PFK-015 产品说明书 Chemicals
导航 首页 > 产品 > Featured products
产品编号 DC8026
名称 PFK-015

化学性质

CAS 4382-63-2
分子式 C17H12N2O
分子量 260.29
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents, and suppresses tumor glucose metabolism and growth in an aggressive mouse model of non-small cell lung cancer. PFK-015 is not a Pgp substrate as determined by transport and cell permeability assays in Caco-2 and MDCK-MDR1 (Papp A-B / B-A results 1.8 / 4 and 5 / 5 10–6 cm/s). PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines. PFK-015 suppresses glucose uptake in cancer cells. Rodent PK studies following IV dosing at 5 mg/kg resulted in a profile with a satisfactory half-life (5.1 hours), exposure (AUCinf 1804 ng.h/ml), tissue distribution (Vd 20.5 L/kg) and reasonable clearance (46.2 mL/min/kg). Also, pre-clinical efficacy studies of C57Bl/6 mice bearing Lewis Lung Carcinoma (LLC) xenografts demonstrated 80% tumor growth inhibition relative to vehicle control. Finally, micro-PET studies performed on mice bearing LLC tumors showed a significant inhibition of tumor 2-[18F]-fluoro-2-deoxy-glucose uptake. These results support further development of PFK-015 as a novel anti-cancer agent. For the detailed information of PFK-015, the solubility of PFK-015 in water, the solubility of PFK-015 in DMSO, the solubility of PFK-015 in PBS buffer, the animal experiment (test) of PFK-015, the cell expriment (test) of PFK-015, the in vivo, in vitro and clinical trial test of PFK-015, the EC50, IC50,and affinity,of PFK-015, Please contact DC Chemicals.
退货政策
如果您对于您的订单不满意,您可以在购买日365天内将产品退回。
下订单的时候请提供您的快递地址以及开票信息
电话: +86-21-58447131
传真: +86-21-61642470

Email:
sales@dcchemicals.com
order@dcchemicals.com

网址:
http://www.dcbio.cn/