EGFR-IN-11
Based on 1 Customer Validation
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.76%
- CAS No.: 2463200-44-2
- Formule: C29H35N9O2S
- Masse moléculaire:573.71
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform EGFR
More
Activité biologique
|
EGFRL858R/T790M/C797S 18 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
>10 μM
Compound: D9
|
Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
|
[PMID: 31787359] |
| A549 | IC50 |
2.91 μM
Compound: D9
|
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
|
[PMID: 31787359] |
| HCC827 | IC50 |
0.00088 μM
Compound: D9
|
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
|
[PMID: 31787359] |
| HCC827 | IC50 |
0.88 nM
Compound: D9
|
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
|
[PMID: 31787359] |
| NCI-H1975 | IC50 |
0.2 μM
Compound: D9
|
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
|
[PMID: 31787359] |
EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 µM, respectively[1].
EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1].
EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.[1]
EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human lung cancer cell lines HCC827 (EGFRDel E746-A750), H1975 (EGFRL858R/T790M) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT)
-
Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 µM
-
Incubation Time:72 hours
-
Result:Inhibited HCC827 H1975 A549 cells proliferation with IC50s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively.
-
Cell Line:HCC827, H1975 and A549 cells
-
Concentration:1.00, 0.10 and 0.01 µM for HCC827 cells; 10.00, 1.00 and 0.10 µM for H1975 and A549 cells
-
Incubation Time:8 hours
-
Result:Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines.
-
Cell Line:HCC827 cells
-
Concentration:1 µM
-
Incubation Time:24 hours
-
Result:The percentages of apoptotic cells is 56.91%.
-
Cell Line:HCC827 cells
-
Concentration:1 µM
-
Incubation Time:24 hours
-
Result:The number of HCC827 cells in G0/G1 phase was increased significantly.
Chemical Information
-
CAS No. 2463200-44-2
-
Appearance Solid
-
Masse moléculaire 573.71
-
Formule C29H35N9O2S
-
Color White to yellow
-
SMILES
CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C=N3)N=C(NC5=CC=CC=C5)N4[C@H]6CN(CC6)S(C7CC7)(=O)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (217.88 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (3.63 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Pureté et documentation
-
Fiche technique (277 KB)
-
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)
-
Instruction de manipulation (2659 KB)
Références
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 | 1.7430 mL | 8.7152 mL | 17.4304 mL | 43.5760 mL |
| 5 mM | 0.3486 mL | 1.7430 mL | 3.4861 mL | 8.7152 mL | |
| 10 mM | 0.1743 mL | 0.8715 mL | 1.7430 mL | 4.3576 mL | |
| 15 mM | 0.1162 mL | 0.5810 mL | 1.1620 mL | 2.9051 mL | |
| 20 mM | 0.0872 mL | 0.4358 mL | 0.8715 mL | 2.1788 mL | |
| 25 mM | 0.0697 mL | 0.3486 mL | 0.6972 mL | 1.7430 mL | |
| 30 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4525 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0894 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.8715 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2905 mL | 0.7263 mL | |
| 80 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.4358 mL |
EGFR-IN-11 Related Classifications
HY-130616 Related Classifications
Powered by Bioz