Captisol is a unique reproducible mixture of polyanionic β-cyclodextrin derivatives in which a sodium sulfonate salt is tethered to the lipophilic cyclodextrin cavity by a butyl ether group, or sulfobutylether (SBE). The sulfobutyl ether (SBE) substituent is introduced at the 2, 3, and 6 positions in one or more of the glucopyranose units in the cyclodextrin structure.
|Cell lines||Caco-2 cells|
|Preparation method||The cells were then preincubated for 30 min without Nos solution+permeation enhancer CH or CP and then incubated for 120 min at 37 ℃ with the Nos solution (50 mg/ml)+permeation enhancer CH or CP.|
|Incubation time||2 h|
|Formulation||10-mL solution composed of 25% water and 75% PEG400|
|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||Water > 100 mg/ml|
Int J Cancer. 2013 Nov;133(9):2065-76.
Combined targeting of AKT and mTOR using MK-2206 and RAD001 is synergistic in the treatment of cholangiocarcinoma.
Captisol purchased from AbMole
Humanized vascular endothelial growth factor (VEGF) antibody (bevacizumab; Avastin) is a highly effective monoclonal antibody against metastatic colorectal cancer and several other advanced late stage cancers.
MCC950 is a potent, selective NLRP3 inhibitor with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
MAK683, an epigenetic drug for nasopharyngeal carcinoma, which is more prevalent in China than elsewhere, has entered Phase I clinical trials.
MTX-211 is a enamide hydrate.
GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain.
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