Chemical Structure : CK2 inhibitor 7h
CAS No.:
1461658-59-2
CK2 inhibitor 7h
Catalog No.: PC-22047Not For Human Use, Lab Use Only.
CK2 inhibitor 7h is a potent, selective Casein Kinase 2 (CK2) inhibitor with IC50 of <3 nM and SPR KD of 6.33 pM, pAKTS129 IC50 of 4 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CK2 inhibitor 7h is a potent, selective Casein Kinase 2 (CK2) inhibitor with IC50 of <3 nM and SPR KD of 6.33 pM, pAKTS129 IC50 of 4 nM.
CK2 inhibitor 7h potently inhibits the Wnt pathway with IC50 of 43 nM using the DLD-1 Topflash reporter assay.
CK2 inhibitor 7h dispalys limited off-target activity (12 kinases with >50% inhibition) against a panel of 402 kinases at 0.1 uM.
CK2 inhibitor 7h dose-dependently modulates the downstream markers pAKTS129 and β-catenin in SW620 tumor-bearing murine xenografts.
CK2 inhibitor 7h (30 mg/kg) showed a dose-dependent tumor growth inhibition, achieving 94% TGI in a HCT-116 (β-catenin mutant/model) and 74% TGI in a SW620 (APC mutant) model.
Physicochemical Properties
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M.Wt
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419.49
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Formula
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C21H25N9O
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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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N-(2-((2-aminoethyl)(methyl)amino)-5-((3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl)amino)phenyl)acetamide
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References
1. Dowling JE, et al. ACS Med Chem Lett. 2016 Jan 20;7(3):300-5.
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