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EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor, with an IC50 value of 18.94 nM. It induces apoptosis and causes G1 phase arrest. Additionally, EGFR-IN-175 downregulates the expression of p-EGFR, p-AKT, and p-ERK. It is applicable in cancer research, including studies on lung cancer.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor, with an IC50 value of 18.94 nM. It induces apoptosis and causes G1 phase arrest. Additionally, EGFR-IN-175 downregulates the expression of p-EGFR, p-AKT, and p-ERK. It is applicable in cancer research, including studies on lung cancer. |
| Targets&IC50 | EGFR WT:125.9 nM |
| In vitro | EGFR-IN-175 (Compound M49) inhibits the proliferation of BaF3-EGFR L858R/T790M/C797S, A431, and H1975 cells with IC50 values of 0.77, 5.11, and 5.94 μM, respectively. In a dose-dependent manner, EGFR-IN-175 (0.1-2.5 μM) reduces the phosphorylation levels of p-EGFR, p-AKT, and p-ERK in BaF3-TM cells. Additionally, EGFR-IN-175 (0.1-2.5 μM, 48 h) induces apoptosis and G1 phase arrest in BaF3-TM cells. |
| In vivo | EGFR-IN-175 (Compound M49) [administered via intraperitoneal injection at 30 mg/kg or orally at 30-60 mg/kg, once daily for 14 days] effectively inhibits tumor growth in BaF3-EGFR L858R/T790M/C797S xenografts in BALB/c nude mice. |
| 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.
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