1. Stem Cell/Wnt
  2. Wnt
  3. CCT251545

CCT251545 

Cat. No.: HY-12681 Purity: 99.27%
Handling Instructions

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

CCT251545 Chemical Structure

CAS No. : 1661839-45-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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]

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-STAT1SER727 levels in SW620 cells with an IC50 of 9 nM[2].
CCT251545 displays potent cell-based activity[2].

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].

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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (118.51 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

CCT251545CCT 251545CCT-251545WntInhibitorinhibitorinhibit

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Product Name:
CCT251545
Cat. No.:
HY-12681
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