Art. -Nr.: HY-12681

CCT251545

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC₅₀ of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

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Reinheit: 99.39%
CAS. Nr.: 1661839-45-7
Formel: C₂₃H₂₄ClN₅O
Molecular Weight:421.92

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CCT251545 Chemical Structure

CAS. Nr.: 1661839-45-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC₅₀ of 5 nM in 7dF3 cells^[1]. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease^[2].

IC₅₀ & Target

IC50: 5 nM (WNT, 7dF3 cells)^[1]

Alle Wnt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	35.85 μM Compound: CCT251545	Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
COLO 205	GI₅₀	37.73 μM Compound: CCT251545	Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
COLO 205	IC₅₀	0.035 μM Compound: 74, CCT251545	Inhibition of basal WNT signaling in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay Inhibition of basal WNT signaling in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay	[PMID: 25680029]
COLO 205	IC₅₀	35 nM Compound: 6; CCT251545	Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant	[PMID: 26796641]
CT26	GI₅₀	11.3 μM Compound: CCT-251545	Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
GES1	GI₅₀	42.7 μM Compound: CCT-251545	Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
HCT-116	GI₅₀	46.16 μM Compound: CCT251545	Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HCT-116	GI₅₀	9.6 μM Compound: CCT-251545	Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
HL-60	GI₅₀	>50 μM Compound: CCT251545	Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HT-29	GI₅₀	48.59 μM Compound: CCT251545	Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HT-29	GI₅₀	7.8 μM Compound: CCT-251545	Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
Kasumi 1	GI₅₀	37.03 μM Compound: CCT251545	Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
KG-1	GI₅₀	19.98 μM Compound: CCT251545	Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
KG-1a	GI₅₀	32.71 μM Compound: CCT251545	Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
LS174T	IC₅₀	0.023 μM Compound: 74, CCT251545	Inhibition of basal WNT signaling in human LS174T cells harboring beta-catenin mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay Inhibition of basal WNT signaling in human LS174T cells harboring beta-catenin mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay	[PMID: 25680029]
LS174T	IC₅₀	23 nM Compound: 6; CCT251545	Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant	[PMID: 26796641]
MCF7	GI₅₀	>50 μM Compound: CCT251545	Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MDA-MB-231	GI₅₀	29.91 μM Compound: CCT251545	Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MDA-MB-453	GI₅₀	43.06 μM Compound: CCT251545	Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MOLM-13	GI₅₀	2.8 μM Compound: CCT251545	Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MV4-11	GI₅₀	0.03 μM Compound: CCT251545	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay	[PMID: 33571827]
NB-4	GI₅₀	>50 μM Compound: CCT251545	Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
PA-1	IC₅₀	0.007 μM Compound: 74, CCT251545	Inhibition of ligand-induced WNT3A signaling in human PA-1 cells harboring TCF preincubated for 6 hrs before ligand addition measured after 24 hrs by luciferase reporter assay Inhibition of ligand-induced WNT3A signaling in human PA-1 cells harboring TCF preincubated for 6 hrs before ligand addition measured after 24 hrs by luciferase reporter assay	[PMID: 25680029]
PA-1	IC₅₀	20 nM Compound: 6; CCT251545	Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells	[PMID: 26796641]
PANC-1	GI₅₀	0.55 μM Compound: CCT251545	Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
SW480	GI₅₀	10.4 μM Compound: CCT-251545	Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
SW480	IC₅₀	0.19 μM Compound: 74, CCT251545	Inhibition of basal WNT signaling in human SW480 cells harboring APC mutant Inhibition of basal WNT signaling in human SW480 cells harboring APC mutant	[PMID: 25680029]
SW480	IC₅₀	190 nM Compound: 6; CCT251545	Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant	[PMID: 26796641]
T47D	GI₅₀	15.05 μM Compound: CCT251545	Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
THP-1	GI₅₀	>50 μM Compound: CCT251545	Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
U-937	GI₅₀	22.44 μM Compound: CCT251545	Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
WI-38	GI₅₀	>50 μM Compound: CCT251545	Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]

In Vitro

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^[1].
CCT251545 has weak inhibition of tankyrase enzymes (TNKS1 IC₅₀ > 10 μM, TNKS2 IC₅₀ = 15.0)^[1].
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^[2].
CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1^[2].
CCT251545 also reduces phospho-STAT1^SER727 levels in SW620 cells with an IC₅₀ of 9 nM^[2].
CCT251545 displays potent cell-based activity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CCT251545 (70mg/kg; p.o.; twice daily) causes an inhibition of tumor growth in NCr athymic mice bearing established SW620 human colorectal cancer xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6-8 weeks female NCr athymic mice bearing established SW620 xenografts^[2]
Dosage:

70mg/kg
Administration:

Oral administration; twice daily; from days 0-7 and days 10-14
Result:

Caused an inhibition of tumor growth with a 70% reduction in final tumor weight relative to control.

Chemical Information

CAS. Nr. 1661839-45-7
Appearance Solid
Molecular Weight 421.92
Formel C₂₃H₂₄ClN₅O
Color White to off-white
SMILES

O=C1NCCC12CCN(C3=C(Cl)C=NC=C3C4=CC=C(C5=CN(C)N=C5)C=C4)CC2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Clin Transl Med

Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology. [Abstract]

2022 Jul;12(7):e961. PMID: 35839307
Br J Cancer

Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma. [Abstract]

2023 May;128(10):1941-1954. PMID: 36959380

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (118.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3701 mL

11.8506 mL

23.7012 mL

5 mM

0.4740 mL

2.3701 mL

4.7402 mL

10 mM

0.2370 mL

1.1851 mL

2.3701 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.67 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.67 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mallinger A, et al. 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. [Content Brief]

[2]. 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):973-980. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3701 mL	11.8506 mL	23.7012 mL	59.2529 mL
	5 mM	0.4740 mL	2.3701 mL	4.7402 mL	11.8506 mL
	10 mM	0.2370 mL	1.1851 mL	2.3701 mL	5.9253 mL
	15 mM	0.1580 mL	0.7900 mL	1.5801 mL	3.9502 mL
	20 mM	0.1185 mL	0.5925 mL	1.1851 mL	2.9626 mL
	25 mM	0.0948 mL	0.4740 mL	0.9480 mL	2.3701 mL
	30 mM	0.0790 mL	0.3950 mL	0.7900 mL	1.9751 mL
	40 mM	0.0593 mL	0.2963 mL	0.5925 mL	1.4813 mL
	50 mM	0.0474 mL	0.2370 mL	0.4740 mL	1.1851 mL
	60 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9875 mL
	80 mM	0.0296 mL	0.1481 mL	0.2963 mL	0.7407 mL
	100 mM	0.0237 mL	0.1185 mL	0.2370 mL	0.5925 mL

Keywords

CCT251545

3 Cited Publications

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CCT251545

Differentiation Inducing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) CCT251545

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCT251545

Differentiation Inducing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) CCT251545

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCT251545 Related Classifications

HY-12681 Related Classifications