ASTX-029
- Product Name
- 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
- Formula Weight
- 584.05
- MOL File
- 2095719-92-7.mol
ASTX-029 Property
- Density
- 1.387±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 250 mg/mL (428.05 mM)
- form
- A crystalline solid
- pka
- 13.39±0.46(Predicted)
- InChI
- InChI=1/C29H31ClFN5O5/c1-16(27(38)34-25(15-37)19-9-20(31)12-22(10-19)40-2)36-14-18-4-3-17(11-23(18)28(36)39)26-24(30)13-32-29(35-26)33-21-5-7-41-8-6-21/h3-4,9-13,16,21,25,37H,5-8,14-15H2,1-2H3,(H,34,38)(H,32,33,35)/t16-,25-/s3
- 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|
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-0101412
- Product name
- ERK1/2inhibitor2
- Purity
- 99.61%
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0101412
- Product name
- ERK1/2inhibitor2
- Purity
- 99.61%
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0101412
- Product name
- ERK1/2inhibitor2
- Purity
- 99.61%
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-0101412
- Product name
- ERK1/2inhibitor2
- Purity
- 99.61%
- Packaging
- 50mg
- Price
- $2200
- Updated
- 2021/12/16
- Product number
- CS-0101412
- Product name
- ERK1/2inhibitor2
- Purity
- 99.61%
- Packaging
- 100mg
- Price
- $3400
- Updated
- 2021/12/16
ASTX-029 Chemical Properties,Usage,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].
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.
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
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- +1-2135480471 +1-2135480471
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