In vitro: Lenalidomide and pomalidomide, targeting cereblon, are immunomodulatory drugs that are clinically effective in the treatment of cancer, including newly diagnosed and relapsed multiple myeloma. Iberdomide contains a glutarimide ring that binds in the try-tryptophan pocket of cereblon and an isoindolinone ring that can interact with both cereblon and substrates. Treatment with Iberdomide results in the loss of Ikaros and Aiolos protein levels with EC50s of 1 nM and 0.5 nM. In vivo: Iberdomide (CC-220) is currently in phase 2 clinical trials for the treatment of systematic lupus erythematosus (SLE) and phase 1b/2a clinical trials for relapsed and refractory multiple myeloma (MM).
|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||30 mg/mL in DMSO|
Urothelial endocytic vesicle recycling and lysosomal degradative pathway regulated by lipid membrane composition.
Grasso EJ, et al. Histochem Cell Biol. 2013 Feb;139(2):249-65. PMID: 23064746.
Differential response of the urothelial V-ATPase activity to the lipid environment.
Grasso EJ, et al. Cell Biochem Biophys. 2011 Sep;61(1):157-68. PMID: 21359951.
LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity.
TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120).
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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