2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Dosimertinib-d5 mesylate

Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

For research use only. We do not sell to patients.

Dosimertinib-d<sub>5</sub> mesylate Chemical Structure

Dosimertinib-d5 mesylate Chemical Structure

CAS No. : 2403760-72-3

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5 mg USD 960 In-stock
10 mg USD 1480 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Dosimertinib-d5 mesylate:

Dosimertinib-d5 mesylate Related Antibodies

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Description

Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

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.

Dosimertinib-d5 mesylate Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 Cells
Concentration: 0-10 µM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: A431, H1975 cells
Concentration: 1, 10, 100, 100 nM
Incubation Time: 2 h
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

Dosimertinib mesylate (0.75, 1.5, 3 mg/kg; oral gavage, daily for 24 days) shows anti-tumor activity in mouse[1].
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
Sprague-Dawley rats, 2 mg/kg iv; 2, 6, 12 mg/kg for i.g..

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 18-20 g, BALB/c nude mice (H1975 mouse xenograft model)[1]
Dosage: 0.75, 1.5, 3 mg/kg
Administration: Oral gavage; daily for 24 days
Result: Significantly reduced tumor size with tumor growth inhibition (TGI) of 72.94% and 97.62% at 1.5, 3 mg/kg, respectively.
Molecular Weight

600.74

Formula

C29H32D5N7O5S
CAS No.
Appearance

Solid

Color

White to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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Dosimertinib-d5 mesylate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dosimertinib-d52403760-72-3EGFREpidermal growth factor receptorErbB-1HER1p-EGFRp-ERKNSCLCorally activeantiproliferativeanti-tumorInhibitorinhibitorinhibit

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