EGFR-IN-49

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EGFR-IN-49 is a potent and selective EGFR inhibitor with IC₅₀s of 65.0 nM and 13.6 nM for EGFR^T790M and EGFR^T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner.

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

EGFR-IN-49 Chemical Structure

CAS No. : 2459932-81-9

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR^T790M

65.0 nM (IC₅₀)

EGFR^L858R/T790M

13.6 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	3.79 μM Compound: 13a	Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	4.34 μM Compound: 13a	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
HeLa	IC₅₀	6.39 μM Compound: 13a	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	> 50 μM Compound: 13a	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
MCF7	IC₅₀	18.99 μM Compound: 13a	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H1975	IC₅₀	699.2 nM Compound: 13a	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 32679450]

In Vitro

EGFR-IN-49 (compound 13a) (1, 10 µM) shows inhibition activity for H1975 cells with an IC₅₀ of 699.2 nM^[1].
EGFR-IN-49 (1 µM) shows an strong inhibitory activity to EGFR^T790M, EGFR^T790M/L858R, EGFR^WT with IC₅₀s of 65.0, 13.6, >1000 nM, respectively^[1].
EGFR-IN-49 (0.2, 4, 8 µM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	A549, A431, Hela, MCF7, LO2 cells
Concentration:	0-50 µM
Incubation Time:
Result:	Showed excellent anti-proliferative activities with IC₅₀s of 4.34, 3.79, 6.39, 18.99, >50 µM for A549, A431, Hela, MCF7, LO2 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:	A431 cells
Concentration:	0.2, 4, 8 µM
Incubation Time:	48 h
Result:	Induced cell apoptosis in a low concentration (0.33 µM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 µM.

Molecular Weight

413.45

Formula

C₂₂H₁₅N₅O₂S

CAS No.

2459932-81-9

SMILES

C=CC(NC1=CC(OC2=NC(NC3=CC=CC(C#N)=C3)=NC4=C2SC=C4)=CC=C1)=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]. Xiao Z, et al. Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. Eur J Med Chem. 2020 Oct 1;203:112511. [Content Brief]

EGFR-IN-49 Related Classifications

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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:

EGFR-IN-492459932-81-9EGFREpidermal growth factor receptorErbB-1HER1SelectiveapoptosisA431 cellsEGFR^T790MEGFR^T790M/L858Rdose-dependent manneranti-proliferationlow cytotoxicInhibitorinhibitorinhibit

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