| S1210 |
Methotrexate
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Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
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Cancer Res, 2026, 86(7):1724-1738
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J Clin Invest, 2025, e190215
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Theranostics, 2025, 15(10):4526-4549
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| S5097 |
Methotrexate disodium
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Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
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Chin Med J (Engl), 2023, 10.1097/CM9.0000000000002816
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Pharmaceutics, 2023, 15(2)576
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Bioact Mater, 2022, 18:459-470
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| S1135 |
Pemetrexed Disodium (LY231514)
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Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
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Frontiers in Pharmacology, September 27, 2021, 718675
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Cancer Research, November 2, 2022, 4079-4092
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Frontiers in Oncology, August 18, 2021, 711043
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| S5264 |
L-5-Methyltetrahydrofolate calcium
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Calcium L-5-methyltetrahydrofolate (L-5-MTHF-Ca) is a synthetic derivative of folic acid, the predominant, naturally occurring form of folate.
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| S7785 |
Pemetrexed Disodium Hydrate
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Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. This compound stimulates autophagy and apoptosis.
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Translational Lung Cancer Research, April 2022, 543-559
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iScience, 2024, 27(10):110862
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Cell Rep, 2022, 38(9):110448
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| S5971 |
Pemetrexed
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Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. This compound induces autophagy and apoptosis.
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Anticancer Research, 2026, 1323-1335
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Nat Commun, 2025, 16(1):7853
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Nat Commun, 2025, 16(1):8476
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| S1497 |
Pralatrexate
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Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. This compound induces tumor cell apoptosis.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Br J Haematol, 2024, 10.1111/bjh.19658
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Discov Oncol, 2024, 15(1):709
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| S1236 |
Leucovorin Calcium Pentahydrate (Folinic acid)
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Leucovorin (Folinic acid) Calcium Pentahydrate is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.Solutions are unstable and should be fresh-prepared.
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Journal of Hepatocellular Carcinoma, March 27, 2023, 483-495
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Journal of Student Research, August 2024, nan
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J Exp Clin Cancer Res, 2025, 44(1):13
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| S2006 |
Pyrimethamine
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Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
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Antimicrob Agents Chemother, 2025, e0047125.
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Int J Parasitol Drugs Drug Resist, 2025, 29:100626
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BMC Cancer, 2024, 24(1):116
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| S3129 |
Trimethoprim
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Trimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.
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Cell Rep, 2024, 43(7):114500
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Sci Rep, 2024, 14(1):9167
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CHALMERS UNIVERSITY OF TECHNOLOGY, 2023,
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