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 .
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- CAS. Nr.: 2568086-81-5
- Formel: C32H41BrN9O2P
- Molecular Weight:694.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
0.09 , 0.06 nM (EGFRL858R/T790M/C797S, EGFRDel19/T790M/C797S)
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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] |
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.
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. Nr. 2568086-81-5
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Molecular Weight 694.60
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EGFR-IN-82 Related Classifications
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