货号	规格	价格	上海	北京	武汉	南京
S80284-5mg	98.1%	￥720.00 S80284-5mg ￥720.00 现货	5 5	-	-	-
S80284-10mg	98.1%	￥990.00 S80284-10mg ￥990.00 现货	6 6	-	-	-
S80284-50mg	≥98%	￥2900.00 S80284-50mg ￥2900.00 2-3天	0 货期：2-3天	-	-	-

产品介绍

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.

产品描述：

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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