LSN 3213128

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. LSN 3213128 exhibits anti-tumor activity[1].

Product Specifications

CAS Number

[1941211-99-9]

UNSPSC

12352005

Target

Antifolate

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/lsn-3213128.html

Concentration

10mM

Purity

98.36

Solubility

DMSO : 83.33 mg/mL (ultrasonic)

Smiles

O=C1NC=CC2=C1C=C(NS(=O)(C3=CC=C(N4CC[C@@H](O)C4)S3)=O)C(F)=C2

Molecular Formula

C17H16FN3O4S2

Molecular Weight

409.46

References & Citations

[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.