化合物CUDC-907 T2078

Product Introduction
Bioactivity


英文名: Fimepinostat

描述: Fimepinostat (CUDC 907) 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。

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].

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].

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 94 mg/mL (184.8 mM)


关键字: CUDC907 | Fimepinostat | inhibit | HDAC | Inhibitor | Apoptosis | PI3K | Phosphoinositide 3-kinase | Histone deacetylases

相关产品: PR-619 | Anticancer agent 136 | Deoxypodophyllotoxin | Myristoleic acid | SCR7 | Isatuximab | Domatinostat tosylate | Lonicerin | Lorlatinib | Buparlisib

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Autophagy Compound Library | Reprogramming Compound Library

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