[CAS NO. 1661839-45-7] CCT251545
PRODUCTS SPECIFICATIONS [1661839-45-7]
DESCRIPTION [1661839-45-7]
Overview
| MDL | MFCD29472582 |
|---|---|
| Molecular Weight | 421.92 |
| Molecular Formula | C23H24ClN5O |
| SMILES | O=C1NCCC12CCN(C3=C(Cl)C=NC=C3C4=CC=C(C5=CN(C)N=C5)C=C4)CC2 |
1 Publications Citing Use of MCE
Summary
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 IC
50
of 0.035 μM
[1]
.
CCT251545 has weak inhibition of tankyrase enzymes (TNKS1 IC
50
> 10 μM, TNKS2 IC
50
= 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 IC
50
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. |
Appearance
Solid
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
DMSO : ≥ 50 mg/mL ( 118.51 mM )
* "≥" means soluble, but saturation unknown.
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 |
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.
- [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.
