Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ricolinostat (Rocilinostat) 是一种选择性HDAC6抑制剂,IC50为 5 nM。它还抑制HDAC1,HDAC2和HDAC3,IC50分别为 58,48 和 51 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 209 | 现货 | ||
2 mg | ¥ 292 | 现货 | ||
5 mg | ¥ 525 | 现货 | ||
10 mg | ¥ 798 | 现货 | ||
25 mg | ¥ 1,430 | 现货 | ||
50 mg | ¥ 2,320 | 现货 | ||
100 mg | ¥ 3,950 | 现货 | ||
500 mg | ¥ 8,560 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 571 | 现货 |
产品描述 | Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. |
靶点活性 | HDAC6:4.7 nM, HDAC8:100 nM, HDAC1:58 nM, HDAC3:51 nM, HDAC2:48 nM |
体外活性 | 在浆细胞瘤模型和弥散性MM模型中,ACY-1215易被肿瘤组织吸收并且不会在组织中积累,能够抑制肿瘤生长. |
体内活性 | 在极低剂量时,ACY-1215能够显著诱导α-tubulin乙酰化,同时在较高剂量时,能够诱导组蛋白H3和H4组蛋白赖氨酸的乙酰化。在HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1,和 Sirtuin2,对HDAC8中,ACY-1215,ACY-1215(IC50=0.1 μM) 有轻微的活性。 |
激酶实验 | ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated[1]. |
细胞实验 | ACY-1215 is dissolved in DMSO (10 mM) and stored, and then in diluted with appropriate culture medium before use[1]. The effect of ACY-1215 with or without Bortezomib on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+ T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3×104 cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, Bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured[1]. |
别名 | ACY-1215, Rocilinostat |
分子量 | 433.5 |
分子式 | C24H27N5O3 |
CAS No. | 1316214-52-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 80 mg/mL (184.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3068 mL | 11.534 mL | 23.0681 mL | 57.6701 mL |
5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL | 11.534 mL | |
10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL | 5.767 mL | |
20 mM | 0.1153 mL | 0.5767 mL | 1.1534 mL | 2.8835 mL | |
50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1534 mL | |
100 mM | 0.0231 mL | 0.1153 mL | 0.2307 mL | 0.5767 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ricolinostat 1316214-52-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibit ACY 1215 ACY1215 Inhibitor ACY-1215 Histone deacetylases Rocilinostat inhibitor