JH-XVII-10
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3034312-17-6
- 分子式: C22H18F4N8O
- 分子量:486.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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DYRK1A 3 nM (IC50) |
DYRK1B 5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-22 | IC50 |
>100 μM
Compound: 16; JH-XVII-10
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAL27, FaDu, HEK293FT cells
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Concentration:10 µM
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Incubation Time:72 h
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Result:Decreased cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively.
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Cell Line:CAL27 cells
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Concentration:0.5, 1, 5, 10 µM
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Incubation Time:24 h
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Result:Showed inhibitory effects on pro-tumor signaling.
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Cell Line:CAL27 cells
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Concentration:1, 10 µM
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Incubation Time:24 h
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Result:Induced increases in the proapoptotic marker (cleaved PARP), and decreased the expression of antiapoptotic protein BCL-xL.
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 male mice[1]
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Dosage:
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Administration:2 mg/kg, i.v.; 10 mg/kg, p.o.
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Result:Showed oral bioavailability (F=12%).
化学情報
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CAS 番号 3034312-17-6
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分子量 486.42
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分子式 C22H18F4N8O
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SMILES
FC(F)(F)C1=NN2C=C1C3=C(F)NC4=NC=C(C=C43)C5=C(C#N)N(C)N=C5CN(C)C(CCC2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
JH-XVII-10 関連分類
HY-144614 関連分類
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