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Chemical Structure : MTX-241F
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.
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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).
| M.Wt | 392.82 | |
| Formula | C20H14ClFN6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Monika Sharma, et al. Mol Cancer Ther. 2023 Sep 19. doi: 10.1158/1535-7163.MCT-23-0026.
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