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[CAS NO. 209783-80-2]  Entinostat

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PRODUCTS SPECIFICATIONS [209783-80-2]

Catalog
HY-12163
Brand
MCE
CAS
209783-80-2

DESCRIPTION [209783-80-2]

Overview

MDLMFCD08272435
Molecular Weight376.41
Molecular FormulaC21H20N4O3
SMILESO=C(NCC1=CC=C(C=C1)C(NC2=CC=CC=C2N)=O)OCC3=CC=CN=C3

For research use only. We do not sell to patients.

32 Publications Citing Use of MCE


Summary

Entinostat is an oral and selective class I HDAC inhibitor, with IC 50 s of 243 nM, 453 nM, and 248 nM for HDAC1 , HDAC2 , and HDAC3 , respectively.


IC50 & Target

HDAC1

243 nM (IC 50 )

HDAC3

248 nM (IC 50 )

HDAC2

453 nM (IC 50 )


In Vitro

Binding affinity of Entinostat (MS-275) against HDAC1 and HDAC2 is 282 nM and 156 nM, respectively [1] . Effects of the HDAC inhibitor Entinostat (MS-275) have been examined in human leukemia and lymphoma cells (U937, HL-60, K562, and Jurkat) as well as in primary acute myelogenous leukemia blasts in relation to differentiation and apoptosis. MS-275 displays dose-dependent effects in each of the cell lines. When administered at a low concentration (e.g., 1 μM), MS-275 exhibits potent antiproliferative activity, inducing p21CIP1/WAF1-mediated growth arrest and expression of differentiation markers (CD11b) in U937 cells. Entinostat (MS-275) potently induces cell death, triggering apoptosis in ~70% of cells at 48 h [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Entinostat (MS-27-275) at 49 mg/kg shows marked antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and a moderate effect against Capan-1 tumor. Entinostat at 24.5 mg/kg and 12.3 mg/kg also shows significant effects against these tumors. In addition, oral administration of Entinostat apparently increases the level of histone acetylation in HT-29 tumor xenografts 4-24 h after the administration [3] . MS-275 administration (3.5 mg/kg i.p.) to Experimental autoimmune neuritis (EAN) rats once daily from the appearance of first neurological signs greatly reduces the severity and duration of EAN and attenuated local accumulation of macrophages, T cells and B cells, anddemyelination of sciatic nerves. In addition, MS-275 treatment increases proportion of infiltrated Foxp3 + cells and anti-inflammatory M2 macrophages in sciatic nerves of EAN rats [4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01594398 Syndax Pharmaceuticals
Lung Cancer|Non Small Cell Lung Cancer (NSCLC)|Breast Cancer|Estrogen Receptor Breast Cancer
May 2012 Phase 1
NCT00185302 Bayer
Melanoma
December 2004 Phase 2
NCT03179930 Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme LLC|Syndax Pharmaceuticals
Lymphoma|Relapsed|Refractory
June 7, 2017 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 132.83 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6567 mL 13.2834 mL 26.5668 mL
5 mM 0.5313 mL 2.6567 mL 5.3134 mL
10 mM 0.2657 mL 1.3283 mL 2.6567 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Carbamic acid, N-[[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]-, 3-pyridinylmethyl ester
Carbamic acid, [[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]-, 3-pyridinylmethyl ester
MS 275
MS 27-275
MS 275-27
SNDX 275
Entinostat
(Pyridin-3-yl)methyl 4-(2-aminophenylcarbamoyl)benzylcarbamate

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