Domatinostat

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.

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2mg

￥875.00

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5mg

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1040.00

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10mg

￥1962.00

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50mg

￥5500.00

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￥8787.00

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货号: ajce56028
CAS: 910462-43-0
别名: (2E)-N-(2-氨基苯基)-3-[1-[[4-(1-甲基-1H-吡唑-4-基)苯基]磺酰基]-1H-吡咯-3-基]-2-丙烯酰胺,4SC-202 free base
分子式: C23H21N5O3S
分子量: 447.51
纯度: >98%
溶解度: DMSO: ≥ 58 mg/mL (129.61 mM)
储存: Store at -20°C
库存: 现货

Background

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. [1]

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. [1]

[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.