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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- CAS No.: 2403760-70-1
- Formule: C28H28D5N7O2
- Masse moléculaire:504.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
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. Further protocols information, click here.
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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.
Application
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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CAS No. 2403760-70-1
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Masse moléculaire 504.64
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Formule 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; AZD-9291-d5; Mereletinib-d5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dosimertinib Related Classifications
HY-142283 Related Classifications
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