrations up to 2,500 nmol/L|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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