推荐产品
质量水平
方案
≥95% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
N(Cc3ccc(cc3)C(=O)Nc4c(cccc4)N)c1nc(ccn1)c2cnccc2
InChI
1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29)
InChI key
HRNLUBSXIHFDHP-UHFFFAOYSA-N
生化/生理作用
MGCD0103 (Mocetinostat) is an orally active, potent and subtype-selective histone deacetylase (HDAC) inhibitor (IC50: class I HDAC1/2/3 = 0.15/0.29/1.66 μM, class IV HDAC11 = 0.59 μM, HDAC4/5/7/8 >10 μM) that effectively inhibits cellular HDAC activity (IC50 = 450 nM; Du145, HCT15, HCT116), resulting in an upregulated acetylation of histone H3 and H4, but not that of tubulin. MGCD0103 daily orally administration (60-120 mg/kg) is efficacious against A549 & H1437 tumor growth in mice in vivo.
Orally active, potent and HDAC1/2/3/11 subtype-selective histone deacetylase inhibitor with anti-tumor efficacy in mice in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Marielle Fournel et al.
Molecular cancer therapeutics, 7(4), 759-768 (2008-04-17)
Nonselective inhibitors of human histone deacetylases (HDAC) are known to have antitumor activity in mice in vivo, and several of them are under clinical investigation. The first of these, Vorinostat (SAHA), has been approved for treatment of cutaneous T-cell lymphoma.
Hanna Jung et al.
BioMed research international, 2020, 4705615-4705615 (2020-08-11)
The use of histone deacetylase (HDAC) inhibitor is a novel therapeutic strategy for cardiovascular disease. Studies have shown that many HDAC inhibitors have the ability to reduce the aortic remodeling in various animal models. We hypothesized that the HDAC inhibitor
W-J Wu et al.
European review for medical and pharmacological sciences, 24(8), 4467-4475 (2020-05-07)
To investigate the effect and mechanism of mocetinostat on diminishing epidural fibrosis. Dysregulated wound repair usually occurs after injury or surgery and is featured by excessive scar tissue contributed by fibrosis. Increasing researches demonstrated that histone acetylation, an epigenetic alteration
W-J Wu et al.
European review for medical and pharmacological sciences, 25(9), 3396-3396 (2021-05-19)
The article "Mocetinostat suppresses epidural fibrosis following laminectomy by inhibiting myofibroblast activation and increasing apoptosis, by W.-J. Wu, J. Wang, J. Liang, Q. Zhou, Y. Liang, published in Eur Rev Med Pharmacol Sci 2020; 24 (8): 4467-4475-DOI: 10.26355/eurrev_202004_21029-PMID: 32373984" has
Bo Liao et al.
Journal of Cancer, 11(7), 1915-1926 (2020-03-21)
Background: Liver cancer is a common cause of cancer-related death all over the world. MGCD0103, a histone deacetylase inhibitor, exerts antitumor effect on various cancers. However, its role in liver cancer remains unclear. Methods: The effect of MGCD0103 on HepG2
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