CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM). CAY10603 shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of <1 μM. CAY10603 can be used as a new molecular probe in exploring HDAC biology.
|Cell lines||BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 cells|
|Preparation method||Growing the pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 in medium (DMEM or RPMI) which contains 10% fetal calf serum and l-glutamine. Plating pancreatic cancer cells out in duplicate into 6 wells of a 96-well microtiter plate. Four hours post plating, treting individual wells with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nM to 50 mM.Measuring cytotoxicity at time “0”, and 72 h post treatment using the colorimetric MTT assay according to the manufacturer’s suggestions. Using XLfit to calculate the IC50 values .|
|Incubation time||72 hours|
|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.
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
Kozikowski AP, et al. J Med Chem. 2008 Aug 14;51(15):4370-3. PMID: 18642892.
|Related HDAC Products|
Givinostat is an HDAC inhibitor with IC50s of 198 and 157 nM for HDAC1 and HDAC3, respectively.
Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM.
HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs.
HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines.
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