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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-AMPK-OICR19451
OICR19451

Chemical Structure : OICR19451

CAS No.: 2803349-61-1

OICR19451 (OICR-19451)

货号: PC-26480Not For Human Use, Lab Use Only.

OICR19451 is a potent and selective dual NUAK1/2 and MARK2/3 inhibitor with IC50 of 12/10 nM for NUAK1/NUAK2, 101/124 nM for MARK2/MARK3 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

OICR19451 is a potent and selective dual NUAK1/2 and MARK2/3 inhibitor with IC50 of 12/10 nM for NUAK1/NUAK2, 101/124 nM for MARK2/MARK3 respectively.
OICR19451 showed >200-fold selectivity over MST1 (IC50=2064 nM), MST2 (IC50 = 3493 nM) and LATS1 (IC50 = 3607 nM) with reduced selectivity (45-fold) over only LATS2 (IC50 = 454 nM).
OICR19451 increases YAP phosphorylation in MDA-MB-231 breast cancer cells with EC50 of 125 nM, potently inhibit YAP/TAZ nuclear translocation, decreases expression of the YAP/TAZ target genes ANKRD1 and CTGF.
OICR19451 (30, 60 mg/kg, p.o. QD) demonstrated good tumor growth inhibition and prolongation of survival in orthotopic metastatic TNBC model, decreased YAP/TAZ protein levels.

物理化学性质&存储条件

分子量 593.09
分子式 C26H31ClF2N8O2S
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

3-((5-Chloro-2-((2-(difluoromethoxy)-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)thiophene-2-carboxamide

参考文献

1. Smil D, et al. Eur J Med Chem. 2026 Mar 31;311:118798.

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