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

CCT251545 

Cat. No.: HY-12681 Purity: 99.34%
Handling Instructions

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells.

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

CCT251545 Chemical Structure

CCT251545 Chemical Structure

CAS No. : 1661839-45-7

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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
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10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
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100 mg USD 1200 In-stock
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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].

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].

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].

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

Purity: 99.34%

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