Powder: -20°C for 3 years | In solvent: -80°C for 2 years
PI3K/HDAC Inhibitor 是一种 I 型PI3K 及 I 和 II 型HDAC 酶抑制剂,作用于 PI3Kα/PI3Kβ/PI3Kδ 和 HDAC1/HDAC2/HDAC3/HDAC10 ,IC50分别为 19/54/39 nM 和 1.7/5.0/1.8/2.8 nM。
产品描述 | CUDC-907 is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types. |
靶点活性 | HDAC1:1.7 nM, HDAC10:2.8 nM, HDAC11:5.4 nM, HDAC3:1.8 nM, HDAC2:5.0 nM |
体外活性 | 在作用于NHL和MM模型的高效性研究中, CUDC-907按最大耐受剂量处理,比单独药剂PI3K或HDAC抑制剂或两者联用效果更明显.且按最大耐受剂量处理,CUDC-907比PI3Kδ选择性抑制剂CAL-101更有效.CUDC-907对犬类具有口服生物有效性.CUDC-907在小鼠肿瘤中的半衰期较长.作用于移植瘤时,CUDC-907诱导凋亡并抑制癌细胞增殖. |
体内活性 | CUDC-907对一系列B细胞淋巴瘤的生长具有抑制作用,如Granta 519(IC50:7 nM),DOHH2(IC50:1 nM),RL(IC50:2 nM),Pfeiffer(IC50:4 nM),SuDHL4(IC50:3 nM),Daudi(IC50:15 nM) 和 Raji(IC50:9 nM)。CUDC-907对骨髓瘤增殖也有阻断作用,如RPMI8226(IC50:2 nM),OPM-2(IC50:1 nM)和ARH77(IC50:5 nM)。CUDC-907对多发性骨髓瘤和B细胞淋巴瘤均有明显抗癌活性。CUDC-907对其他PI3K亚型有抑制作用抑制,如 PI3Kβ/γ/δ和 PI3KαE545K, IC50分别为 54/311/39/62 nM。而且, CUDC-907对HDAC亚型HDAC8//6/11(IC50:191/27/5.4 nM)也有抑制效果。此外,CUDC-907对其他类型 HDAC 酶活性也有微弱抑制。 |
激酶实验 | The activities of classes I and II HDACs are measured using the Color-de-Lys assay system. The activity of PI3K is measured using the ADP-Glo luminescent kinase assay. Recombinant PI3K protein, a complex of N-terminal GST-tagged recombinant full-length human p110 and untagged recombinant full-length human p85, is coexpressed in a baculovirus-infected Sf9 cell expression system[1]. |
细胞实验 | CUDC-907 is dissolved in DMSO and stored (-80°C), and then diluted with appropriate medium before use[1]. Human cancer cell lines are plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells are then incubated with compounds (e.g.,CUDC-907) at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition is assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit[1]. |
别名 | CUDC-907, CUDC 907, PI3K/HDAC Inhibitor |
分子量 | 508.55 |
分子式 | C23H24N8O4S |
CAS No. | 1339928-25-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Ethanol: <1 mg/mL
DMSO: 94 mg/mL (184.8 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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。
Fimepinostat 1339928-25-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair PI3K/Akt/mTOR signaling HDAC PI3K inhibit CUDC-907 Inhibitor CUDC907 CUDC 907 PI3K/HDAC Inhibitor Phosphoinositide 3-kinase Histone deacetylases inhibitor