AGF154 | Antifolate | Probechem Biochemicals

Chemical Structure : AGF154

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AGF154 (AGF 154)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	447.466
分子式	C19H21N5O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-({5-[3-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)-propyl]-thiophene-3-carbonyl}-amino)-pentanedioic Acid

参考文献

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.

AGF154 (AGF 154)

生物&药学活性

物理化学性质&存储条件

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AGF154 (AGF 154)

生物&药学活性

物理化学性质&存储条件

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