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ASTX-029

编号: 20298
Cas号: 2095719-92-7
纯度: 98% Min.

ASTX029 is a highly potent and selective dual-mechanism ERK inhibitor. ASTX029 inhibits both ERK catalytic activity and the phosphorylation of ERK itself by MEK, despite not directly inhibiting MEK activity. ASTX029 preferentially inhibited the proliferation of MAPK-activated cell lines, including those with BRAF or RAS mutations. ASTX029 also demonstrated activity in both in vitro and in vivo models of acquired resistance to MAPK pathway inhibitors.

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化学信息

名称ASTX-029
Iupac 化学名称(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
同义词ASTX-029; ASTX029; ASTX 029;
英文同义词ASTX-029; ASTX029; ASTX 029;
分子式C29H31ClFN5O5
分子量584.04
SmileClC(C(C1=CC=C2C(C(N([C@H](C)C(N[C@H](CO)C3=CC(OC)=CC(F)=C3)=O)C2)=O)=C1)=N4)=CN=C4NC5CCOCC5
InChiKeyBVRGQPJKSKKGIH-PUAOIOHZSA-N
InChiInChI=1S/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-/m1/s1
Cas号2095719-92-7
相关CAS号

订购信息

包装价格库存纯度备货期
大货询价询价询价
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外观性状固体粉末
纯度98% Min.
存储短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度
可溶性溶于DMSO
处理方式
运输条件作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Heightman TD, Berdini V, Bevan L, Buck IM, Carr MG, Courtin A, Coyle JE, Day JEH, East C, Fazal L, Griffiths-Jones CM, Howard S, Kucia-Tran J, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Peakman TM, Reader M, Rees DC, Rich SJ, Shah A, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2021 Aug 26;64(16):12286-12303. doi: 10.1021/acs.jmedchem.1c00905. Epub 2021 Aug 13. PMID: 34387469.

2: Munck JM, Berdini V, Bevan L, Brothwood JL, Castro J, Courtin A, East C, Ferraldeschi R, Heightman TD, Hindley CJ, Kucia-Tran J, Lyons JF, Martins V, Muench S, Murray CW, Norton D, O'Reilly M, Reader M, Rees DC, Rich SJ, Richardson CJ, Shah AD, Stanczuk L, Thompson NT, Wilsher NE, Woolford AJ, Wallis NG. ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK. Mol Cancer Ther. 2021 Oct;20(10):1757-1768. doi: 10.1158/1535-7163.MCT-20-0909. Epub 2021 Jul 30. PMID: 34330842.


化学结构

20298 - ASTX-029 | CAS 2095719-92-7

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