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CAY10603 (BML-281)

Cat. No. M3888
CAY10603 (BML-281) Structure
Synonym:

BML-281; Isox

Size Price Availability Quantity
10mM*1mL in DMSO USD 110  USD110 In stock
2mg USD 70  USD70 In stock
5mg USD 110  USD110 In stock
10mg USD 175  USD175 In stock
25mg USD 325  USD325 In stock
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Quality Control & Documentation
Biological Activity

CAY10603 (BML-281) prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM). CAY10603 (BML-281) 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.

Protocol (for reference only)
Cell Experiment
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 .
Concentrations ~50 μM
Incubation time 72 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 446.5
Formula C22H30N4O6
CAS Number 1045792-66-2
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Kozikowski AP, et al. J Med Chem. 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.

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  Catalog
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Keywords: CAY10603 (BML-281), BML-281; Isox supplier, HDAC, inhibitors, activators


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