EGFR/C797S-IN-1
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner.
For research use only. We do not sell to patients.
- CAS No.: 2378188-21-5
- Formula: C28H30N4O3
- Molecular Weight:470.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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EGFRL858R/T790M/C797S 0.128 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.09 μM
Compound: 14d
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Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay
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[PMID: 36279692] |
| BaF3 | IC50 |
0.75 μM
Compound: 14d
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay
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[PMID: 36279692] |
EGFR/C797S-IN-1 (compound 14d) (0-10 µM; 72 h) shows anti-proliferative activities with IC50s of 0.75, 0.09 µM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively[1].
EGFR/C797S-IN-1 (1-10000 nM; 24 h) decreases the expression of p-EGFR, p-AKT, p-ERK protein 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:BaF3 cells with EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S Mutations
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed anti-proliferative activitie with IC50s of 0.75, 0.09 µM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively.
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Cell Line:BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S cells
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Concentration:1, 10, 100, 1000, 10000 nM
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Incubation Time:24 h
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Result:Decreased the expression of p-EGFR, p-AKT. p-ERK protein in a dose dependent manner.
Pharmacokinetic Parameters of EGFR/C797S-IN-1 in Male Sprague-Dawley rats[1].
| Parameter | i.v. (1 mg/kg) | p.o. (10 mg/kg) |
| Tmax (h) | 0.08±0 | 3.33±1.15 |
| T1/2 (h) | 1.97±0.14 | 3.89±0.42 |
| Cmax (ng/mL) | 69.57±6.78 | 7.43±1.17 |
| AUC0-t (h*ng/mL) | 65.48±5.55 | 61.12±6.23 |
| AUC0-∞ (h*ng/mL) | 67.98±5.56 | 62.15±6.36 |
| CL-obs (L/h/kg) | 14.78±1.19 | -- |
| Vss-obs (L/kg) | 26.11±2.58 | -- |
| F (%) | -- | 9.33±0.95 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD male rats[1]
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Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o.
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Administration:i.v. or p.o.
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Result:Displayed good biochemical activity and promising cellular activity.
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Animal Model:BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)[1]
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Dosage:10, 30 mg/kg
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Administration:I.p.; daily for 14 days
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Result:Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.
Chemical Information
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CAS No. 2378188-21-5
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Molecular Weight 470.56
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Formula C28H30N4O3
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SMILES
COC1=C(C=C2N=CN=C(C2=C1)NC3=CC=C(C=C3)OC4=CC=CC=C4)OCC5CCN(CC5)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/C797S-IN-1 Related Classifications
HY-152019 Related Classifications
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