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Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. )

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. ) |
| Targets&IC50 | EGFR (L858R/T790M):12 nM, EGFR (C797S):13 nM |
| In vitro | Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 μM, 2.7 μM, 0.36 μM and 0.20 μM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 cells[1].Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 μM, 3.3 μM, 3.8 μM, 4.0 μM and 4.5 μM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells[1]. |
| Molecular Weight | 508.59 |
| Formula | C31H29FN4O2 |
| Cas No. | 2375107-27-8 |
| Smiles | O=C1C2=CC(OC3=CC=C(C=C3)N4CCN(C)CC4)=CC=C2NC5=CC=C(F)C=C5N1CC=6C=CC=CC6 |
| Relative Density. | 1.259 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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.
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.
| Size | Quantity | Unit Price | Amount | Operation |
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