Chemical Structure : OICR19451
CAS No.:
2803349-61-1
OICR19451
(OICR-19451)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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593.09
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Formula
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C26H31ClF2N8O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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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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3-((5-Chloro-2-((2-(difluoromethoxy)-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)thiophene-2-carboxamide
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References
1. Smil D, et al. Eur J Med Chem. 2026 Mar 31;311:118798.
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