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EGFR-IN-1 hydrochloride
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Catalog No. T11157LCas No. 2227455-78-7
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
EGFR-IN-1 hydrochloride
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Purity: 99.16%
Catalog No. T11157LCas No. 2227455-78-7
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $59 | In Stock | In Stock | |
| 5 mg | $153 | In Stock | In Stock | |
| 10 mg | $227 | In Stock | In Stock | |
| 25 mg | $355 | In Stock | In Stock | |
| 50 mg | $476 | In Stock | In Stock | |
| 100 mg | $653 | In Stock | In Stock | |
| 200 mg | $883 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $212 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.16%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively. |
| Targets&IC50 | p-EGFR:4-9nM |
| In vitro | EGFR-IN-1 is highly selective against a panel of 100 kinases and inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively[1]. |
| In vivo | In female athymic nude mice with H1975 Tumor Xenograft, gavage administration of EGFR-IN-1 hydrochloride (30 mg/kg) significantly inhibits the tumor growth without observed loss in body weight. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR and a systemic exposure (AUC0-inf.) of 0.33 μM. h[1]. |
| Molecular Weight | 551.04 |
| Formula | C28H31ClN6O4 |
| Cas No. | 2227455-78-7 |
| Smiles | Cl.O=C(C=C)NC1=CC=CC(=C1)N2C(=O)C=C(C=3C=NC(=NC32)NC4=CC=C(OCCN(C)C)C=C4OC)C |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (18.15 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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