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CCT251545

Chemical Structure : CCT251545

CAS No.: 1661839-45-7

CCT251545 (CCT 251545;CCT-251545)

Catalog No.: PC-43145Not For Human Use, Lab Use Only.

CCT251545 is a potent, orally bioavailable inhibitor of Wnt signaling with IC50 of 5 nM, also is a potent and selective chemical probe for CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CCT251545 is a potent, orally bioavailable inhibitor of Wnt signaling with IC50 of 5 nM, also is a potent and selective chemical probe for CDK8 and CDK19 with >100-fold selectivity over 291 other kinases; potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand with IC50 of 23 and 190 nM, respectively; demonstrates potent inhibition of WNT pathway activity in APC mutant human colorectal cancer cell line with IC50 of 35 nM; inhibits phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM; demonstrate in vivo activity in WNT-dependent tumors.

Physicochemical Properties

M.Wt 421.9225
Formula C23H24ClN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 50 mg/mL

Chemical Name/SMILES

2,8-Diazaspiro[4.5]decan-1-one, 8-[3-chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-

References

1. Mallinger A, et al. J Med Chem. 2015 Feb 26;58(4):1717-35.

2. Dale T, et al. Nat Chem Biol. 2015 Dec;11(12):973-980.

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