产品名称

PFK 158

产品货号

Axon 2542 CAS [1462249-75-7] MF C18H11F3N2OMW 328.29 Purity: 99% Soluble in DMSO Description Nanomolar small molecule inhibitor of PFKFB3 (IC50 value 137 nM) that is selectively cytotoxic to cancer cells and displays broad anti-tumor activity causing significant growth inhibition in preclinical models of breast, lung, glioblastoma, ovarian, pancreatic, melanoma and colon cancer. PFK158 is well tolerated in rats and dogs resulting in an acceptable pre-clinical therapeutic index. KEYWORDS: PFK 158 | supplier | PFKFB3 inhibitor | PFK158 | CAS [1462249-75-7] | Fructose 6-phosphate | PFKFB3 | Inhibitor | glycolysis | solid malignancy | Ras | AKT | PI3K | p53 | PTEN | cytotoxic | cancer cells | anti-tumor activity | breast cancer | lung cancer | glioblastoma | ovarian cancer | pancreatic cancer | melanoma | colon cancer

产品价格

现货询价，电话：010-67529703

产品规格

产品品牌

axonmedchem

产品概述

产品详情

PFK 158

Based on 49 reference(s) in Google Scholar 9 10 49

Axon 2542

CAS [1462249-75-7]

MF C18H11F3N2O
MW 328.29

Purity: 99%
Soluble in DMSO

PFK 158

Description

Nanomolar small molecule inhibitor of PFKFB3 (IC50 value 137 nM) that is selectively cytotoxic to cancer cells and displays broad anti-tumor activity causing significant growth inhibition in preclinical models of breast, lung, glioblastoma, ovarian, pancreatic, melanoma and colon cancer. PFK158 is well tolerated in rats and dogs resulting in an acceptable pre-clinical therapeutic index.

KEYWORDS: PFK 158 | supplier | PFKFB3 inhibitor | PFK158 | CAS [1462249-75-7] | Fructose 6-phosphate | PFKFB3 | Inhibitor | glycolysis | solid malignancy | Ras | AKT | PI3K | p53 | PTEN | cytotoxic | cancer cells | anti-tumor activity | breast cancer | lung cancer | glioblastoma | ovarian cancer | pancreatic cancer | melanoma | colon cancer

R Redman et al. Abstract CT206: PFK-158, first-in-man and first-in-class inhibitor of PFKFB3/ glycolysis: A phase I, dose escalation, multi-center study in patients with advanced solid malignancies. Cancer Res August 1, 2015 75; CT206

S Telang et al. Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.

GH Tapolsky et al. Pfkfb3 inhibitor and methods of use as an anti-cancer therapeutic. US Patent US2015064175 (A1), 2015

Cell Signaling & Oncology Diabetes & Metabolism Immunology PFKFB3 NF-κB EC 2.7.1.105

Nanomolar small molecule inhibitor of PFKFB3

Chemical name

(E)-1-(pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one

Parent CAS No.

[1462249-75-7]

产品资料