Dosimertinib-d₃

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Dosimertinib-d₃-d₃ is a potent and orally active EGFR inhibitor. Dosimertinib-d₃-d₃ decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d₃-d₃ shows antiproliferative and anti-tumor activity. Dosimertinib-d₃-d₃ 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>3</sub> Chemical Structure

Dosimertinib-d₃ Chemical Structure

CAS No. : 2403760-70-1

Size		Stock
1 mg		Get quote	Estimated Time of Arrival: December 31
5 mg		Get quote	Estimated Time of Arrival: December 31

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Other Forms of Dosimertinib-d₃:

Dosimertinib-d₅ mesylate In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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 (0.75, 1.5, 3 mg/kg; oral gavage, daily for 24 days) shows anti-tumor activity in mouse^[1].
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 C_max (nM)	277 ± 105	46.7 ± 10.7	113 ± 19.8	283 ± 137
T_max (h)		4.17 ± 2.56	4.67 ± 1.63	5.00 ± 1.67
t_1/2 (h)	5.40 ± 1.84	3.76 ± 1.08	3.27 ± 0.43	4.04 ± 1.50
AUC_0-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

Male 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

504.64

Formula

C₂₈H₂₈D₅N₇O₂

CAS No.

2403760-70-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Chen C, et al. Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury. Eur J Med Chem. 2022 Dec 16;247:115023. [Content Brief]