Chemical Structure : MTX-241F
CAS No.:
MTX-241F
(MTX241F)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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392.82
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Formula
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C20H14ClFN6
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(4-(6-chloro-5-fluoroindolin-1-yl)quinazolin-6-yl)pyrimidin-2-amine
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References
1. Monika Sharma, et al. Mol Cancer Ther. 2023 Sep 19. doi: 10.1158/1535-7163.MCT-23-0026.
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