CAS 1661839-45-7|CCT251545

Introduction：Basic information about CAS 1661839-45-7|CCT251545, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. CCT251545 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	CCT251545
CAS Number	1661839-45-7	Molecular Weight	421.923
Density	1.4±0.1 g/cm3	Boiling Point	709.7±60.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₄ClN₅O	Melting Point	/
MSDS	/	Flash Point	383.0±32.9 °C

Names

Name	CCT251545
Synonym	More Synonyms

CCT251545 BiologicalActivity

Description	CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: 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 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. 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. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1]
Related Catalog	Signaling Pathways >>Stem Cell/Wnt >>WntResearch Areas >>Cancer
References	[1]. Dale T, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-80. [2]. Mallinger A, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathwayscreen. J Med Chem. 2015 Feb 26;58(4):1717-35.

Description

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: 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 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. 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. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1]

Related Catalog

Signaling Pathways >>Stem Cell/Wnt >>WntResearch Areas >>Cancer

References

[1]. Dale T, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-80.

[2]. Mallinger A, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathwayscreen. J Med Chem. 2015 Feb 26;58(4):1717-35.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	709.7±60.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₄ClN₅O
Molecular Weight	421.923
Flash Point	383.0±32.9 °C
Exact Mass	421.166931
LogP	2.53
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.701
InChIKey	LBFYQISQYCGDDW-UHFFFAOYSA-N
SMILES	Cn1cc(-c2ccc(-c3cncc(Cl)c3N3CCC4(CCNC4=O)CC3)cc2)cn1
Storage condition	2-8℃

Synonyms

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

8-{3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl}-2,8-diazaspiro[4.5]decan-1-one

CCT251545

Recommended......