EGFR T790M/L858R-IN-2
Based on 1 Customer Validation
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 2955607-40-4
- Formula: C28H28FN7O
- Molecular Weight:497.57
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL858R/T790M 3.5 nM (IC50) |
EGFR (WT) 1290 nM (IC50) |
EGFRT790M 6.7 nM (IC50) |
EGFRL858R 2.1 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
2.486 μM
Compound: 28f
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Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 37042119] |
| A549 | IC50 |
4.02 μM
Compound: 28f
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Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 37042119] |
| HCC827 | IC50 |
0.008 μM
Compound: 28f
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Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 37042119] |
| NCI-H1975 | IC50 |
0.019 μM
Compound: 28f
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 37042119] |
In Vitro
EGFRT790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h) decreases the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells[1].
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 48 h) induces apoptosis and cell cycle arrest in the G1 phase in H1975, HCC827 cells[1].
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 14 days) inhibits colony formation and cell migration in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975, HCC827, A549, A431cells
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Concentration:0.1, 1, 10 µM
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Incubation Time:4 h
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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.
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Cell Line:H1975, HCC827, A549, A431cells
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Concentration:0.1, 1, 10 µM
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Incubation Time:48 h
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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.
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Cell Line:H1975, HCC827, A549, A431cells
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Concentration:0.1, 1, 10 µM
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Incubation Time:48 h
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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
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks, BALB/c female nude mice(H1975 cell xenografts)[1]
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Dosage:5, 10, 20 mg/kg
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Administration:I.p.; once per day
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Result:Inhibited tumor growth, both in volume and weight in a dose-dependent manner.
Chemical Information
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CAS No. 2955607-40-4
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Appearance Solid
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Molecular Weight 497.57
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Formula C28H28FN7O
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Color Light yellow to yellow
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SMILES
C=CC(NC1=CC=CC(NC2=C3C=C(F)C=CC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (200.98 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)
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
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 | 2.0098 mL | 10.0488 mL | 20.0977 mL | 50.2442 mL |
| 5 mM | 0.4020 mL | 2.0098 mL | 4.0195 mL | 10.0488 mL | |
| 10 mM | 0.2010 mL | 1.0049 mL | 2.0098 mL | 5.0244 mL | |
| 15 mM | 0.1340 mL | 0.6699 mL | 1.3398 mL | 3.3496 mL | |
| 20 mM | 0.1005 mL | 0.5024 mL | 1.0049 mL | 2.5122 mL | |
| 25 mM | 0.0804 mL | 0.4020 mL | 0.8039 mL | 2.0098 mL | |
| 30 mM | 0.0670 mL | 0.3350 mL | 0.6699 mL | 1.6748 mL | |
| 40 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2561 mL | |
| 50 mM | 0.0402 mL | 0.2010 mL | 0.4020 mL | 1.0049 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3350 mL | 0.8374 mL | |
| 80 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6281 mL | |
| 100 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5024 mL |
EGFR T790M/L858R-IN-2 Related Classifications
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