| CAS: | 910462-43-0 | |
| 分子式: | C23H21N5O3S | |
| 分子量: | 447.51 | |
| 英文名称: |
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| 用途: | 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。 |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||
| D872867 | MACKLIN | 4SC-202游离碱 | 99% | 286元/5mg; 599元/25mg; 1640元/100mg; | 咨询 | ||||||||||||||||||||||
储存：-20℃ 状态：浅黄色固体 | |||||||||||||||||||||||||||
| D792347 | MACKLIN | 4SC-202游离碱 | 10mM in DMSO | 520元/1ml; | 咨询 | ||||||||||||||||||||||
储存：-20°C | |||||||||||||||||||||||||||
| 2062986 | J&K | Domatinostat | 98%, 一种 I 型 HDAC 抑制剂 | 760元/2MG; 1710元/10MG; | 咨询 | ||||||||||||||||||||||
基本信息
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
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