Free shipping on all orders over $ 500

Droxinostat

Cat. No. M1993

Droxinostat Structure
Size Price Availability Quantity
10mg USD 97 In stock
50mg USD 395 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by down-regulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). Droxinostat also downregulated c-FLIP expression, induced caspase-8- and caspase-3/7-mediated apoptosis, and increased apoptosis in bicalutamide-treated cells. Droxinostat shows a significant action on gene transcription hence controlling tumor progression. Droxinostat (10 μM - 100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis in MCF-7 breast cancer cells. In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.

Protocol
Cell Experiment
Cell lines PPC-1 cells
Preparation method Viability of PPC-1 cells treated with 5809354 or 7271570 (0, 20, 40, 60, and 80 μM) with and without CH-11 (100 ng/mL) or cultured under adherent or suspension conditions and MEFs treated with 5809354 (0, 20, 40, 60, and 80 μM) under adherent or suspension conditions was assessed using the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium inner salt reduction assay (Promega, Madison, WI) according to the manufacturer's protocols as previous described (18). The percent relative cell viability was expressed as (optical density of treated cells/optical density of controls) × 100%. Two independent experiments were performed in triplicate (n = 6).
Concentrations 0, 20, 40, 60, and 80 μM
Incubation time 30 h
Animal Experiment
Animal models male SCID mice between 5 and 7 weeks of age prostate cancer cells in vivo
Formulation PBS
Dosages 30 μM
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 243.69
Formula C11H14ClNO3
CAS Number 99873-43-5
Purity >99%
Solubility DMSO 40 mg/mL
Ethanol 40 mg/mL
Storage at -20°C
References

Elevation of c-FLIP in castrate-resistant prostate cancer antagonizes therapeutic response to androgen receptor-targeted therapy.
McCourt C, et al. Clin Cancer Res. 2012 Jul 15;18(14):3822-33. PMID: 22623731.

4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide (CMH) targets mRNA of the c-FLIP variants and induces apoptosis in MCF-7 human breast cancer cells.
Bijangi-Vishehsaraei K, et al. Mol Cell Biochem. 2010 Sep;342(1-2):133-42. PMID: 20446019.

Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands.
Wood TE, et al. Mol Cancer Ther. 2010 Jan;9(1):246-56. PMID: 20053768.

Critical role for Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein in anoikis resistance and distant tumor formation.
Mawji IA, et al. J Natl Cancer Inst. 2007 May 16;99(10):811-22. PMID: 17505076.

Related HDAC Products
WT161

WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.

EDO-S101

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.

Citarinostat

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.

BRD73954

BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

Sodium Butyrate

Sodium butyrate is the sodium salt of butyric acid, which has been reported to cause hyperacetylation of histones due to its role as a HDAC inhibitor with IC50 values of 0.3, 0.4, 0.3 mM for HDAC1, 2 and 7 respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Droxinostat supplier, HDAC, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.