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NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. It is a minor metabolite of methotrexate. It inhibited L1210 cell proliferation in culture (IC50 = 0.3 uM), and prolonged the survival of L1210 leukemic mice (98% increase in lifespan at 120 mg/kg, qdx9). Studies on the interaction of mAPA-HCysA with partially purified mouse liver folyl polyglutamate synthetase revealed that mAPA-HCysA was not a substrate. Hence, the increased dose of mAPA-HCysA required to inhibit tumor growth in vitro and in vivo relative to methotrexate may reflect, in part, the inability of this compound to form non-effluxing polyglutamates.
| Molecular Weight | 325.33 |
| Formula | C15H15N7O2 |
| CAS Number | 19741-14-1 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Antifolate Products |
|---|
| Pemetrexed disodium
Pemetrexed is a novel antifolic acid antimetabolic compound with K I of 1.3 nM, 7.2 nM, and 65 nM for TS, DHFR, and GARFT, respectively. |
| Methotrexate
Methotrexate (Amethopterin) is an antimetabolite and antifolate agent with antineoplastic and immunosuppressant activities. |
| Folinic acid calcium salt
Folic acid is an adjuvant compound used in cancer chemotherapy. *The compound is unstable in solutions, freshly prepared is recommended |
| Sulfamethazine
Sulfamethazine is a sulfonamide antibacterial. |
| Pyrimethamine
Pyrimethamine is a dihydrofolate reductase(DHFR) inhibitor with an IC50 of 15.4 nM. |
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