LSN 3213128

Names

[ CAS No. ]:
1941211-99-9

[ Name ]:
LSN 3213128

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate

[Target]

IC50: 16 nM (AICARFT), 19 nM (AICARFT in cells)[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 Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model. J Med Chem. 2017 Dec 14;60(23):9599-9616.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₆FN₃O₄S₂

[ Molecular Weight ]:
409.46

Related Compounds

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