2409140-12-9
Chemical Structure
HRX-0233
- CAS No.: 2409140-12-9
- Formula:C24H21F2N5O3S
- Molecular Weight:497.52
InChIKey: KWMYCLFOKISDSV-UHFFFAOYSA-N
SMILES: O=C(C1=CNC2=NC=C(C3=CN=C(C4CC4)N=C3)C=C21)C5=CC=C(C(NS(=O)(CCC)=O)=C5F)F
Biological Activity: HRX-0233 is an orally potent MAP2K4 inhibitor. HRX-0233 inhibits the MAP2K4-JNK-JUN signaling pathway, blocks the feedback activation of receptor tyrosine kinases, and sustains the inhibitory effect on KRAS signaling. HRX-0233 exerts synergistic inhibition on the mTORC1 and MAPK pathways. When combined with Ipatasertib (HY-15186) or Sotorasib (HY-114277), it produces synergistic antiproliferative, pro-apoptotic (apoptosis) and antitumor effects, and shows good tolerability in mouse models. HRX-0233 can be used in CRISPR knockout screens to identify vulnerability-related genes. HRX-0233 is applicable to research related to prostate cancer, non-small cell lung cancer and colorectal cancer[1][2].
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HRX-0233 | 98.92% | HRX-0233 is an orally potent MAP2K4 inhibitor. HRX-0233 inhibits the MAP2K4-JNK-JUN signaling pathway, blocks the feedback activation of receptor tyrosine kinases, and sustains the inhibitory effect on KRAS signaling. HRX-0233 exerts synergistic inhibition on the mTORC1 and MAPK pathways. When combined with Ipatasertib (HY-15186) or Sotorasib (HY-114277), it produces synergistic antiproliferative, pro-apoptotic (apoptosis) and antitumor effects, and shows good tolerability in mouse models. HRX-0233 can be used in CRISPR knockout screens to identify vulnerability-related genes. HRX-0233 is applicable to research related to prostate cancer, non-small cell lung cancer and colorectal cancer. | ||||||||||||||||||||
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References
- [1]. Tipayasri P. Development of Rational Combination Therapies for Patients with Metastatic Prostate Cancer and Loss of the PTEN Tumor Suppressor Gene[D]. , 2024.
- [2]. Jansen RA, et al. Small-molecule inhibition of MAP2K4 is synergistic with RAS inhibitors in -mutant cancers. Proceedings of the National Academy of Sciences of the United States of America. 2024 Feb 27;121(9):e2319492121. [Content Brief]
