INCB3619
Based on 1 Customer Validation
INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 99.46%
- CAS 番号: 791826-72-7
- 分子式: C22H27N3O5
- 分子量:413.47
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1 μM
Compound: INCB3619
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Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
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[PMID: 26192023] |
| BT-474 | IC50 |
68 nM
Compound: 22, INCB-3619
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Inhibition of Her2 sheddase activity in BT474 cell line
Inhibition of Her2 sheddase activity in BT474 cell line
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[PMID: 17256836] |
INCB3619 (0-10 μM, 96 h) can inhibit heregulin-dependent HER3-Akt pathway, but not ERK activity in A549 cells, and induce apoptosis in A549 cells[1].
INCB3619 (0-10 μM, 72 h) can inhibit EGFR ligand signaling in the EGFR autocrine cell line NCI-H1666 and can be used in combination with other anti-EGFR drugs such as gefitinib[1].
INCB3619 (2 µM) inhibits ERK1/2 expression in NCI-H1666 and make it sensitive to Gefitinib (HY-50895)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cell
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Concentration:1, 10 μM
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Incubation Time:
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Result:Induced about 3% apoptosis at a concentration of 1 μM and about 5% at a concentration of 10 μM.
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Cell Line:NCI-H1666 cell
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Concentration:0-10 μM
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Incubation Time:72 h
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Result:Inhibited proliferation of NCI-H1666 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nu/nu mouse model of A549 xenograft
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Dosage:50, 60 mg/kg
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Administration:subcutaneous injection, daily, 14 d
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Result:Significant tumor growth inhibition and delay at 60 mg/kg dose, less active effect at 50 mg/kg.
化学情報
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CAS 番号 791826-72-7
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性状 Solid
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分子量 413.47
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分子式 C22H27N3O5
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Color White to off-white
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SMILES
O=C(N([C@H](C(N1CC=C(C2=CC=CC=C2)CC1)=O)[C@@H](C(NO)=O)C3)CC43CC4)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (241.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4186 mL | 12.0928 mL | 24.1856 mL | 60.4639 mL |
| 5 mM | 0.4837 mL | 2.4186 mL | 4.8371 mL | 12.0928 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4186 mL | 6.0464 mL | |
| 15 mM | 0.1612 mL | 0.8062 mL | 1.6124 mL | 4.0309 mL | |
| 20 mM | 0.1209 mL | 0.6046 mL | 1.2093 mL | 3.0232 mL | |
| 25 mM | 0.0967 mL | 0.4837 mL | 0.9674 mL | 2.4186 mL | |
| 30 mM | 0.0806 mL | 0.4031 mL | 0.8062 mL | 2.0155 mL | |
| 40 mM | 0.0605 mL | 0.3023 mL | 0.6046 mL | 1.5116 mL | |
| 50 mM | 0.0484 mL | 0.2419 mL | 0.4837 mL | 1.2093 mL | |
| 60 mM | 0.0403 mL | 0.2015 mL | 0.4031 mL | 1.0077 mL | |
| 80 mM | 0.0302 mL | 0.1512 mL | 0.3023 mL | 0.7558 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2419 mL | 0.6046 mL |