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.
|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|
|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."|
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
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
Pancreatic enzymes also known as pancrelipase and pancreatin, are commercial mixtures of amylase, lipase, and protease. They are used to treat malabsorption syndrome due to pancreatic problems.
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Treatment with the kinin B1 receptor antagonist, SSR240612, provided a protective effect against organ damage by interfering with multiple target functions, including the suppression of B1R-induced inflammation and platelet aggregation.
KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.