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PFK158
Axon 2542
CAS:
1462249-75-7
Purity:
99%
- Soluble in DMSO
- MF: C18H11F3N2O
- MW: 328.29
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.
More Information
| Parent CAS No. | 1462249-75-7 |
|---|---|
| Chemical Name | (E)-1-(pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one |
| SMILES | C(C1C=CN=CC=1)(=O)/C=C/C1C=CC2C(N=1)=CC(C(F)(F)F)=CC=2 |
| MFCD | N.A. |
| InChi | InChI=1S/C18H11F3N2O/c19-18(20,21)14-3-1-12-2-4-15(23-16(12)11-14)5-6-17(24)13-7-9-22-10-8-13/h1-11H/b6-5+ |
| InChiKey | IAJOMYABKVAZCN-AATRIKPKSA-N |
| CID | 71730058 |
| Short Description | PFKFB3 inhibitor |
PFK158
PFKFB3 inhibitor
Axon Medchem
Axon 2542
PFK 158
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
Supplier
Vendor
References
- 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
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