CCT251545 analogue
CCT251545 analogue (CAS 1860885-61-5) is a potent, selective dual inhibitor of CDK8/19 and a regulator of transcription pathways. It plays a key role in tumor-associated signaling, particularly by inhibiting the WNT pathway and STAT1SER727 phosphorylation. By binding to critical sites in the CDK8 active pocket, it suppresses abnormal tumor cell proliferation and regulates biomarkers. In preclinical models, such as the SW620 xenograft, oral administration leads to sustained target inhibition and tumor growth suppression. This compound reduces STAT1SER727 phosphorylation levels in tumor tissues, enhancing its anti-tumor effects. CCT251545 analogue is a valuable molecular tool for studying CDK8/19 function and holds promise for the therapeutic development of colorectal and related cancers.
Reference:
Mallinger A, Schiemann K, Rink C, et al. 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. ACS Med Chem Lett. 2016 Mar 28;7(6):573-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 414.46 |
| Cas No. | 1860885-61-5 |
| Formula | C23H22N6O2 |
| Synonyms | Compound 51, CDK8/19-IN-51, CDK8-IN-16 |
| Solubility | ≥20.7 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
| Chemical Name | (5-amino-8-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)-1,6-naphthyridin-2-yl)(3-methoxyazetidin-1-yl)methanone |
| SDF | Download SDF |
| Canonical SMILES | C[n]1ncc(-c(cc2)ccc2-c(c2c3ccc(C(N(C4)CC4OC)=O)n2)cnc3N)c1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
SW620 cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
N/A |
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Applications |
In human colorectal carcinoma SW620 cells harboring an activating APC-mutation, CCT251545 analogue, Compound 51 potently inhibited phospho-STAT1SER727. |
| Animal experiment [1]: | |
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Animal models |
Mice bearing human colorectal carcinoma SW620 cells |
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Dosage form |
5 mg/kg; p.o.; b.i.d. |
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Applications |
In mice bearing human colorectal carcinoma SW620 cells, CCT251545 analogue, Compound 51, reduced phospho-STAT1SER727 level in a time-dependent manner. At the dose of 5 mg/kg, a b.i.d. schedule would be required in order to achieve the maximal inhibitory effect. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Mallinger A, Schiemann K, Rink C, et al. 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. |
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Quality Control & MSDS
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Chemical structure
