HDAC-IN-57 (Compound 5e) (静脉注射1 mg/kg，口服10 mg/kg) 显示 T＜sub＞1/2HDAC-IN-57 (25或50 mg/kg灌胃；每天1次，连续21天) 在 NOD-SCID 小鼠 MGC-803 异种移植模型中实现了剂量依赖性肿瘤生长抑制[1]。 Animal Model: MGC-803 xenograft model in NOD-SCID mice[1] Dosage: 25 or 50 mg/ kg Administration: Oral gavage (p.o.); Result: Achieved a dose-dependent tumor growth inhibition (TGI) of 44.8% at 25 mg/kg and 71.5% at 50 mg/kg. Animal Model: Male SD rats (Pharmacokinetic assay)[1] Dosage: 1 mg/kg; 10 mg/kg Administration: Intravenous injection (i.v.); Oral gavage (p.o.) Result: Pharmacokinetic parameters for HDAC-IN-57 (Compound 5e) in SD rats[1] Route Dose (mg/kg) T1/2 (h) Tmax (h) CL (mL•min-1/kg-1) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) Cmax (ng/mL) VZ (L/kg) F (%) i.v. 1 0.37 / 1.61 644.1 645.8 1892.8 0.82 / p.o. 10 2.75 0.25 / 685.2 766.2 716.4 52.2 10.6 分子量 377.39 Formula C21H19N3O4 CAS 号 2716217-79-5 运输条件 Room temperature in continental US; may vary elsewhere. 储存方式 Please store the product under the recommended conditions in the Certificate of Analysis. 纯度 & 产品资料 Data Sheet (535 KB) 产品使用指南 (1538 KB) 参考文献 [1].
In Vitro
HDAC-IN-57 (Compound 5e) (1.0 μM，2.5 μM，5.0 μΜ； 48 小时) 抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的迁移和侵袭[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 显著抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的生长，IC50s 值分别为 0.45 μM, 1.48 μM 和 0.57 μM[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 以剂量依赖性方式触发 MGC-803 和 HCT-116 细胞凋亡[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 抑制 MGC-803 和 HCT-116 细胞系内 LSD1 和 HDACs[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 诱导 MGC-803 和 HCT-116 细胞周期 G2/M 期阻滞[1]。 HDAC-IN-57 在体外代谢稳定性高。在人肝脏 (HLM) 和大鼠肝脏微粒体 (RLM) 中孵育1 小时后分别保持母体化合物的 86.1% 和 87.4%，T1/2超过 120 分钟[1]。 Western Blot Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.5 μM Incubation Time: 48 hours Result: Inhibited cellular LSD1 and HDACs. Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2. Apoptosis Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.5 μM, 5.0 μM Incubation Time: 48 hours Result: Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner. Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM. Cell Migration Assay [1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.0 μM, 4 μM Incubation Time: 48 hours Result: Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells. Cell Cycle Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.5 μM, 5.0 μM Incubation Time: 48 hours Result: Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
