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Cat. No.: HY-142283

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Dosimertinib

Name: Dosimertinib
Brand: MedChemExpress
SKU: HY-142283
Availability: PreOrder

(Synonyms: Osimertinib-d₅)

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).

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

CAS No.: 2403760-70-1
Formula: C₂₈H₂₈D₅N₇O₂
Molecular Weight:504.64

Storage:

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

Data Sheet (292 KB)

Dosimertinib Chemical Structure

CAS No.: 2403760-70-1

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Application
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	243.9 nM Compound: 2h	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	[PMID: 33459024]
BaF3	IC₅₀	18 nM Compound: 2h	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	[PMID: 33459024]
BaF3	IC₅₀	3.5 nM Compound: 2h	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	[PMID: 33459024]
NCI-H1975	IC₅₀	28.4 nM Compound: 2h	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	[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.

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.

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

CAS No. 2403760-70-1
Molecular Weight 504.64
Formula C₂₈H₂₈D₅N₇O₂
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
Synonyms

Osimertinib-d₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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