CCT251545 is a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.
Chemical Formula: C23H24ClN5O
Exact Mass: 421.1669
Molecular Weight: 421.93
Elemental Analysis: C, 65.47; H, 5.73; Cl, 8.40; N, 16.60; O, 3.79
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
CCT251545 potently inhibits WNT pathway activity in COLO205-F1756 clone 4 (an APC -mutant human colorectal cancer cell line engineered to express a modified luciferase-based WNT reporter construct) with an IC50 of 0.035 μM.
CCT251545 has weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0).
CCT251545 is a potent and selective chemical probe for the human mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.
CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.
CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with an IC50 of 9 nM.
CCT251545 displays potent cell-based activity.
CCT251545 (70mg/kg; p.o.; twice daily) causes an inhibition of tumor growth in NCr athymic mice bearing established SW620 human colorectal cancer xenografts.
Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ,Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-80. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26. PubMed PMID: 26502155; PubMed Central PMCID: PMC4677459.
Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13. PubMed PMID: 25680029.
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