Dosimertinib mesylate
Based on 1 Customer Validation
Dosimertinib mesylate is a potent and orally active EGFR inhibitor. Dosimertinib mesylate decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib mesylate shows antiproliferative and anti-tumor activity. Dosimertinib mesylate has the potential for the research of non-small-cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Purity : 99.50%
- CAS No.: 2403760-72-3
- Formula: C29H32D5N7O5S
- Molecular Weight:600.74
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Dosimertinib mesylate (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 mesylate 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. 2403760-72-3
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Unlabeled CAS 1421373-65-0
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Appearance Solid
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Molecular Weight 600.74
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Formula C29H32D5N7O5S
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Color White to yellow
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SMILES
CS(=O)(O)=O.[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 mesylate; AZD-9291-d5 mesylate; Mereletinib-d5 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (166.46 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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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.
Purity & Documentation
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Data Sheet (299 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6646 mL | 8.3231 mL | 16.6461 mL | 41.6153 mL |
| 5 mM | 0.3329 mL | 1.6646 mL | 3.3292 mL | 8.3231 mL | |
| 10 mM | 0.1665 mL | 0.8323 mL | 1.6646 mL | 4.1615 mL | |
| 15 mM | 0.1110 mL | 0.5549 mL | 1.1097 mL | 2.7744 mL | |
| 20 mM | 0.0832 mL | 0.4162 mL | 0.8323 mL | 2.0808 mL | |
| 25 mM | 0.0666 mL | 0.3329 mL | 0.6658 mL | 1.6646 mL | |
| 30 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 40 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 50 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 60 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6936 mL | |
| 80 mM | 0.0208 mL | 0.1040 mL | 0.2081 mL | 0.5202 mL | |
| 100 mM | 0.0166 mL | 0.0832 mL | 0.1665 mL | 0.4162 mL |
Dosimertinib mesylate Related Classifications
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