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CAS No. : 2375554-02-0
MCE 国际站:Senexin C
产品活性:Senexin C 是一种选择性和具有口服活性的 CDK8/19 抑制剂。Senexin C 显示出强烈的肿瘤富集药代动力学 (PK) 谱和肿瘤药效学 (PD) 标志物反应。Senexin C 抑制 MV4-11 白血病细胞的生长具有良好的耐受性。
研究领域:Cell Cycle/DNA Damage
作用靶点:CDK
In Vitro: Senexin C (compound 20a) exhibits potent CDK8/19 inhibitory activity with high selectivity (IC50s of 56 and 108 nM for 293-NFκB-Luc and MV4-11-Luc cells, respectively).
Senexin C (2 µM) shows potency in different kinase assays (IC50= 3.6 nM for CD8/CycC, Kd=1.4 nM for CD8/CycC, Kd=2.9 nM for CDK19/CycC).
Senexin C (1 µM, 3 h) shows inhibition on CDK8/19 dependent cellular gene expression.
In Vivo: Senexin C (2.5 mg/kg, i.v.; 100 mg/kg, p.o.) shows good oral bioavailability.
Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability.Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice.
parameters |
iv (2.5 mg/kg) |
po (100 mg/kg) |
plasma |
tumor |
plasma |
tumor |
C0 (μg/mL) |
503 |
Kel (h-1) |
0.93 |
0.06 |
0.2 |
0.1 |
T1/2 (h) |
0.75 |
12.1 |
3.53 |
7.27 |
Tmax (h) |
0.58 |
12 |
12 |
Cmax (ng/mL or ng/g) |
488 |
144 |
5728 |
AUC0-24 h (ng x h/ml or ng x h/g) |
331 |
6408 |
2182 |
88,600 |
F% |
16.5% |
34.6% |
Eight-week-old female Balb/c mice ( CT26 tumor mode), 2.5 mg/kg, i.v.(2.5 mg/mL Senexin C solution in 5% dextrose); 100 mg/kg, p.o.(10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle).
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