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 a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers[1][2].
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HRX-0233 | 98.92% | HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers. | ||||||||||||||||||||
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- [1]. Jansen RA, et al. Small-molecule inhibition of MAP2K4 is synergistic with RAS inhibitors in KRAS-mutant cancers. Proc Natl Acad Sci U S A. 2024 Feb 27;121(9):e2319492121. [Content Brief]
- [2]. Tipayasri P. Development of Rational Combination Therapies for Patients with Metastatic Prostate Cancer and Loss of the PTEN Tumor Suppressor Gene[D]. , 2024.
Keywords
