LSN 3213128 |
| Catalog No.GC36486 |
LSN 3213128은 아미노이미다졸-4-카르복사미드 리보뉴클레오티드 포르밀트랜스퍼라제(AICARFT)에 대한 강력하고 특이적 억제 활성을 가진 선택적, 비고전적, 경구 생체이용성 항엽산제이며 IC50은 AICARFT 효소 억제에 대해 16nM이고 세포에서 19nM입니다. 항종양 활성.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1941211-99-9
Sample solution is provided at 25 µL, 10mM.
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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]. IC50: 16 nM (AICARFT), 19 nM (AICARFT in cells)[1]
[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.
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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