Chemical Structure : YAP1-TEAD inhibitor MRK-A
CAS No.:
2821763-12-4
YAP1-TEAD inhibitor MRK-A
货号: PC-26276Not For Human Use, Lab Use Only.
MRK-A is a highly potent, selective, orally bioavailable inhibitor of YAP1/TEAD with EC50 of 3.4 nM in cellular MCF7 assay expressing TEAD-reporter luciferase, inhibits TEAD palmitoylation that leads to allosteric YAP1/TEAD complex disruption.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
MRK-A is a highly potent, selective, orally bioavailable inhibitor of YAP1/TEAD with EC50 of 3.4 nM in cellular MCF7 assay expressing TEAD-reporter luciferase, inhibits TEAD palmitoylation that leads to allosteric YAP1/TEAD complex disruption.
MRK-A exhibits potent cell growth inhibition in the Hippo pathway-deficient NCI-H226 and MSTO-211H vs proficient NCI-H28 and NCI-2452 CTG assays.
MRK-A suppressed the transcription of endogenous YAP1/TEAD target genes in H226 cells
MRK-A (30 mg/kg BID) demonstrated dose-dependent efficacy in the NCI-H226 (mesothelioma) xenograft model, showed suppression of TEAD target genes ANKRD1 and CTGF in a dose-dependent manner over 24 h in NF2-deficient NCI-H226 (mesothelioma) tumor-bearing mice.
物理化学性质&存储条件
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分子量
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438.43
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分子式
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C19H17F3N4O3S
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-N-methyl-6-(4-(trifluoromethyl)phenoxy)pyridine-3-sulfonamide
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参考文献
1. Vara BA, et al. J Med Chem. 2026 Feb 26;69(4):4303-4316.
