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MS-275

Cat. No. M1791
MS-275 Structure
Synonym:

Entinostat, SNDX-275, MS-27-275

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 36  USD40 In stock
10mg USD 36  USD40 In stock
50mg USD 81  USD90 In stock
100mg USD 117  USD130 In stock
200mg USD 189  USD210 In stock
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Quality Control
Biological Activity

MS-275 (Entinostat) is a potent Histone Deacetylase inhibitor with IC50 value of 0.3 and 8µM for HDAC1 and HDAC3 respectively. It inhibited in vitro cell growth in all cell lines tested with an IC50 ranging from 50 nM to 1.3 uM. MS-275 showed antiproliferative activity against all human breast cancer cell lines examined and induced TbRII mRNA, but not TGF-b type I receptor mRNA. MS-275 caused an accumulation of acetylated histones H3 and H4 in total cellular chromatin. An increase in the accumulation of acetylated histones H3 and H4 was detected in the TbRII promoter after treatment with MS-275.

Product Citations
Customer Product Validations & Biological Datas
Source Int J Clin Exp Pathol (2015). Figure 2. MS-275
Method i.v.
Cell Lines Sprague-Dawley rats
Concentrations 12.3, 24.5, 49.0 mg/kg
Incubation Time 7 days
Results There was no hepatocytic macrovesicular steatosis, lobular inflammatory cell infiltration and necrosis in both control group and MS-275 group
Protocol
Cell Experiment
Cell lines HDACi-treated Y79, Weri-Rb1, and Y79-LUC human RB cell lines
Preparation method Cell survival assays. For colorimetric analysis, cells were exposed to WST-8 Cell Proliferation Reagent (Dojindo), and absorbance was quantified after 2 h using a SpectraMax microplate reader (Molecular Devices). For bioluminescence analysis (Y79-LUC cells only), cells were exposed to 150 μg/mL D-luciferin, and plates were imaged in an IVIS Imaging System (Xenogen) using a 15-s exposure. Luminescence was quantified using Living Image software (Xenogen). For both assays, cell survival was expressed as a percentage of vehicle-treated control values.
Concentrations 0~100 μM
Incubation time 24, 48, or 72 h
Animal Experiment
Animal models LHβ-Tag mice model
Formulation DMSO
Dosages every other day for 21 d with 20 mg/kg MS-275
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 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.

Chemical Information
Molecular Weight 376.4
Formula C21H20N4O3
CAS Number 209783-80-2
Purity 99.36%
Solubility DMSO 45 mg/mL
Storage -20°C, sealed
References

Histone deacetylase inhibitors suppress mechanical stress-induced expression of RUNX-2 and ADAMTS-5 through the inhibition of the MAPK signaling pathway in cultured human chondrocytes.
Saito T, et al. Osteoarthritis Cartilage. 2012 Sep 24. PMID: 23017871.

MS-275 sensitizes osteosarcoma cells to Fas ligand-induced cell death by increasing the localization of Fas in membrane lipid rafts.
Rao-Bindal K, et al. Cell Death Dis. 2012 Aug 9;3:e369. PMID: 22875006.

MS-275, a benzamide histone deacetylase inhibitor, prevents osteoclastogenesis by down-regulating c-Fos expression and suppresses bone loss in mice.
Kim HN, et al. Eur J Pharmacol. 2012 Sep 15;691(1-3):69-76. PMID: 22846626.

P38 MAP kinase functions as a switch in MS-275-induced reactive oxygen species-dependent autophagy and apoptosis in human colon cancer cells.
Zhan Y, et al. Free Radic Biol Med. 2012 Aug 1;53(3):532-43. PMID: 22634147.

MS-275, an Histone Deacetylase Inhibitor, Reduces the Inflammatory Reaction in Rat Experimental Autoimmune Neuritis
Z Y Zhang, et al. Neuroscience. 2010 Aug 11;169(1):370-7. PMID: 20451583.

Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma.
Dalgard CL, et al. Clin Cancer Res. 2008 May 15;14(10):3113-23. PMID: 18483379.

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Keywords: MS-275, Entinostat, SNDX-275, MS-27-275 supplier, HDAC, inhibitors

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