MTX-241F | EGFR inhibitor | Probechem Biochemicals

Chemical Structure : MTX-241F

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MTX-241F (MTX241F)

货号: 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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生物&药学活性

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).

物理化学性质&存储条件

分子量	392.82
分子式	C20H14ClFN6
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(4-(6-chloro-5-fluoroindolin-1-yl)quinazolin-6-yl)pyrimidin-2-amine

参考文献

1. Monika Sharma, et al. Mol Cancer Ther. 2023 Sep 19. doi: 10.1158/1535-7163.MCT-23-0026.

MTX-241F (MTX241F)

生物&药学活性

物理化学性质&存储条件

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MTX-241F (MTX241F)

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物理化学性质&存储条件

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