| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H28FN7O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
EGFR T790M/L858R-IN-2 is a potent, selective inhibitor of EGFR T790M/L858R, with IC50 values of 3.5 nM against the mutant and 1290 nM against EGFR WT. It decreases expression of p-EGFR, p-AKT, and p-ERK1/2, induces apoptosis, and arrests the cell cycle in G1 phase, giving it anti-cancer activity[1]. It is supplied as a light yellow to yellow solid (C28H28FN7O, MW 497.57) at 99.66% purity.
Physical & Chemical Properties
| CAS Number | 2955607-40-4 |
|---|---|
| Molecular Formula | C28H28FN7O |
| Molecular Weight | 497.57 g/mol |
| Purity | 99.66% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | C=CC(NC1=CC=CC(NC2=C3C=C(F)C=CC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O |
| Target | EGFR L858R/T790M, EGFR (WT), EGFR T790M, EGFR L858R |
| Signaling Pathway | JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (200.98 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
EGFRL858R/T790M 3.5 nM (IC50) |
EGFR (WT) 1290 nM (IC50) |
EGFRT790M 6.7 nM (IC50) |
EGFRL858R 2.1 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (200.98 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In H1975 and HCC827 cells, EGFRT790M/L858R-IN-2 (0.1, 1, 10 μM; 4 h) lowers expression of p-EGFR, P-AKT, and P-ERK1/2 in a dose-dependent manner[1]. In H1975 and HCC827 cells, EGFRT790M/L858R-IN-2 (0.1, 1, 10 μM; 48 h) induces apoptosis and G1 phase cell cycle arrest[1]. EGFRT790M/L858R-IN-2 (0.1, 1, 10 μM; 14 days) dose-dependently inhibits colony formation and cell migration[1].
Western Blot Analysis[1]
| Cell Line | H1975, HCC827, A549, A431cells |
|---|---|
| Concentration | 0.1, 1, 10 μM |
| Incubation Time | 4 h |
| Result | Decreased the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells, showed a weak inhibitory effect on EGF-induced EGFR and AKT and ERK1/2 phosphorylation in A549 and A431 cells. |
Apoptosis Analysis[1]
| Cell Line | H1975, HCC827, A549, A431cells |
|---|---|
| Concentration | 0.1, 1, 10 μM |
| Incubation Time | 48 h |
| Result | Significantly induced apoptosis of H1975 and HCC827 cells in a dose-dependent manner, exhibited weaker apoptosis-inducing ability than osimertinib in A549 and A431 cells, inducing only 14.80 and 17.93% apoptosis, respectively, at 10 μM. |
Cell Cycle Analysis[1]
| Cell Line | H1975, HCC827, A549, A431cells |
|---|---|
| Concentration | 0.1, 1, 10 μM |
| Incubation Time | 48 h |
| Result | Induced cell cycle arrest in the G1 phase with the G0/G1 phase ratios approximately 80.5% for H1975 and approximately 81.1% for HCC827，approximately 63.8% for A549 and approximately 64.5% for A431 cells. |
In Vivo
EGFR T790M/L858R-IN-2 (5, 10, 20 mg/kg; i.p.; daily) dose-dependently inhibits tumor growth[1].
Pharmacokinetic Parameters of EGFR T790M/L858R-IN-2 in Male Sprague-Dawley rats[1]
| parameter | i.v. (1 mg/kg) |
| T1/2 (h) | 1.76 ± 0.65 |
| Cmax (ng/mL) | 649.90 ± 54.71 |
| AUC0-t (h*ng/ml) | 1036.86 ± 137.03 |
| AUC0–∞ (h ng/ml) | 1048.74 ± 134.39 |
| Vz (mL/kg) | 2515.40 ± 1184.92 |
| CL(mL/min/kg) | 16.07 ± 2.06 |
Dosing in male Sprague-Dawley rats: 1 mg/kg, iv[1]
| Animal Model | 6-8 weeks, BALB/c female nude mice(H1975 cell xenografts)[1] |
|---|---|
| Dosage | 5, 10, 20 mg/kg |
| Administration | I.p.; once per day |
| Result | Inhibited tumor growth, both in volume and weight in a dose-dependent manner. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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