| Identification | Back Directory | [Name]
LSN 3213128
(LSN3213128) | [CAS]
1941211-99-9 | [Synonyms]
LSN 3213128
(LSN3213128)
2-Thiophenesulfonamide, N-(6-fluoro-1,2-dihydro-1-oxo-7-isoquinolinyl)-5-[(3R)-3-hydroxy-1-pyrrolidinyl]- | [Molecular Formula]
C17H16FN3O4S2 | [MDL Number]
MFCD32174255 | [MOL File]
1941211-99-9.mol | [Molecular Weight]
409.45 |
| Chemical Properties | Back Directory | [density ]
1.596±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 62.5 mg/mL (152.64 mM) | [form ]
Solid | [pka]
14.70±0.20(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity[1]. | [References]
[1] Fales KR, et al. Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransfera DOI:10.1021/acs.jmedchem.7b01046 |
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