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

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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)
color: White to off-white
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|

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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..…

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0101412
Product name: ERK1/2inhibitor2
Purity: 99.61%
Packaging: 5mg
Price: $400
Updated: 2021/12/16

ChemScene

Product number: CS-0101412
Product name: ERK1/2inhibitor2
Purity: 99.61%
Packaging: 10mg
Price: $680
Updated: 2021/12/16

ChemScene

Product number: CS-0101412
Product name: ERK1/2inhibitor2
Purity: 99.61%
Packaging: 25mg
Price: $1350
Updated: 2021/12/16

ChemScene

Product number: CS-0101412
Product name: ERK1/2inhibitor2
Purity: 99.61%
Packaging: 50mg
Price: $2200
Updated: 2021/12/16

ChemScene

Product number: CS-0101412
Product name: ERK1/2inhibitor2
Purity: 99.61%
Packaging: 100mg
Price: $3400
Updated: 2021/12/16

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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].

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

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ASTX-029 Suppliers

China 33 United States 4 Global 37

Wuhan Jingkangen Biomedical Technology Co., Ltd

Tel: 13720134139 13720134139
Email: orders@jknbiochem.com
Country: China
ProdList: 5821
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3466
Advantage: 58

Shanghai Taibao Pharmaceutical Technology Co., Ltd.

Tel: 13816752554
Email: 1745533547@qq.com
Country: China
ProdList: 129
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4566
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8012
Advantage: 62

ChengDu TongChuangYuan Pharmaceutical Co.Ltd

Tel: 028-83379370 13880556291
Fax: 028-87747383
Email: tcy@tcypharm.com
Country: China
ProdList: 6270
Advantage: 58

Chuzhou KeMail Chemical Technology Co., Ltd

Tel: 0550-5196001 15000891977
Fax: 0550-5196001
Email: wj520wjxby@126.com
Country: China
ProdList: 1925
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Kaixin Chemical (Hong Kong) Limited

Tel: 010-88886666-01 13112345678
Fax: CDXH21@126.com
Email: loyson@tcypharm.com
Country: China
ProdList: 595
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Jiaxing Deyi Chemical Co., Ltd.

Tel: 0573-86-0573-85866609 13325730825
Fax: 0573-85866609
Email: 945717149@qq.com
Country: China
ProdList: 8024
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32161
Advantage: 58

2095719-92-7, ASTX-029Related Search:

ASTX-029

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)-

(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

ERK1/2 inhibitor 2(ASTX-029)

ERK1/2 inhibitor 2

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

2095719-92-7

C29H31ClFN5O5