| Identification | Back Directory | [Name]
3-(1H-Pyrrolo[2,3-b]pyridin-5-yl)benzamide | [CAS]
918523-75-8 | [Synonyms]
CDK8-IN-13
3-(1H-Pyrrolo[2,3-b]pyridin-5-yl)benzamide | [Molecular Formula]
C14H11N3O | [MOL File]
918523-75-8.mol | [Molecular Weight]
237.26 |
| Hazard Information | Back Directory | [Uses]
CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity[1]. | [in vivo]
CDK8-IN-13 (40, 80 mg/kg; p.o.; for 15 days) inhibits tumor growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of CDK8-IN-13 in Sprague-Dawley rats[1].
| dose/routes | t1/2 (h) | Tmax (h) | MRT(h)/td>
| Cmax (μg/L) | AUC0-∞ (μg/L × h) | CL (mL/h/kg) | F (%) | | 10 mg/kg (po) | 1.40 | 1.00 | 2.47 | 206.1 | 434.09 | 17.12 | 28.00 | | 2 mg/kg (iv) | 0.81 | 0.083 | 1.50 | 230.7 | 310.02 | 7.05 | / |
Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po [1]| Animal Model: | 6-week-old Balb/C mice (C1498 cells)[1] | | Dosage: | 40, 80 mg/kg | | Administration: | P.o.; for 15 days | | Result: | Decreased the tumor growth with no significant weight loss, the expression of Ki67 decreased in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated. |
| [IC 50]
CDK8: 51.9 nM (IC50) | [References]
[1] Zhang XX, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia. Eur J Med Chem. 2023 May 5;251:115214. DOI:10.1016/j.ejmech.2023.115214 |
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