| Identification | Back Directory | [Name]
L-Glutamic acid, N-[[5-[3-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]-3-thienyl]carbonyl]- | [CAS]
1286279-90-0 | [Synonyms]
AGF154
AGF-154
AGF 154
Antifolate C2
L-Glutamic acid, N-[[5-[3-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]-3-thienyl]carbonyl]- | [Molecular Formula]
C19H21N5O6S | [MOL File]
1286279-90-0.mol | [Molecular Weight]
447.46 |
| Hazard Information | Back Directory | [Description]
Antifolate C2, also known as AGF154, is an inhibitor of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter (PCFT) over the reduced folate carrier (RFC). | [Uses]
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed[1]. | [References]
[1] Wilson M R, et al. Targeting nonsquamous nonsmall cell lung cancer via the proton-coupled folate transporter with 6-substituted pyrrolo [2, 3-d] pyrimidine thienoyl antifolates[J]. Molecular pharmacology, 2016, 89(4): 425-434. DOI:10.1124/mol.115.102798 |
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