CCT251545

Name: CCT251545
Brand: MedChemExpress
SKU: HY-12681
Rating: 5.0 (2 reviews)

Cat. No.: HY-12681 Purity: 99.39%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

CCT251545 Chemical Structure

CAS No. : 1661839-45-7

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE CCT251545

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

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	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	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]
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]
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]
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]
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.

Molecular Weight

421.92

Formula

C₂₃H₂₄ClN₅O

CAS No.

1661839-45-7

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.39%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (260 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

CCT251545 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCT2515451661839-45-7CCT 251545CCT-251545WntInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

CCT251545

Customer Review

CCT251545 Related Antibodies

2 Publications Citing Use of MCE CCT251545

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

CCT251545 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CCT251545 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report