ChemicalBook > CAS DataBase List > 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
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
- CAS No.726169-73-9
- Chemical Name:N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
- CBNumber:CB42484945
- Molecular Formula:C23H20N6O
- Formula Weight:396.44
- MOL File:726169-73-9.mol
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Property
- Melting point >170oC (dec.)
- Density 1.340±0.06 g/cm3(Predicted)
- storage temp. RT
- solubility Soluble in DMSO (up to 25 mg/ml)
- pka 13.13±0.70(Predicted)
- form solid
- color Off-white
- Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
- NCI Dictionary of Cancer Terms MGCD0103; mocetinostat
- FDA UNII A6GWB8T96J
- NCI Drug Dictionary mocetinostat
- UNSPSC Code 12352200
- NACRES NA.77
- Symbol(GHS)
- Signal word
- Hazard statements
- Precautionary statements
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Chemical Properties,Usage,Production
- Description 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
- Uses 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.
-
in vivo
Mocetinostat (MGCD0103) significantly inhibits growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors. The p.o. administration of Mocetinostat (MGCD0103) (2HBr salt) significantly reduces growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. Mocetinostat (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocks growth of tumors compared with vehicle treatment alone (P<0.05 in post-ANOVA Dunnett's test) with no change in body weight[1].
- target HDAC1
- IC 50 HDAC1: 0.15 μM (IC50); HDAC2: 0.29 μM (IC50); HDAC11: 0.59 μM (IC50); HDAC3: 1.66 μM (IC50)
- References 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 Preparation Products And Raw materials
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726169-73-9, N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamideRelated Search:
- API
- Inhibitors
- Inhibitor
- 信号转导通路激酶抑制剂
- 抑制剂
- 生物试剂
- 合成有机化合物配体
- 标准品
- 细胞生物学试剂
- 小分子抑制剂,天然产物
- 表观遗传学
- 小分子抑制剂
- C23H20ON6
- 化合物MOCETINOSTAT,10 MM DMSO 溶液
- MOCETINOSTAT(MGCD0103),HDAC抑制剂
- 化合物MOCETINOSTAT
- BKT140, TF 14016, 4-FLUOROBENZOYL, 4F-BENZOYL-TN14003, T140
- HDAC抑制剂(MOCETINOSTAT)
- N-(2-氨基苯基)-4-([[4-(吡啶-3-基)嘧啶-2-基]氨基]甲基)苯甲酰胺
- 726169-73-9
- CD0103) Mocetinostat
- Mocetinostat, 10 mM in DMSO
- MGCD0103
- Mocetinostat
- N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide USP/EP/BP
- Benzamide, N-(2-aminophenyl)-4-[[[4-(3-pyridinyl)-2-pyrimidinyl]amino]methyl]-
- CS-1929
- MGCD0103; MGCD 0103; MGCD-0103
- MGCD0103;MGCD 0103;MGCD-0103;MG0103
- N-(2-Aminophenyl)-4-[[[4-(3-pyridyl)pyrimidin-2-yl]amino]methyl]benzamide
- Mocetinostat, >=98%
- N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide Mocetinostat (MGCD0103)
- Mocetinostat (MGCD0103)
- N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
- Mocetinostat (MGCD0103,MG0103)
- MG0103
- MGCD0103(Mocetinostat)