EGFR-IN-82
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
For research use only. We do not sell to patients.
- CAS No.: 2568086-81-5
- Formula: C32H41BrN9O2P
- Molecular Weight:694.60
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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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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
0.09 , 0.06 nM (EGFRL858R/T790M/C797S, EGFRDel19/T790M/C797S)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
13 nM
Compound: 8h
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Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
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[PMID: 35810715] |
In Vitro
EGFR-IN-82 (compound 8a) (72 h) significantly inhibits the growth of Ba/F3-EGFRDel19/T790M/C797S cells with the IC50 value of 12.7 nM, but has no significant effect on the growth of A431 cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
EGFR-IN-82 (15 -30 mg/kg；Oral gavage (p.o.)；14 -21 days) exhibits moderate inhibition on PC9-EGFR Del19/T790M/C797S xenograft mice model, while presents a very strong tumor growth inhibition effect on tumor with high expression of EGFRDel19/T790M/C797S[1].
Pharmacokinetic Analysis in Male Balb/C mice Model[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | AUC0-t (ng/mL*h) | AUC0-∞(ng/mL*h) | t1/2 (h) | MRT (h) |
| p.0. | 5 | 1574 | 15375 | 15632 | 3.5 | 6 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC9-EGFRDel19/T790M/C797S xenograft mice model
Ba/F3-EGFR Del19/T790M/C797S xenograft mice model [1] -
Dosage:15 or 30 mg/kg/day, 14-21 days
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Administration:Oral gavage (p.o.)
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Result:Exhibited moderate inhibition on tumor growth, with a tumor growth inhibition rate (TGI) of 21.60% at 15 mg/kg and 46.79% at 30 mg/kg in PC9-EGFR Del19/T790M/C797S xenograft mice model. Presented a very strong tumor growth inhibition effect with the TGI of 48.43% at low dose(15 mg/kg) and 82.60% at high dose(30 mg/kg) in xenograft mice model of Ba/F3-EGFR Del19/T790M/C797S.
Chemical Information
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CAS No. 2568086-81-5
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Molecular Weight 694.60
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Formula C32H41BrN9O2P
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SMILES
COC1=C(NC2=NC=C(Br)C(NC3=C(P(C)(C)=O)C(N=CC=N4)=C4C=C3)=N2)C=C(C)C(N5CCC(N6CC(N(C)C)C6)CC5)=C1
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-82 Related Classifications
HY-149401 Related Classifications
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