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|
Chidamide is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
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