Chemical Structure : LIB3S0280
CAS No.:
LIB3S0280
Catalog No.: PC-23440Not For Human Use, Lab Use Only.
LIB3S0280 is a potent TANK-binding kinase 1 (TBK1) inhibitor with IC50 of 493.9 nM, inhibits TBK1 downstream signaling.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LIB3S0280 is a potent TANK-binding kinase 1 (TBK1) inhibitor with IC50 of 493.9 nM, inhibits TBK1 downstream signaling.
LIB3S0280 suppresses pancreatic cancer growth and exert cytotoxic effects on high TBK1-expressing pancreatic cancer cells (MIA PaCa-2, MTT IC50=7.5 uM, 72h).
LIB3S0280 decreases phosphorylation of IκBα, phosphorylation level of AKT on the ser473 in pancreatic cancer cell lines.
LIB3S0280 treatment (96 h), the KRAS G12D-mutant pancreatic cancer cell line (PANC-1) exhibited a GI50 value of 4.71 μM and an IC50 value of 10.98 μM, while the KRAS G12C-mutant pancreatic cancer cell line (MIA PaCa-2) showed a GI50 value of 2.24 μM and an IC50 value of 6.64 μM.
LIB3S0280 treatment leads to G2/M arrest and induces apoptosis in pancreatic cancer cells, increases the granularity of pancreatic cells.
Physicochemical Properties
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M.Wt
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460.92
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Formula
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C22H25ClN4O5
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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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4-(2-((5-chloro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)ethyl)-2-methoxyphenol
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References
1. Wan-Hsi Shih, et al. Int J Biol Macromol. 2024 Nov 6:137296.
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