化合物HDAC-IN-57 T77334

Product Introduction
Bioactivity


英文名: HDAC-IN-57

描述: HDAC-IN-57 是一种具有口服活性的组蛋白脱乙酰酶 (HDAC) 泛抑制剂，对 HDAC1, HDAC2, HDAC6, HDAC8 具有抑制作用， IC50 值分别为 2.07 nM, 4.71 nM, 2.4 nM 和 107 nM。HDAC-IN-57 对 LSD1具有抑制作用， IC50 值为 1.34 μΜ。HDAC-IN-57 具有抗肿瘤活性，可诱导凋亡 (apoptosis)。

体外活性: HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μM; 48 h) effectively suppresses the migration and invasion of solid tumor cell lines, namely MGC-803, A549, and HCT-116. Furthermore, HDAC-IN-57 demonstrates significant growth inhibition in these solid tumor cell lines, exhibiting IC50 values of 0.45 μM, 1.48 μM, and 0.57 μM, respectively. Additionally, HDAC-IN-57 elicits apoptosis in MGC-803 and HCT-116 cells in a dose-dependent manner. It also exerts inhibitory effects on LSD1 and HDACs within the MGC-803 and HCT-116 cell lines. Moreover, HDAC-IN-57 induces cell cycle arrest in the G2/M phase for both MGC-803 and HCT-116 cells.[1] HDAC-IN-57 has high metabolic stability in vitro. Retains 86.1% and 87.4% of the parent compound after 1 hour of incubation in human liver (HLM) and rat liver microsomes (RLM), respectively, with a T1/2 of over 120 minutes.[1]

体内活性: HDAC-IN-57 (Compound 5e) (1 mg/kg, i.v.; 10 mg/kg, p.o.) demonstrated T1/2 of 0.37 hours (IV) and 2.75 hours (OR), with an oral bioavailability (F%) of 10.6%.[1] HDAC-IN-57 (25 or 50 mg/kg gavage; once daily for 21 days) achieved dose-dependent tumor growth inhibition in the NOD-SCID mouse MGC-803 xenograft model.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (119.24 mM)


关键字: HDACIN57 | HDAC-IN-57

相关产品: DBEQ | Oncrasin-1 | BMS-1 | Antitumor agent-103 | Nimbolide | dBET6 | Salubrinal | Scriptaid | GSK-1070916 | SNS-032

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

化合物HDAC-IN-57 T77334信息由TargetMol中国为您提供，如您想了解更多关于化合物HDAC-IN-57 T77334报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途