2125500-60-7
Chemical Structure
DFX117
- CAS No.: 2125500-60-7
- Formula:C26H26F2N6O5S
- Molecular Weight:572.58
InChIKey: AOFNYCXYCYLTJD-UHFFFAOYSA-N
SMILES: O=C(C1=CN=C2C=CC(C3=CC(NS(=O)(C4=CC=C(C=C4F)F)=O)=C(OC)N=C3)=CN21)NCCN5CCOCC5
Biological Activity: DFX117 is an orally active PI3Kα/c-Met inhibitor. DFX117 blocks PI3K/Akt and Met downstream signaling through selective inhibition of PI3Kα (IC50 = 0.5 nM) and c-Met tyrosine kinase activity (IC50 = 17.1 nM), and induces G0/G1 phase arrest, caspase-dependent intrinsic apoptosis (apoptosis), and PTEN upregulation in non-small cell lung cancer cells, thereby inhibiting tumor growth. DFX117 can be used for research on non-small cell lung cancer[1][2].
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DFX117 | DFX117 is an orally active PI3Kα/c-Met inhibitor. DFX117 blocks PI3K/Akt and Met downstream signaling through selective inhibition of PI3Kα (IC50 = 0.5 nM) and c-Met tyrosine kinase activity (IC50 = 17.1 nM), and induces G0/G1 phase arrest, caspase-dependent intrinsic apoptosis (apoptosis), and PTEN upregulation in non-small cell lung cancer cells, thereby inhibiting tumor growth. DFX117 can be used for research on non-small cell lung cancer. | |||||||||||||||||||||
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References
- [1]. Fan Y, et al. Antitumor Activity of DFX117 by Dual Inhibition of c-Met and PI3Kα in Non-Small Cell Lung Cancer. Cancers. 2019 May 05;11(5):627. [Content Brief]
- [2]. Sun H, et al. Hepatocyte growth factor/c-Met signaling axis in human diseases: Mechanistic insights and therapeutic potential. Journal of cell communication and signaling. 2026 Jun;20(2):e70075.