Beroterkib

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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

(alphaR)-6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-alpha-methyl-1-oxo-2H-isoindole-2-acetamide

(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

US10457669,

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

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 KHSO ₄(10 ml), NaHCO ₃(10 ml), brine (2×10 ml) and then water (4×10 ml), was dried (MgSO ₄) and evaporated. The residue was purified by chromatography (SiO ₂, 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 (2×1 ml) and dried under vacuum at 50° C. overnight to give the title compound (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

US10457669,

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

Tags: 14FDK6ISC9, Antineoplastic, ASTX 029, ASTX029, Beroterkib, Beroterkib anhydrous, extracellular signal-regulated kinases (ERK) inhibitor

By DR ANTHONY MELVIN CRASTO Ph.D in Antineoplastic on January 8, 2026.

Latest Posts

Beroterkib
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 (alphaR)-6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-alpha-methyl-1-oxo-2H-isoindole-2-acetamide (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]propanamideextracellular signal-regulated kinases (ERK) inhibitor, antineoplastic, ASTX029, ASTX 029, 14FDK6ISC9, Beroterkib anhydrous, AT 35029 Beroterkib…
Balinatunfib
Balinatunfib CAS 2248726-53-4 MF C27H24F2N6O2, 502.5 g/mol (1R,11R)-5-[2-(1-aminocyclobutyl)pyrimidin-5-yl]-18-(difluoromethoxy)-12-methyl-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-13-one (7R,14R)-11-[2-(1-AMINOCYCLOBUTYL)-5-PYRIMIDINYL]-1-(DIFLUOROMETHOXY)-6,7-DIHYDRO-6-METHYL-7,14-METHANOBENZIMIDAZO[1,2-B][2,5]BENZODIAZOCIN-5(14H)-ONE (7R,14R)-11-[2-(1-Aminocyclobutyl)pyrimidin-5-yl]-1-(difluoromethoxy)-6-methyl-6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one (7R,14R)-11-[2-(1-aminocyclobutyl)pyrimidin-5-yl]-1-(difluoromethoxy)-6-methyl-6,7-dihydro-7,14-methano[1,3]benzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-onetumor necrosis factor (TNF) signaling inhibitor, SAR441566, SAR 441566, PLY98MAN4C Balinatunfib (SAR441566) is an experimental drug which…
Atirmociclib
Atirmociclib CAS 2380321-51-5 MF C22H27ClFN5O3, 463.9 g/mol (3S,4R)-4-[[5-chloro-4-[7-fluoro-2-(2-hydroxypropan-2-yl)-3-propan-2-ylbenzimidazol-5-yl]pyrimidin-2-yl]amino]oxan-3-ol (3S,4R)-4-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan2-yl)-1H-1,3-benzimidazol-6-yl]pyrimidin-2-yl}amino)oxan-3-ol 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxpropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-D-threo-pentitol D-threo-Pentitol, 1,5-anhydro-3-[[5-chloro-4-[4-fluoro-2-(1-hydroxy-1-methylethyl)-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinyl]amino]-2,3-dideoxy-cyclin-dependent kinase (CDK) inhibitor, antineoplastic, PF 07220060, S743GOJ5LJ, CDK4/6-IN-6 Atirmociclib is an orally bioavailable inhibitor…
Asaretoclax
Asaretoclax CAS 2363074-01-3 MF C47H57F2N7O7S, MW 902.1 g/mol 4-[4-[[2-[3-(difluoromethyl)-1-bicyclo[1.1.1]pentanyl]-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[(4-hydroxy-4-methylcyclohexyl)methylamino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((2-(3-(difluoromethyl)bicyclo[1.1.1]pentan-1-yl)-4,4-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)benzamide B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, GY6FD5FXA3, HY 159817, ABT 263 Asaretoclax is an orally bioavailable…

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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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

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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

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