Dosimertinib
Dosimertinib is a potent and orally active EGFR inhibitor. Dosimertinib decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib shows antiproliferative and anti-tumor activity. Dosimertinib has the potential for the research of non-small-cell lung cancer (NSCLC).
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- No. CAS: 2403760-70-1
- Fòrmula: C28H28D5N7O2
- Peso molecular:504.64
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Almacenamiento:
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
243.9 nM
Compound: 2h
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Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
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[PMID: 33459024] |
| BaF3 | IC50 |
18 nM
Compound: 2h
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
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[PMID: 33459024] |
| BaF3 | IC50 |
3.5 nM
Compound: 2h
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Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
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[PMID: 33459024] |
| NCI-H1975 | IC50 |
28.4 nM
Compound: 2h
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Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
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[PMID: 33459024] |
In Vitro
Dosimertinib (compound 2h) (1, 10, 100, 100 nM; 2h) decreases the expression of p-EGFR and p-ERK protein levels 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:A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 Cells
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed antiproliferative activity with IC50s of 243.9, 28.4, 18.0, 3.5 nM for A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 cells, respectively.
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Cell Line:A431, H1975 cells
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Concentration:1, 10, 100, 100 nM
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Incubation Time:2 h
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Result:Decreased the expression of p-EGFR and p-ERK protein levels in a dose-dependent mannet when co-incubationed with 50 ng/mL EGF.
In Vivo
Pharmacokinetic Parameters of Dosimertinib in Sprague-Dawley rats[1].
| detected compound | dosimertinib | |||
| administration route | i.v. | i.g. | i.g. | i.g. |
| dose (mg/kg) | 2 | 2 | 6 | 12 |
| C0 or Cmax (nM) | 277 ± 105 | 46.7 ± 10.7 | 113 ± 19.8 | 283 ± 137 |
| Tmax (h) | 4.17 ± 2.56 | 4.67 ± 1.63 | 5.00 ± 1.67 | |
| t1/2 (h) | 5.40 ± 1.84 | 3.76 ± 1.08 | 3.27 ± 0.43 | 4.04 ± 1.50 |
| AUC0-t (nM·h) | 1070 ± 565 | 459 ± 191 | 1020 ± 313 | 2830 ± 1780 |
| CL/F (L/h/kg) | 22.3 ± 11.1 | 32.2 ± 13.6 | 19.5 ± 5.1 | 14.9 ± 6.4 |
| bioavailability (%) | 41.2 | 29.6 | 43.0 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:18-20 g, BALB/c nude mice (H1975 mouse xenograft model)[1]
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Dosage:0.75, 1.5, 3 mg/kg
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Administration:Oral gavage; daily for 24 days
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Result:Significantly reduced tumor size with tumor growth inhibition (TGI) of 72.94% and 97.62% at 1.5, 3 mg/kg, respectively.
Aplicación
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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No. CAS 2403760-70-1
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Peso molecular 504.64
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Fòrmula C28H28D5N7O2
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SMILES
[2H]/C([2H])=C\C(NC1=CC(NC2=NC=CC(C3=CN(C4=C3C=CC=C4)C([2H])([2H])[2H])=N2)=C(C=C1N(CCN(C)C)C)OC)=O
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Synonyms
Osimertinib-d5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dosimertinib Related Classifications
HY-142283 Related Classifications
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