product name CAY10603
Description: CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. It has 271 nM, 252 nM, 0.42 nM, 6851 nM, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively. CAY10603 has potent antiproliferative activity against pancreatic cancer cell lines with IC50 of <1 μM. It could be useful chemical probe to study HDAC biology.
References: J Med Chem. 2008 Aug 14;51(15):4370-3
446.5
Formula
C22H30N4O6
CAS No.
1045792-66-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (11.2 mM)
Solubility (In vivo)
5% DMSO+50% PEG 300+ddH2O: 9 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424767
| In Vitro |
In vitro activity: CAY10603, via inhibition of HDAC6, shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of <1 μM, which can be used as a new molecular probe in exploring HDAC biology Kinase Assay: Purified HDACs are incubated with 1 mM carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25 °C in HDAC assay buffer containing 100 mM HEPES (pH 7.5), 25 mM KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model: ((A+((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve. The standard errors of the IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the formula xf4_FitResultStdError. Cell Assay: The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nM to 50 mM. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay according to the manufacturer’s suggestions. The IC50 values are calculated using XLfit. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2008 Aug 14;51(15):4370-3. |
