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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Domatinostat (4SC-202)
Dangerous GoodsCAS number：910462-43-0 molecular formula：C23H21N5O3S
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| Chinese alias | 多马汀 (4SC-202) | ||
| English alias | DB13101 | DOMATINOSTAT [WHO-DD] | HY-16012A | 4SC202 | 4SC-202 | 4SC-202 (free base) | AS-77606 | A860619 | C3202 | DOMATINOSTAT [INN] | CCG-269205 | SCHEMBL1613943 | 264ARM7UXX | Q27254045 | (E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl | ||
| CAS number | 910462-43-0 | molecular formula | C23H21N5O3S |
| molecular weight | 447.51 g/mol | Exact mass | ≥97% |
| PSA | 120.000 Ų | logp | 2.955 |
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Safety information
pictogram：
GHS08 , GHS09
Signal word：
Warning
Hazard Statement：
H341: 怀疑引起遗传缺陷 H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响
Statement of Preventive Measures：
P273: 避免释放到环境中。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P281: 根据需要使用个人防护设备。 P391: 收集溢出物 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。
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