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AGF94

Chemical Structure : AGF94

CAS No.: 136784-51-5

AGF94 (AGF 94)

Catalog No.: PC-49050Not For Human Use, Lab Use Only.

AGF94 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AGF94 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.
AGF94 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=3.3 nM).
AGF94 exhibites substantial anti-tumor efficacy in late-stage subcutaneous BR-Luc xenografts, accompanied by significantly decreased M2-like FRβ-expressing macrophages and increased CD3+ T cells.

Physicochemical Properties

M.Wt 447.466
Formula C19H21N5O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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-2-carbonyl)-amino)-pentanedioic acid

References

1. Wang L, et al. J Med Chem. 2015 Sep 10;58(17):6938-59.

2. Deis SM, et al. Biochemistry. 2016 Aug 16;55(32):4574-82.

3. Hou Z, et al. Mol Cancer Ther. 2017 May;16(5):819-830.

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