CDK8-IN-13

• CAT Number: I041187
• CAS Number: 918523-75-8
• Molecular Formula: C14H11N3O
• Molecular Weight: 237.26
• Purity: ≥95%
• Synonyms: 3-(1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide
• InChI: InChI=1S/C14H11N3O/c15-13(18)10-3-1-2-9(6-10)12-7-11-4-5-16-14(11)17-8-12/h1-8H,(H2,15,18)(H,16,17)
• InChIKey: PQAJMNITAQGSCS-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)C(=O)N)C2=CN=C3C(=C2)C=CN3

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].
CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 µM; 12 h) decreases the expression of p-STAT1 S727 and p-STAT5 S726 i a dose-dependent manner in HCT-116 cells[1].
CDK8-IN-13 (0, 1, 5, 10 µM; 48 h) induces apoptosis in a dose-dependent manner[1].
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]

Reference

[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.
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