JH-XVII-10

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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].

上海金畔生物科技有限公司 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]

上海金畔生物科技有限公司 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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