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Chemical Structure : AGF154
Catalog No.: PC-49049Not For Human Use, Lab Use Only.
AGF154 is a 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate with potent antiproliferative activities against tumor cells, with proton-coupled folate transporter (PCFR) and folate receptor (FR) selectivity over the reduced folate carrier (FRC), inhibtis de novo purine nucleotide biosynthesis.
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AGF154 is a 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate with potent antiproliferative activities against tumor cells, with proton-coupled folate transporter (PCFR) and folate receptor (FR) selectivity over the reduced folate carrier (FRC), inhibtis de novo purine nucleotide biosynthesis.
AGF154 inhibited proliferation of Chinese hamster ovary (CHO) sublines expressing folate receptors (FRs) α or β (IC50s<1 nM) or the proton-coupled folate transporter (PCFT, IC50<7 nM).
AGF154 exhibited potent antiproliferative activities toward all of the EOC cell lines, reflecting selective cellular uptake by FRα and/or PCFT over RFC.
AGF154 shows sensitivity against KD-10 tumor xenografts, with FRα- and substantial PCFT-mediated uptake.
| M.Wt | 447.466 | |
| Formula | C19H21N5O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Deis SM, et al. Biochemistry. 2016 Aug 16;55(32):4574-82.
2. Hou Z, et al. Mol Cancer Ther. 2017 May;16(5):819-830.
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