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Domatinostat

SKU: orb1300834

描述

Domatinostat (4SC202) is a selective class I HDAC inhibitor targeting HDAC1, HDAC2, and HDAC3, and also inhibits LSD1. It has been investigated in Phase 1 clinical trials for oncology research, with studies demonstrating its activity in both in vitro cellular assays and in vivo cancer models.

研究领域

Cell Biology, Epigenetics & Chromatin, Molecular Biology

图片与验证

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关键属性

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CAS 号910462-43-0
MW447.51
纯度99.74% (May vary between batches)
分子式C23H21N5O3S
SMILESCn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1
靶点HDAC,Apoptosis
溶解性DMSO:82 mg/mL (183.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.37 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

生物活性

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靶点 IC50
HDAC2:1.12 μM|HDAC1:1.20 μM|HDAC9:50 μM|HDAC5:11.3 μM|HDAC10:21 μM|HDAC3:0.57 μM|HDAC11:9.7 μM
体内
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.
体外
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.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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Domatinostat, 4SC202, 4SC-202, 4SC-202 (free base), 4SC 202, Apoptosis, inhibit, Histone deacetylases, Inhibitor, HDAC, HDAC3, HDAC5, HDAC2, HDAC1, HDAC11

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  • Domatinostat tosylate [orb1302825]

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    25 mg, 5 mg, 10 mg, 50 mg, 100 mg, 1 mg, 1 ml x 10 mM (in DMSO)
  • 4SC-202 free base [orb1223678]

    >98% (HPLC)

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    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g
质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

1 mg
¥ 1,040.00
5 mg
¥ 1,690.00
1 ml x 10 mM (in DMSO)
¥ 1,690.00
10 mg
¥ 2,210.00
25 mg
¥ 3,510.00
50 mg
¥ 5,460.00
100 mg
¥ 7,800.00
发货Usually dispatched within 5-10 working days
批量询价