JH-XVII-10

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JH-XVII-10 

JH-XVII-10 是一种有效的，具有选择性和口服活性的 DYRK1A 和 DYRK1B 抑制剂，IC50值分别为 3 nM 和 5 nM。JH-XVII-10 在颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

JH-XVII-10

JH-XVII-10 Chemical Structure

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生物活性

JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines[1].

IC50 & Target[1]

DYRK1A

3 nM (IC50)

DYRK1B

5 nM (IC50)

体外研究
(In Vitro)

JH-XVII-10 (compound 10) (1 µM; CAL27 cells) shows active against JNK1 (IC50=1130 nM), JNK2 (IC50=1100 nM), JNK3 (IC50=>10 000 nM), FAK (IC50=90 nM), RSK1 (IC50=82 nM), RSK2 (IC50=80 nM), RSK3 (IC50=61 nM)[1].
JH-XVII-10 (10 µM; 72 h) decreases cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively[1].
JH-XVII-10 (1, 10 µM; 24 h) induces apoptosis in CAL27 cells[1].
JH-XVII-10 (0.5, 1, 5, 10 µM; 24 h) shows inhibitory effects on pro-tumor signaling in CAL27 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: CAL27, FaDu, HEK293FT cells
Concentration: 10 µM
Incubation Time: 72 h
Result: Decreased cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively.

Western Blot Analysis[1]

Cell Line: CAL27 cells
Concentration: 0.5, 1, 5, 10 µM
Incubation Time: 24 h
Result: Showed inhibitory effects on pro-tumor signaling.

Apoptosis Analysis[1]

Cell Line: CAL27 cells
Concentration: 1, 10 µM
Incubation Time: 24 h
Result: Induced increases in the proapoptotic marker (cleaved PARP), and decreased the expression of antiapoptotic protein BCL-xL.

体内研究
(In Vivo)

JH-XVII-10 (2 mg/kg, i.v.; 10 mg/kg, p.o.) shows oral bioavailability (F=12%)[1]. Pharmacokinetic Parameters of JH-XVII-10 in C57Bl/6 male mice[1].

administration parameters rat dog
i.v. T1/2 (h) 1.4±0.3 5.70±1.2
AUC0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4
CL (mL/min/kg) 17.6±2.0 149.9±62.5
Vss (L/kg) 1.7±0.2 828.7±134.2
p.o. Cmax (ng/mL) 1661.1±916.6 3979.4±483.5
Tmax(h) 0.9±0.8 1.3±0.5
T1/2 (h) 1.4±0.2 4.9±0.6
AUC0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2
F (%) 54.2 31.8

C57Bl/6 male mice; 2 mg/kg, i.v.; 10 mg/kg, p.o.[1]

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6 male mice[1]
Dosage:
Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o.
Result: Showed oral bioavailability (F=12%).

分子量

472.40

Formula

C21H16F4N8O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022; 13(4):577-585.

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