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HRX-0233

Chemical Structure : HRX-0233

CAS No.: 2409140-12-9

HRX-0233 (HRX0233)

Catalog No.: PC-21799Not For Human Use, Lab Use Only.

HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers.
Combination of sotorasib, a drug targeting KRASG12C, and the MAP2K4 inhibitor HRX-0233 prevents this feedback activation and is highly synergistic in a panel of KRASG12C-mutant lung and colon cancer cells.
Combining HRX-0233 and sotorasib is well-tolerated and resulted in durable tumor shrinkage in mouse xenografts of human lung cancer cells.
HRX-0233 combined with MEK inhibition suppresses tumor growth without toxicity in a H2122 xenograft model.

Physicochemical Properties

M.Wt 497.52
Formula C24H21F2N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-(5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl) -2,6-difluorophenyl)propane-1-sulfonamide

References

1. Robin A Jansen, et al. Proc Natl Acad Sci U S A. 2024 Feb 27;121(9):e2319492121.

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