CHMFL-EGFR-202
Based on 1 Customer Validation
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) 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。
- 純度 : 99.75%
- CAS 番号: 2089381-40-6
- 分子式: C25H24ClN7O2
- 分子量:489.96
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
- 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
製品説明
IC50 & Target
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EGFRT790M 5.3 nM (IC50) |
EGFR 8.3 nM (IC50) |
ErbB2 8.1 nM (IC50) |
ErbB4 3.2 nM (IC50) |
MEK1 161 nM (IC50) |
Btk 24.5 nM (IC50) |
BLK 8.1 nM (IC50) |
BMX 111 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
>10 μM
Compound: 19; CHMFL-EGFR-202
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Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
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[PMID: 28282122] |
| BaF3 | GI50 |
<0.3 nM
Compound: 8; CHMFL-EGFR-202
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Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay
Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay
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[PMID: 36324498] |
| BaF3 | GI50 |
>10 μM
Compound: 19; CHMFL-EGFR-202
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Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 28282122] |
| CHO | GI50 |
>10 μM
Compound: 19; CHMFL-EGFR-202
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Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
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[PMID: 28282122] |
体外実験
CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M[1].
CHMFL-EGFR-202 displays strong binding affinities against wild-type, G719C/S, L858R, L858R/T790M, L861Q, and T790M among EGFR wild-type and mutant kinases[1].
CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM)[1].
CHMFL-EGFR-202 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively[1].
CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50 of 111.0 nM and 161.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2089381-40-6
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性状 Solid
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分子量 489.96
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分子式 C25H24ClN7O2
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Color White to off-white
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SMILES
O=C(N(C1)CCC[C@H]1N2C3=NC=NC(N)=C3C(C4=CC(Cl)=C(OCC5=NC=CC=C5)C=C4)=N2)C=C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : ≥ 110 mg/mL (224.51 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
体内:
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: ≥ 2.75 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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 (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light, stored under nitrogen). 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 | 2.0410 mL | 10.2049 mL | 20.4098 mL | 51.0246 mL |
| 5 mM | 0.4082 mL | 2.0410 mL | 4.0820 mL | 10.2049 mL | |
| 10 mM | 0.2041 mL | 1.0205 mL | 2.0410 mL | 5.1025 mL | |
| 15 mM | 0.1361 mL | 0.6803 mL | 1.3607 mL | 3.4016 mL | |
| 20 mM | 0.1020 mL | 0.5102 mL | 1.0205 mL | 2.5512 mL | |
| 25 mM | 0.0816 mL | 0.4082 mL | 0.8164 mL | 2.0410 mL | |
| 30 mM | 0.0680 mL | 0.3402 mL | 0.6803 mL | 1.7008 mL | |
| 40 mM | 0.0510 mL | 0.2551 mL | 0.5102 mL | 1.2756 mL | |
| 50 mM | 0.0408 mL | 0.2041 mL | 0.4082 mL | 1.0205 mL | |
| 60 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8504 mL | |
| 80 mM | 0.0255 mL | 0.1276 mL | 0.2551 mL | 0.6378 mL | |
| 100 mM | 0.0204 mL | 0.1020 mL | 0.2041 mL | 0.5102 mL |
CHMFL-EGFR-202 関連分類
HY-101522 関連分類
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