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• 产品描述： Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

• 靶点： PI3Kα:19 nM (IC50);PI3Kβ:54 nM (IC50);PI3Kδ:39 nM (IC50);PI3Kγ:311 nM (IC50);HDAC1:1.7 nM (IC50);HDAC2:5 nM (IC50);HDAC3:1.8 nM (IC50);HDAC4:409 nM (IC50);HDAC5:674 nM (IC50);HDAC6:27 nM (IC50);HDAC7:426 nM (IC50);HDAC8:191 nM (IC50);HDAC9:554 nM (IC50);HDAC10:2.8 nM (IC50);HDAC11:5.4 nM (IC50);Apoptosis;PI3K;HDAC

• 体内研究：
  Oral administration of Fimepinostat inhibits growth of the Daudi cancer cell xenografts in a dose-dependent manner. Tumor stasis is observed at 100 mg/kg in this model without obvious toxicity. Importantly, in the same model, Fimepinostat achieves better efficacy than GDC-0941, SAHA, or a combination of these 2 compounds given at their maximal tolerated doses (MTD). Furthermore, Fimepinostat causes tumor regression or stasis after intravenous (50 mg/kg) or oral administration (100 mg/kg) in a xenograft tumor model of SU-DHL4 diffuse large B-cell lymphoma (DLBCL) and causes tumor stasis in KRAS-mutant A549 NSCLC cell xenografts

• 参考文献：
  1. Qian C, et al. Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin Cancer Res. 2012 Aug 1;18(15):4104-13.

• 溶解性： DMSO  :  50  mg/mL  (98.32  mM;  Need  ultrasonic)    DMF  :  5  mg/mL  (9.83  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.966 ml	9.832 ml	19.664 ml
  5 mM	0.393 ml	1.966 ml	3.933 ml
  10 mM	0.197 ml	0.983 ml	1.966 ml
  50 mM	0.039 ml	0.197 ml	0.393 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *