EGFR kinase inhibitor 1

Cat. No.: HY-143246: Data Sheet Handling Instructions
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EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC₅₀s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.

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EGFR kinase inhibitor 1 화학구조

CAS No. : 2413958-04-8

사이즈		재고
MOQ		Minimum order quantity
50 mg		견적 받기
100 mg		견적 받기
250 mg		견적 받기
Other size		견적 받기

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

EGFR (WT)

37 nM (IC₅₀)

EGFR^L858R/T790M

1.7 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

>300 nM (IC₅₀)

In Vitro

EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC₅₀s of 4.17, 0.052 µM for A549, H1975 cells, respectively^[1].
EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner^[1].
EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase^[1].
EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	A549, H1975 cells
Concentration:
Incubation Time:	72 h
Result:	Showed antiproliferation activity with IC₅₀s of 4.17, 0.052 µM for A549, H1975 cells, respectively.

Apoptosis Analysis [1]

Cell Line:	H1975 cells
Concentration:	0.05, 0.5, 5 µM
Incubation Time:	48 h
Result:	Induced apoptosis in a dose-dependent manner.

Apoptosis Analysis [1]

Cell Line:	H1975 cells
Concentration:	4, 20, 100 nM
Incubation Time:	48 h
Result:	Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM.

분자량

521.61

화학식

C₃₀H₃₁N₇O₂

CAS No.

2413958-04-8

SMILES

C=CC(NC1=C(C=C(C(NC2=NC(C3=CN(C4=C3C=CC=C4)C)=CC=N2)=C1)OC)N5C=CC=C5CN(C)C)=O

선적

Room temperature in continental US; may vary elsewhere.

보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Ding S, et al. Design, synthesis and biological evaluation of novel N-(3-amino-4-methoxyphenyl)acrylamide derivatives as selective EGFRL858R/T790M kinase inhibitors. Bioorg Chem. 2022 Jan;118:105471. [Content Brief]