LSN 3213128 |
| رقم الكتالوجGC36486 |
LSN 3213128 هو مضاد انتقائي ، غير كلاسيكي ، متاح حيويًا عن طريق الفم مع نشاط مثبط قوي ومحدد لأمينو إيميدازول-4-كاربوكساميد ريبونوكليوتيد فورميل ترانسفيراز (AICARFT) ، مع IC50 من 16 نانومتر لمثبط إنزيم AICARFT و 19 نانومتر في الخلايانشاط مضاد للورم
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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