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
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M.Wt
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497.52
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Formula
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C24H21F2N5O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(3-(5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl) -2,6-difluorophenyl)propane-1-sulfonamide
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References
1. Robin A Jansen, et al. Proc Natl Acad Sci U S A. 2024 Feb 27;121(9):e2319492121.
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