EGFR-IN-5
Based on 1 Customer Validation
EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
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: 99.49%
- CAS 番号: 2225887-26-1
- 分子式: C31H38FN9O
- 分子量:571.69
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
|
EGFR 10.4 nM (IC50) |
EGFRL858R 1.1 nM (IC50) |
EGFRL858R/T790M 34 nM (IC50) |
EGFRL858R/T790M/C797S 7.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.06 μM
Compound: B30
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Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
|
[PMID: 29466773] |
| HCC827 | IC50 |
0.044 μM
Compound: B30
|
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
|
[PMID: 29466773] |
| HCC827 | IC50 |
0.04 μM
Compound: 39
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Antiproliferative activity against human HCC827 assessed as cell growth inhibition
Antiproliferative activity against human HCC827 assessed as cell growth inhibition
|
[PMID: 33992931] |
| HCC827 | IC50 |
40 nM
Compound: 23
|
Growth inhibition of human HCC827 cells
Growth inhibition of human HCC827 cells
|
[PMID: 34323489] |
| NCI-H1975 | IC50 |
0.4 μM
Compound: B30
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
|
[PMID: 29466773] |
| NCI-H1975 | IC50 |
400 nM
Compound: 23
|
Growth inhibition of human NCI-H1975 cells
Growth inhibition of human NCI-H1975 cells
|
[PMID: 34323489] |
化学情報
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CAS 番号 2225887-26-1
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性状 Solid
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分子量 571.69
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分子式 C31H38FN9O
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Color Light yellow to yellow
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SMILES
OCC(CC1)CCN1C2=NC(NC3=CC=C(F)C=C3)=NC(C=N4)=C2C=C4NC5=NC=C(N6CCC(N(C)C)CC6)C=C5
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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 (174.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (3.64 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.
Please enter the basic information of animal experiments:
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-
-
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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.
純度とドキュメンテーション
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データシート (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 1.7492 mL | 8.7460 mL | 17.4920 mL | 43.7300 mL |
| 5 mM | 0.3498 mL | 1.7492 mL | 3.4984 mL | 8.7460 mL | |
| 10 mM | 0.1749 mL | 0.8746 mL | 1.7492 mL | 4.3730 mL | |
| 15 mM | 0.1166 mL | 0.5831 mL | 1.1661 mL | 2.9153 mL | |
| 20 mM | 0.0875 mL | 0.4373 mL | 0.8746 mL | 2.1865 mL | |
| 25 mM | 0.0700 mL | 0.3498 mL | 0.6997 mL | 1.7492 mL | |
| 30 mM | 0.0583 mL | 0.2915 mL | 0.5831 mL | 1.4577 mL | |
| 40 mM | 0.0437 mL | 0.2186 mL | 0.4373 mL | 1.0932 mL | |
| 50 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8746 mL | |
| 60 mM | 0.0292 mL | 0.1458 mL | 0.2915 mL | 0.7288 mL | |
| 80 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5466 mL | |
| 100 mM | 0.0175 mL | 0.0875 mL | 0.1749 mL | 0.4373 mL |