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4SC-202 (free base)

    
99.20%

4SC-202 (free base)

源叶(MedMol)
S81091 一键复制产品信息
910462-43-0
C23H21N5O3S
447.50954
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S81091-2mg买3赠1
99.20%

¥240.00

3 - - - -
S81091-5mg买3赠1
99.20%

¥510.00

6 - - - -
S81091-10mg买3赠1
99.20%

¥840.00

6 - - - -
S81091-25mg买3赠1
99.20%

¥1600.00

6 - - - -
S81091-100mg买3赠1
≥98%

¥3610.00

货期:2-3天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述:

Domatinostat (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: HDAC3(Cell-free assay):0.57 μM; HDAC2(Cell-free assay):1.12 μM; HDAC1(Cell-free assay):1.20 μM; HDAC11(Cell-free assay):9.7 μM; HDAC5(Cell-free assay):11.3 μM; HDAC10(Cell-free assay):21 μM; HDAC9(Cell-free assay):50 μM;Apoptosis; HDAC
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
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
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.
动物实验: Animal Models: A549 NSCLC 移植瘤模型和 RKO27 结肠癌模型 Dosages: 120 mg/kg Administration: p.o.
参考文献: 1. Henning SW, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor. 22nd EORTC-NCI-AACR symposium. 2010. Abstract # 178. 2. Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67.
溶解性: soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.235 ml 11.173 ml 22.346 ml
5 mM 0.447 ml 2.235 ml 4.469 ml
10 mM 0.223 ml 1.117 ml 2.235 ml
50 mM 0.045 ml 0.223 ml 0.447 ml
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参考文献

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