CK2 inhibitor 7h

Chemical Structure : CK2 inhibitor 7h

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	419.49
分子式	C21H25N9O
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	N-(2-((2-aminoethyl)(methyl)amino)-5-((3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl)amino)phenyl)acetamide

参考文献

1. Dowling JE, et al. ACS Med Chem Lett. 2016 Jan 20;7(3):300-5.

CK2 inhibitor 7h

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物理化学性质&存储条件

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CK2 inhibitor 7h

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