Zabadinostat

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Chemical Structure| 934828-12-3 同义名 : CXD101; HDAC-IN-4; AZD 9468
CAS号 : 934828-12-3
货号 : A623282
分子式 : C24H29N5O
纯度 : 99%+
分子量 : 403.52
MDL号 : MFCD30489755
存储条件:

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Histone deacetylases (HDAC) are enzymes that catalyze the removal of acetyl functional groups from the lysine residues of histones and non-histone proteins. HDAC inhibitors are a new class of anti-cancer agents that induce apoptosis and cell cycle arrest in cancer cells. CXD-101 is a class I-selective HDAC inhibitor that inhibits HDAC1, HDAC2, and HDAC3 with IC50 values of 63, 570, and 550nM, respectively, and had no activity against class II HDAC[1]. The IC50 values of CXD-101 in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines ranged from 0.2 to 15μM. In murine lung (A549a) and colon (HT29) models, CXD-101 reduced tumor size at a dose of 50mg/kg, which was found to be associated with decreased HDAC enzyme activity and increased histone acetylation[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.39mL

2.48mL

1.24mL

24.78mL

4.96mL

2.48mL

参考文献

[1]WO2007045844A1

[2]Eyre T.A. Predictive biomarkers for disease sensitivity in lymphoma - the holy grail for HDAC inhibitors? Oncotarget. 2018;9(99):37280-37281.

[3]Eyre T.A, Collins G.P, Gupta A., et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019;125(1):99-108.