基本信息
| 分子式 | C23H21N5O3S |
| 分子量 | 447.51 |
| 存储条件 | Freezer -20℃ |
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.
安全信息
| 图形或危害标志 |   |
| 提示语 | Warning |
| 危险说明 | H302 H410 |
| 防范说明 | P264 P270 P273 P301+P312 P330 P391 P501 |
| UN号码 | 3077 |
| 危险分类 | 9 |
| 包装等级 | III |
