CCT251545 is an orally active, potent WNT inhibitor with an IC50 value of 5 nM for WNT inhibition in 7dF3 cells.In addition, CCT251545 is a selective chemical probe for studies related to the roles of CDK8 and CDK19 in human diseases.
| Molecular Weight | 421.92 |
| Formula | C23H24ClN5O |
| CAS Number | 1661839-45-7 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Thomas G Boyer. Nat Chem Biol. Transcriptional kinases: Less is more (or less)
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FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. |
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| Foxy-5
Foxy-5, a WNT5A agonist and a mimetic peptide of WNT5A, triggers cytoplasmic free calcium signaling without affecting β-catenin activation and inhibits migration and invasion of epithelial cancer cells.Foxy-5 effectively reduces metastatic spread of prostate cancer cells with low WNT5A expression in an in situ mouse model. |
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