aladdin 阿拉丁 D413781 Domatinostat (4SC-202) 910462-43-0 97%

中文名：Domatinostat (4SC-202)

英文名：Domatinostat (4SC-202)

纯度：≥97%

货号：D413781

Cas号：910462-43-0

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Domatinostat (4SC-202) is a selective class IHDACinhibitor withIC50of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity againstLysine specific demethylase 1 (LSD1). Phase 1.

Targets

HDAC3 (Cell-free assay); HDAC2 (Cell-free assay); HDAC1 (Cell-free assay); HDAC11 (Cell-free assay); HDAC5 (Cell-free assay) 15602,0.57 μM; 1.12 μM; 1.20 μM; 9.7 μM; 11.3 μM

In vitro

In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM.

In vivo

4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model.

Cell Research(from reference)

Cell lines：CRC lines (HT-29, HCT-116, HT-15, and DLD-1) 

Concentrations：0.1, 1, 5, 10 μM 

Incubation Time：72 hours 

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