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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-AZD0364
AZD0364

Chemical Structure : AZD0364

CAS No.: 2097416-76-5

AZD0364 (Tizaterkib, AZD-0364)

货号: PC-63271Not For Human Use, Lab Use Only.

Tizaterkib (AZD0364) is a potent, selective, ATP competitive, orally active ERK1/2 inhibitor with IC50 of 0.66 nM in ERK2 biochemical assay, binds similarly to ERK1 and ERK2 with Ki of 3.9 and 3.8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tizaterkib (AZD0364) is a potent, selective, ATP competitive, orally active ERK1/2 inhibitor with IC50 of 0.66 nM in ERK2 biochemical assay, binds similarly to ERK1 and ERK2 with Ki of 3.9 and 3.8 nM.
AZD0364 inhibits p90RSK phosphorylation with an IC50 of 5.74 nM in an A375 melanoma cell line containing a BRAFV600E mutation.
AZD0364 potently inhibits ERK1/2 phosphorylation with IC50 of 1.73 nM, which is more potent than the reported ERK1/2 competitors, SCH772984, GDC-0994, and BVD-523 (ulixertinib).
AZD0364 is highly selective for ERK1/2 in a broader panel of 353 human kinases, with activity against only nine other kinases in this panel: MEK1, COT, BRAF, MEK2, c-RAF, ERK7, CDK2, CDK5, and ARK5.
AZD0364 directly modulates RAS/MAPK pathway signaling, demonstrates in vivo antitumor activity in KRAS- and BRAF-mutant cancer cell line xenograft models.

物理化学性质&存储条件

分子量 494.507
分子式 C24H24F2N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6R)-7-(3,4-Difluorobenzyl)-6-(methoxymethyl)-2-{5-methyl-2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl}-6,7-dihydroimidazo[1,2-a]pyrazin-8(5H)-one

参考文献

1. Flemington V, et al. Mol Cancer Ther. 2021 Feb;20(2):238-249.
2. Ward RA, et al. J Med Chem. 2019 Dec 26;62(24):11004-11018.

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