Nolatrexed dihydrochloride manufacturers
- Nolatrexed dihydrochloride
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- $15.00 / 1KG
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2021-08-12
- CAS:152946-68-4
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
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| | Nolatrexed dihydrochloride Basic information |
| | Nolatrexed dihydrochloride Chemical Properties |
| Melting point | 301-3020C | | storage temp. | Hygroscopic, -20°C Freezer, Under Inert Atmosphere | | solubility | Methanol, Water | | form | Solid | | pka | 4.1; 5.9; 9.8(at 25℃) | | color | Off-White to Pale Yellow | | Stability: | Hygroscopic | | CAS DataBase Reference | 152946-68-4(CAS DataBase Reference) |
| | Nolatrexed dihydrochloride Usage And Synthesis |
| Chemical Properties | Tan Solid | | Uses | Antifolate thymidylate synthase inhibitor. Antineoplastic. | | Biological Activity | thymidylate synthase (ts) is a crucial enzyme in the synthesis of 2'-deoxythymidine-5'-monophosphate, an essential precursor for dna biosynthesis. thus, this enzyme is a critical target in cancer chemotherapy. nolatrexed (ag-337) is a non-classical thymidylate synthase inhibitor. | | in vitro | nolatrexed was designed using x-ray crystallographic data from the ts molecular modeling and folate binding site. it 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 [1]. | | in vivo | when nolatrexed was administered to nude mice bearing bu25tk- tumor xenografts, a time-dependent increase in antitumor activity was observed [1]. | | IC 50 | 1.0, 0.81 and 1.0 μm for l1210, ccrf-cem and gc3/m tk- cell lines, respectively | | references | [1] hughes an, rafi i, griffin mj, calvert ah, newell dr, calvete ja, johnston a, clendeninn n, boddy av. phase i studies with the nonclassical antifolate nolatrexed dihydrochloride (ag337, thymitaq) administered orally for 5 days. clin cancer res. 1999 jan;5(1):111-8.
[2] rafi i, boddy av, calvete ja, taylor ga, newell dr, bailey np, lind mj, green m, hines j, johnstone a, clendeninn n, calvert ah. preclinical and phase i clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors. j clin oncol. 1998 mar;16(3):1131-41. |
| | Nolatrexed dihydrochloride Preparation Products And Raw materials |
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