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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.
CCT251545 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.
CCT251545 demonstrates potent inhibition of WNT pathway activity in APC mutant human colorectal cancer cell line with IC50 of 35 nM.
CCT251545 inhibits phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM.
CCT251545 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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