Catalog No.: PC-21212Not For Human Use, Lab Use Only.
MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively.
MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively.
MTX-241F not only targets intrinsic vulnerabilities of DIPG encompassing DNA repair and PI3K signal activation, but also EGFR signaling, a key driver of radioresistance.
MTX-241F inhibits DNA repair and PI3K and prevent feedback activation of EGFR-mediated survival signaling in Diffuse Intrinsic Pontine Glioma (DIPG) cells.
MTX-241F sensitizes DIPGs to RT through its inhibition of DNA repair and survival signaling.
MTX-241F (75 mg/kg, oral gavage daily) exhibits tumor growth inhibition in vivo in DIPG, demonstrates exquisite cell kill and synergy in DIPG when combined with inhibition of non-homologous end joining (NHEJ).
