| 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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J Clin Invest, 2025, e190215
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Theranostics, 2025, 15(10):4526-4549
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Antimicrob Agents Chemother, 2025, e0047125.
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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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Nat Commun, 2025, 16(1):8932
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Cell Death Dis, 2024, 15(8):555
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Cell Commun Signal, 2024, 22(1):375
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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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| E7308 |
Calcium N5-methyltetrahydrofolate
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Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
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| E7394 |
Methotrexate metabolite
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Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.
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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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iScience, 2024, 27(10):110862
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Cell Rep, 2022, 38(9):110448
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Front Pharmacol, 2022, 13:1032975
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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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Nat Commun, 2025, 16(1):7853
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Nat Commun, 2025, 16(1):8476
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Sci Adv, 2025, 11(4):eadp4765
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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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J Exp Clin Cancer Res, 2025, 44(1):13
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iScience, 2024, 27(10):110862
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Cell Rep Med, 2023, 4(10):101200
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