CDK8-IN-16
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1860885-61-5
- 화학식: C23H22N6O2
- 분자량:414.46
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
CDK8 5.1 nM (IC50) |
CDK19 5.6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | IC50 |
17.9 nM
Compound: 51
|
In vivo inhibition of STAT1 phosphorylation at ser727 in human SW620 cells harboring APC mutation xenografted in mouse administered through oral gavage every 24 hrs measured after 2 to 24 hrs post last dose by Western blot analysis
In vivo inhibition of STAT1 phosphorylation at ser727 in human SW620 cells harboring APC mutation xenografted in mouse administered through oral gavage every 24 hrs measured after 2 to 24 hrs post last dose by Western blot analysis
|
[PMID: 27326329] |
Chemical Information
-
CAS No. 1860885-61-5
-
분자량 414.46
-
화학식 C23H22N6O2
-
SMILES
O=C(N1CC(C1)OC)C2=NC3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC(N)=C3C=C2
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK8-IN-16 Related Classifications
HY-171174 Related Classifications
Powered by Bioz