CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. 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.Responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay.
Nature. 2018 Jan 4;553(7686):91-95.
Cyclin D–CDK4 kinase destabilizes PD-L1 via Cul3SPOP to control cancer immune surveillance
LEE011 succinate purchased from AbMole
|Source||Nature (2018). Figure 2. Ribociclib (Abmole Bioscience)|
|Cell Lines||4T1 tumor cell lines|
|Incubation Time||36 h|
|Results||"Furthermore, treatment of multiple cancer cell lines with two different selective inhibitors of CDK4/6 kinase, palbociclib or ribociclib, upregulated PD-L1 protein abundance and stability even in pRB knock-down cells."|
|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.
|Solubility||10 mM in DMSO|
LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity.
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GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
EXP-3174 is a potent AT1 antagonist with Kis of 0.57 and 0.67 nM for rat and human forms, respectively.
NAV-2729 is a selective ARF6 inhibitor with IC50 value of 1.0 μM.
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