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Cell Cycle/Checkpoint Cell Cycle/CheckpointAntifolate
Antifolates are a class of antimetabolite medications that antagonise (that is, block) the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently, antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as proguanil, pyrimethamine and trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR).
Levoleucovorin Calcium
T643180433-71-2
Levoleucovorin Calcium (CL307782), a calcium salt of the folinic acid, is used in cancer chemotherapy as an adjuvant.
- $36
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QTY
Pralatrexate
T6120146464-95-1
Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.
- $30
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Methotrexate
Cited
T148559-05-2
Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.
- $38
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CitedPemetrexed
T0189137281-23-3
Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
- $33
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Folinic acid calcium
T01481492-18-8
Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.
- $42
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Folinic acid
T2440358-05-9
Folinic acid (Leucovorin) is a biofolate used in the treatment of methotrexate (MTX) toxicity reduction and as an adjuvant therapy for colon cancer.
- $33
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Pemetrexed disodium
T0189L150399-23-8
Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.
- $37
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Farletuzumab
T76720896723-44-7
Farletuzumab (MORAb-003) is a humanized monoclonal antibody with a high affinity for folate receptor-α (FRα), acting as a potent inhibitor of FRα and impeding the growth of cells that overexpress this receptor, making it useful for cancer research.
- $372
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Metoprine
T85487761-45-7
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
- $55
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Proguanil hydrochloride
T4382637-32-1
Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite.
- $50
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Levomefolate calcium
T7593151533-22-1
Levomefolate calcium, an artificial form of folate, is a coenzymated form of folic acid that offers a more bioavailable alternative in dietary supplements.
- $39
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Pemetrexed disodium hemipenta hydrate Cited
T6226357166-30-4
Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.
- $33
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CitedTrimethoprim
T1153738-70-5
Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.
- $45
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Methotrexate disodium
T80037413-34-5
Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor
- $34
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Pyrimethamine
T084958-14-0
Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
- $38
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Diaveridine
T22045355-16-8
Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.
- $42
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Trimethoprim lactate
T3986223256-42-0
Trimethoprim lactate (NSC-106568 lactate) is an antibiotic that inhibits bacterial dihydrofolate reductase (DHFR). Trimethoprim lactate has demonstrated antimicrobial activity, with excellent inhibition of Gramnegative bacteria. Trimethoprim lactate is used alone for the Trimethoprim lactate is used alone or in combination with other antibiotics to treat a variety of eye, lung, and gastrointestinal infections.
- $30
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Folinic Acid Calcium Salt Pentahydrate
T0148L6035-45-6
Folinic Acid Calcium Salt Pentahydrate (Leucovorin Calcium Pentahydrate), a reduced folic acid, is used in combination with other chemotherapeutics.
- $30
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Methotrexate metabolite
T1604519741-14-1In house
Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.
- $48
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Calcium N5-methyltetrahydrofolate
T759826560-38-3
Calcium N5-methyltetrahydrofolate (NSC-173328) 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
- $46
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Mirvetuximab soravtansine
T778251453084-37-1
Mirvetuximab soravtansine (IMGN853) is an antibody-drug coupling (ADC) targeting folate receptor alpha (FRα), which inhibits cell growth and enhances the antiproliferative effects of DNA damage, and may be useful in the study of drug-resistant ovarian cancer.
- $1,154
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Mirvetuximab
T767661453084-36-0
Mirvetuximab (M9346A) is a novel folate receptor α (FRα) monoclonal antibody targeting anti-FOLR1 (folate receptor 1). Mirvetuximab soravtansine is often conjugated with platinum compounds or other compounds to form antibody-drug conjugates for the treatment of ovarian cancer and other FRα-positive cancers.
- $322
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