Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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ln Vitro |
In a dose-dependent manner, dosimertinib mesylate (compound 2h)(1, 10, 100, 100 nM; 2h) lowers the levels of p-EGFR and p-ERK protein [1].
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ln Vivo |
Mice treated orally with dosimertinib mesylate (0.75, 1.5, or 3 mg/kg; once daily for 24 days) exhibit antitumor activity [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 Cells Tested Concentrations: 0-10 µM Incubation Duration: 72 h Experimental Results: demonstrated 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. Western Blot Analysis[1] Cell Types: A431, H1975 cells Tested Concentrations: 1, 10, 100, 100 nM Incubation Duration: 2 h Experimental Results: diminished the expression of p-EGFR and p-ERK protein levels in a dose-dependent mannet when co-incubated with 50 ng/mL EGF. |
Animal Protocol |
Animal/Disease Models: 18-20 g, BALB/c nude mice (H1975 mouse xenograft model)[1]
Doses: 0.75, 1.5, 3 mg/kg Route of Administration: po (oral gavage); daily for 24 days Experimental Results: Dramatically decreased tumor size with tumor growth Inhibition (TGI) of 72.94% and 97.62% at 1.5, 3 mg/kg, respectively. |
References |
[1]. Meng Y, et al. Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2021 Jan 28;64(2):925-937.
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Molecular Formula |
C29H32D5N7O5S
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Molecular Weight |
600.74
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Related CAS # |
Dosimertinib-d3;2403760-70-1
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6646 mL | 8.3231 mL | 16.6461 mL | |
5 mM | 0.3329 mL | 1.6646 mL | 3.3292 mL | |
10 mM | 0.1665 mL | 0.8323 mL | 1.6646 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.