ChemicalBook Produktkatalog Bio- und Chemieingenieurwesen Inhibitoren Epigenetik HDAC-Inhibitoren N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Struktur

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide

Bezeichnung:N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide

CAS-Nr726169-73-9

Englisch Name:N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide

CBNumberCB42484945

SummenformelC23H20N6O

Molgewicht396.44

MOL-Datei726169-73-9.mol

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide physikalisch-chemischer Eigenschaften

Schmelzpunkt	>170oC (dec.)
Dichte	1.340±0.06 g/cm3(Predicted)
storage temp.	RT
Löslichkeit	Soluble in DMSO (up to 25 mg/ml)
pka	13.13±0.70(Predicted)
Aggregatzustand	solid
Farbe	Off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Mocetinostat (726169-73-9) is a class I, isoform-selective HDAC inhibitor, IC50s=0.15, 0.29, 1.66 and 0.59 μM for HDAC1, 2, 3 and 11 respectively.1 Induces hyperacetylation of histones, induces expression of the tumor suppressor p21WAF1 and inhibits proliferation of human cancer cells.2 Mocetinostat displays antifibrotic effects in ischemic heart failure.3 Attenuates the development of hypersensitivity in models of neuropathic pain.4 Active in vivo.5
Verwenden
Mocetinostat is a multi-targeted histone deacetylase inhibitor used in cancer therapy. Mocetinostat is undergoing clinical trials for the treatment of various cancers including follicular lymphoma, Hodgkin’s lymphoma and acute myelogenous leukemia.
Definition
ChEBI: N-(2-aminophenyl)-4-[[[4-(3-pyridinyl)-2-pyrimidinyl]amino]methyl]benzamide is a member of benzamides.
target
HDAC1
Einzelnachweise
1) Zhou et al. (2008), Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ulpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor; J. Med. Chem., 51 4072 2) Raeppel et al. (2009), SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4((4-(pyridine-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103); Bioorg. Med. Chem. Lett., 19 644 3) Nural-Guvener et al. (2015), Anti-Fibrotic Effects of Class I HDAC Inhibitor, Mocetinostat is Associated with IL-6/Stat3 Signaling in Ischemic Heart Failure; Int. J. Mol. Sci., 16 11482 4) Denk et al. (2013), HDAC inhibitors attenuate the development of hypersensitivity in models of neuropathic pain; Pain, 154 1668 5) Bonfils et al. (2008), Evaluation of the pharmacodynamics effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay; Clin. Cancer Res., 14 3441

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Upstream-Materialien And Downstream Produkte

N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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