ASTX-029
- CAS No.
- 2095719-92-7
- Chemical Name:
- ASTX-029
- Synonyms
- ASTX-029;ERK1/2 inhibitor 2;ERK1/2 inhibitor 2(ASTX-029);ERK-1/2 inhibitor 2,Extracellular signal regulated kinases,Inhibitor,ASTX 029,ERK1/2 inhibitor 2,inhibit,ERK;(2R)-2-[6-[5-chloro-2-(tetrahydropyran-4-ylamino)pyrimidin-4-yl]-1-oxo-isoindolin-2-yl]-N-[(1S)-1-(3-fluoro-5-methoxy-phenyl)-2-hydroxy-ethyl]propanamide;(R)-2-(6-(5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1-oxoisoindolin-2-yl)-N-((S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl)propanamide;2H-Isoindole-2-acetamide, 6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-α-methyl-1-oxo-, (αR)-
- CBNumber:
- CB64664325
- Molecular Formula:
- C29H31ClFN5O5
- Molecular Weight:
- 584.05
- MDL Number:
- MFCD32874105
- MOL File:
- 2095719-92-7.mol
Density | 1.387±0.06 g/cm3(Predicted) |
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storage temp. | Store at -20°C |
solubility | DMSO: 250 mg/mL (428.05 mM) |
form | A crystalline solid |
pka | 13.39±0.46(Predicted) |
color | White to off-white |
InChIKey | BVRGQPJKSKKGIH-YZMAQOALNA-N |
SMILES | O=C1N(CC2=CC=C(C3C(=CN=C(NC4CCOCC4)N=3)Cl)C=C12)[C@H](C)C(=O)N[C@@H](C1C=C(F)C=C(OC)C=1)CO |&1:24,29,r| |
FDA UNII | 14FDK6ISC9 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 | |||||||||
NFPA 704 |
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ASTX-029 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0101412 | ERK1/2inhibitor2 99.61% | 2095719-92-7 | 5mg | $400 | 2021-12-16 | Buy |
ChemScene | CS-0101412 | ERK1/2inhibitor2 99.61% | 2095719-92-7 | 10mg | $680 | 2021-12-16 | Buy |
ChemScene | CS-0101412 | ERK1/2inhibitor2 99.61% | 2095719-92-7 | 25mg | $1350 | 2021-12-16 | Buy |
ChemScene | CS-0101412 | ERK1/2inhibitor2 99.61% | 2095719-92-7 | 50mg | $2200 | 2021-12-16 | Buy |
ChemScene | CS-0101412 | ERK1/2inhibitor2 99.61% | 2095719-92-7 | 100mg | $3400 | 2021-12-16 | Buy |
ASTX-029 Chemical Properties,Uses,Production
Description
ASTX-029 is a highly potent and selective dual-mechanism ERK inhibitor discovered using fragment-based drug design. Because of its distinctive ERK-binding mode, ASTX-029 inhibits both ERK catalytic activity and the phosphorylation of ERK itself by MEK despite not directly inhibiting MEK activity. This dual mechanism was demonstrated in cell-free systems, cell lines and xenograft tumor tissue, where the phosphorylation of both ERK and its substrate, ribosomal S6 kinase (RSK), were modulated on treatment with ASTX-029. Markers of sensitivity were highlighted in a large cell panel, where ASTX-029 preferentially inhibited the proliferation of MAPK-activated cell lines, including those with BRAF or RAS mutations[1].
Chemical Properties
White to off-white Solid
Uses
ASTX-029 is an orally bioavailable extracellular signal-regulated kinase 1/2 (ERK1/2) inhibitor. ASTX029 has the potential to potentially enhance anti-tumour activity in a wide range of tumour types, either as a single agent or in combination with other therapies. ASTX029 is currently in clinical studies for the treatment of relapsed/refractory solid tumours, including non-small cell lung cancer, melanoma, pancreatic cancer and colorectal cancer. Especially in KRAS-mutated NSCLC.
in vivo
In vivo, significant antitumor activity was observed in MAPK-activated tumor xenograft models following oral treatment. ASTX-029 also demonstrated activity in both in vitro and in vivo models of acquired resistance to MAPK pathway inhibitors.
IC 50
2.7 nM
References
[1] Munck, Joanne M. et al. “Supplementary Figures 1-7 from ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK.” 2023. 0.
ASTX-029 Preparation Products And Raw materials
Raw materials
Preparation Products
ASTX-029 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4692 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Suzhou ARTK Medchem Co., Ltd. | +8618168183658 | sales1@artkmedchem.com | China | 39009 | 58 |
Wuhan Jingkangen Biomedical Technology Co., Ltd | 13720134139 13720134139 | orders@jknbiochem.com | China | 5320 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3431 | 58 |
Shanghai Taibao Pharmaceutical Technology Co., Ltd. | 13816752554 | 1745533547@qq.com | China | 129 | 58 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4197 | 55 | |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8018 | 62 |