产品描述

4SC-202是一种选择性的I类HDAC抑制剂，对HDAC1，HDAC2，和HDAC3的IC50分别为1.20 μM，1.12 μM，和0.57 μM。也对Lysine specific demethylase 1 (LSD1)表现出抑制活性。Phase 1。

靶点（IC50 & Targe）

HDAC1,1.20μM

HDAC11,9.7μM

HDAC2,1.12μM

HDAC3,0.57μM

HDAC5,11.3μM

体外研究

在HeLa细胞中，4SC-202诱导组蛋白H3高度乙酰化，EC50 为1.1 μM。4SC-202通过干扰有丝分裂纺锤体的正常发育诱导G2/M细胞周期阻滞，并引起纺锤体塌陷和多个成核中心。此外，4SC-202对人癌症细胞系表现出广谱抗肿瘤活性，IC50 为0.7 μM。[1]

体内研究

在体内，4SC-202具有较高的口服生物利用度，并表现出高代谢稳定性和低血浆清除率。在A549 NSCLC 异种移植和RKO27结肠癌模型中，4SC-202 (120 mg/kg p.o.)表现出显著的强抗肿瘤活性。[1]

细胞实验

Cell lines: NCI-H460，A549，MCF7，MDA-MB-468，SK-BR-3，SK-OV-3，A2780，RKO (p21)，HCT-15，PC-3，HeLa，Cal 27，A-431，Hec-1-A，K-562，EOL1，和 CCRF-CEM 细胞

Concentrations: ~10 μM

Incubation Time: 72小时

Method:CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.

(Only for Reference)

动物实验

Animal Models: A549 NSCLC 移植瘤模型和 RKO27 结肠癌模型

Formulation: Saline

Dosages: 120 mg/kg

Administration: p.o.

(Only for Reference)

参考文献

[1] Henning SW, et al. 22nd EORTC-NCI-AACR symposium. 2010. Abstract # 178.

[2] Zhijun H, et al. Tumour Biol. 2016, 37(8):10257-67.