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 |
百灵威科技