CDK8-IN-13是一种强效、选择性且口服有效的CDK8抑制剂，IC50值为51.9nM。
Cas No.:918523-75-8
Sample solution is provided at 25 µL, 10mM.
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CDK8-IN-13 is a potent, selective, and orally active CDK8 inhibitor with an IC50 value of 51.9nM[1]. CDK8-IN-13 has been widely used as a lead compound to analyze the binding mode with the active site of CDK8 in molecular docking experiments, and to develop a series of CDK8 inhibitors[2].
In vitro, CDK8-IN-13 treatment (10µM) for 12 hours significantly inhibited the phosphorylation of STAT1 at S727 and STAT5 at S726 in HCT-116 cells[1].
In vivo, CDK8-IN-13 treatment via oral administration at a dose of 80mg/kg/day for 15 days significantly inhibited tumor growth in the C1498 xenograft mouse model, without causing significant weight loss[1].
References:
[1] Zhang X X, Yan Y Y, Ma X, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia[J]. European Journal of Medicinal Chemistry, 2023, 251: 115214.
[2] Chen Z, Wang Q, Yan Y Y, et al. Discovery of novel and potent CDK8 inhibitors for the treatment of acute myeloid leukaemia[J]. Journal of Enzyme Inhibition and Medicinal Chemistry, 2024, 39(1): 2305852.
CDK8-IN-13是一种强效、选择性且口服有效的CDK8抑制剂，IC50值为51.9nM[1]。CDK8-IN-13已被广泛用作先导化合物，用于在分子对接实验中分析与CDK8活性位点的结合模式，并用于开发一系列CDK8抑制剂[3]。
在体外，使用10μM的CDK8-IN-13处理HCT-116细胞12小时，显著抑制了STAT1在S727位点和STAT5在S726位点的磷酸化[1]。
在体内，每日口服80mg/kg剂量的CDK8-IN-13，连续15天，显著抑制了C1498异种移植小鼠模型中的肿瘤生长，且未引起显著的体重减轻[1]。
| Cell experiment [1]: | |
Cell lines | HL-60 cells |
Preparation Method | HL-60 cells were cultured in RPMI 1640 medium containing 10% fetal bovine serum (FBS), 50U/ml penicillin, and 100mg/ml streptomycin at 37℃ in the presence of 5% CO2. HL-60 cells were seeded into 60 mm cultural dishes at a density of 2×106 cells per dish. After incubating for 24h, cells were treated with different concentrations of CDK8-IN-13 (0, 1, 5, and 10µM) for 48h. Subsequently, flow cytometry was used to analyze cell apoptosis. |
Reaction Conditions | 1, 2, 5, 7.5, 10µM; 48h |
Applications | CDK8-IN-13 treatment induced cell apoptosis in HL-60 cells in a dose-dependent manner. |
| Animal experiment [1]: | |
Animal models | Balb/C mice |
Preparation Method | Thirty 6-week-old Balb/C mice were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility. Mice were injected with 5×106 C1498 cells into the flanks. After the mean tumor volumes reached about 60mm3, the mice were randomly divided into 2 groups (N=10 per group). 0.9% saline solution (vehicle) and CDK8-IN-13 (80mg/kg/day) were administrated orally for 15 days. The tumor volume and body weight were recorded every 2 days. After 3 weeks, the mice were sacrificed, and the tumors were taken out for analysis. |
Dosage form | 80mg/kg/day for 15 days; p.o. |
Applications | CDK8-IN-13 treatment resulted in significant cessation of tumor growth and no significant weight loss in Balb/C mice with C1498 xenograft. |
References: | |
| Cas No. | 918523-75-8 | SDF | |
| 分子式 | C14H11N3O | 分子量 | 237.26 |
| 溶解度 | DMSO : 125 mg/mL (526.85 mM; Need ultrasonic) | 储存条件 | -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2148 mL | 21.0739 mL | 42.1479 mL |
| 5 mM | 843 μL | 4.2148 mL | 8.4296 mL |
| 10 mM | 421.5 μL | 2.1074 mL | 4.2148 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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