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Nolatrexed 2HCl, also known as AG337, is a thymidylate synthase inhibitor. Nolatrexed is a non-classical TS inhibitor in that it lacks a terminal glutamate side chain and is uncharged at physiological pH. Nolatrexed does not require a specific transport mechanism to enter into cells and, once within the cell, is not a substrate for the enzyme folyl polyglutamate synthetase.
In vivo, when nolatrexed was administered to nude mice bearing Bu25TK- tumor xenografts, a time-dependent increase in antitumor activity was observed.
| Molecular Weight | 357.26 |
| Formula | C14H14Cl2N4OS |
| CAS Number | 152946-68-4 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥ 16 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA/RNA Synthesis Products |
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| Dencatistat
Dencatistat (P115) is an inhibitor of Cytidine Triphosphate Synthase 1 (CTPS1) with an IC50 value of ≤ 0.1 μM. |
| Antipain dihydrochloride
Antipain dihydrochloride is a protease inhibitor. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride also restricts uterine DNA synthesis and function in mice. |
| Tetrahydrouridine
Tetrahydrouridine (THU) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine. |
| Crisnatol
Crisnatol (BWA770U) is a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells. Crisnatol (BWA770U) is also an orally active and anticancer agent. |
| Caf1-IN-1
Caf1-IN-1 is inhibitor for ribonuclease Caf1 with an IC50 of 0.59 µM. Caf1-IN-1 is also a weak inhibitor for poly(A)-specific ribonuclease (PARN) with IC50 of 23.9 µM. |
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