Beroterkib
CAS 2095719-92-7
MF C29H31ClFN5O5 MW584.0 g/mol
(2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1,3-dihydro-2H-1-oxoisoindol-2-yl) -N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide
(2R)-2-[5-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxo-1H-isoindol-2-yl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide
(2R)-2-[5-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxo-1H-isoindol-2-yl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide
extracellular signal-regulated kinases (ERK) inhibitor, antineoplastic, ASTX029, ASTX 029, 14FDK6ISC9, Beroterkib anhydrous, AT 35029
Beroterkib Anhydrous is the anhydrous form of beroterkib, an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. Upon administration, beroterkib specifically binds to and inhibits both ERK 1 and 2, thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The MAPK/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in the proliferation, differentiation and survival of tumor cells.
- Study of ASTX029 in Subjects With Advanced Solid TumorsCTID: NCT03520075Phase: Phase 1/Phase 2Status: CompletedDate: 2025-07-03
- Phase I/II Study of a Combination of Decitabine and Cedazuridine (ASTX727) and ASTX029, an ERK Inhibitor, for Patients With RAS Pathway Mutant Myelodysplastic Syndromes and Myelodysplastic/Myeloproliferative NeoplasmsCTID: NCT06284460Phase: Phase 1/Phase 2Status: WithdrawnDate: 2024-10-24
- A Phase 1 Study to Evaluate the Effect of Food on Pharmacokinetics of ASTX029CTID: NCT04466514Phase: Phase 1Status: CompletedDate: 2024-08-02
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017068412&_cid=P21-MK4TZX-17603-1
Example 685: (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro- 1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide
A stirred solution of (R)-2-(6-(5-chloro-2-((oxan-4-yl)amino)pyrimidin-4-yl)-1-oxoisoindolin-2- yl)propanoic acid (70 mg, 0.168 mmol), (S)-2-amino-2-(3-fluoro-5-methoxyphenyl)ethanol, HCl (41 mg, 0.185 mmol) and triethylamine (0.094 ml, 0.672 mmol) in DMF (1 ml) was treated with TBTU (65 mg, 0.202 mmol) and stirred at room temperature overnight. The mixture was diluted with ethyl acetate (20 ml), was washed successively with 1M KHSO4 (10 ml), NaHCO3 (10 ml), brine (2x 10 ml) and then water (4x 10 ml), was dried (MgSO4) and evaporated. The residue was purified by chromatography (SiO2, 12 g column, 0- 5% EtOOH in EtOAc) to give a glass, which was triturated with ether (2 ml) to give a solid. The solid was collected by filtration, washed with ether (2x 1 ml) and dried under vacuum at 50°C overnight to give the titlecompound (64.3 mg, 64.3 %) as a cream solid. 1H NMR (DMSO, 400 MHz) δ 8.56 (1H, d), 8.44 (1H, s), 8.07 ‒ 8.00 (1H, m), 7.97 (1H, dd), 7.74 (1H, d), 7.61 (1H, s), 6.76 ‒ 6.64 (3H, m), 4.99 (1H, q), 4.91 (1H, t), 4.86 ‒ 4.70 (2H, m), 4.60 (1H, d), 4.00 ‒ 3.80 (3H, m), 3.76 (3H, s), 3.60 ‒ 3.47 (2H, m), 3.40 ‒ 3.33 (2H, m), 1.84 (2H, d), 1.59 ‒ 1.39 (5H, m). ). LCMS: [M+H]+ = 584.
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=US237389744&_cid=P21-MK4U5F-21416-1
Example 685: (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide
SYN
PAT
- Conjugates comprising hydroxyalkyl starch and a cytotoxic agent and process for their preparationPublication Number: AU-2011276120-B2Priority Date: 2010-07-09Grant Date: 2013-12-19
- Conjugates comprising hydroxyalkyl starch and a cytotoxic agent and process for their preparationPublication Number: AU-2011276120-A1Priority Date: 2010-07-09
- Combustion modified flexible polyurethane foamPublication Number: GB-2124634-APriority Date: 1982-07-26
- Benzolactam compounds as protein kinase inhibitorsPublication Number: ES-2989326-T3Priority Date: 2015-10-21Grant Date: 2024-11-26
- Protein kinase inhibitor benzolactam compoundsPublication Number: CN-114948963-APriority Date: 2015-10-21
- Benzolactam compounds as protein kinase inhibitorsPublication Number: US-2024368136-A1Priority Date: 2015-10-21
- Protein Kinase Inhibitors Benzolactam CompoundsPublication Number: CN-108617166-BPriority Date: 2015-10-21Grant Date: 2022-05-17
- Benzolactam compounds as protein kinase inhibitorsPublication Number: CN-114948963-BPriority Date: 2015-10-21Grant Date: 2025-05-27
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REF
- Discovery of ASTX029, a clinical candidate which modulates the phosphorylation and catalytic activity of ERK1/2Publication Name: Journal of Medicinal ChemistryPublication Date: 2021-10-06PMID: 34387469DOI: 10.1021/acs.jmedchem.1c00905
- ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERKPublication Name: Molecular Cancer TherapeuticsPublication Date: 2021-07-30PMID: 34330842DOI: 10.1158/1535-7163.mct-20-0909
//////////////Beroterkib, extracellular signal-regulated kinases (ERK) inhibitor, antineoplastic, ASTX029, ASTX 029, 14FDK6ISC9, Beroterkib anhydrous, AT 35029