NRC-2694
Based on 1 Customer Validation
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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: 99.84%
- CAS 番号: 936446-61-6
- 分子式: C24H26N4O3
- 分子量:418.49
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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EGFR アイソフォーム固有の製品をすべて表示
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生物活性
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EGFR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
<0.1 μM
Compound: 49
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Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 32739648] |
| PC-9 | IC50 |
0.1 μM
Compound: 49
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Antiproliferative activity against human PC-9 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Antiproliferative activity against human PC-9 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
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[PMID: 32739648] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 936446-61-6
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性状 Solid
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分子量 418.49
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分子式 C24H26N4O3
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Color White to off-white
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SMILES
COC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCCN4CCOCC4
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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 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 250 mg/mL (597.39 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
The in vitro invasiveness of H1299 and A549 cells in the presence of various concentrations of NRC compounds (as determined by MTT assay) is assessed using a modified Boyden chamber assay. Cells are treated with these compounds for 48 hr. 1×106 cells are suspended in 600 μL of serum-free medium supplemented with 0.2% BSA and placed in the upper compartment of the transwell chambers coated with matrigel (0.7 mg/mL). The lower compartment of the chamber is filled with 200 μL of serum medium and the cells are allowed to migrate for 24 h. after incubation, the cells are fixed and stained with Hema-3 and quantified. The migrated cells are quantified as percent invasion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Nude mice are implanted with 2×106 A549 cells in the right hind limb flank. Upon the observance of a tumour (>2 mm), mice are given oral or ip treatments of the test compounds including erlotinib HCl used as positive control. A dose of 100 mg/kg of erlotinib HCl is identified as the base line dose.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (276 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3895 mL | 11.9477 mL | 23.8954 mL | 59.7386 mL |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7791 mL | 11.9477 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3895 mL | 5.9739 mL | |
| 15 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL | 3.9826 mL | |
| 20 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9869 mL | |
| 25 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3895 mL | |
| 30 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4935 mL | |
| 50 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL | |
| 60 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9956 mL | |
| 80 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5974 mL |
NRC-2694 関連分類
HY-19909 関連分類
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