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Cat. No.: HY-189291

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EGFR-IN-218

EGFR-IN-218 is an orally effective EGFR inhibitor with IC₅₀ values of 3.85, 0.40, and 140.5 nM against EGFR^WT, EGFR^L858R/T790M, and EGFR^{L858R/T790M/C797S}, respectively. EGFR-IN-218 inhibits EGFR phosphorylation and downstream ERK1/2 signaling, and exhibits in vivo antitumor activity. EGFR-IN-218 can be used for research on EGFR-mutant non-small cell lung cancer, glioblastoma, and brain metastasis.

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

CAS No.: 2410789-80-7
Formula: C₃₄H₃₉FN₈O₂
Molecular Weight:610.72

Storage:

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

EGFR-IN-218 Chemical Structure

CAS No.: 2410789-80-7

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

EGFR^WT

3.85 nM (IC₅₀)

EGFR^L858R/T790M

0.4 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

140.5 nM (IC₅₀)

All EGFR Isoforms :

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC50	2.53 μM	Antiproliferative activity against human A431 cells harboring EGFRWT assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human A431 cells harboring EGFRWT assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42561559
H1975	IC50	0.61 μM	Antiproliferative activity against human H1975 cells expressing EGFRL858R/T790M assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human H1975 cells expressing EGFRL858R/T790M assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42561559
U-87MG ATCC	IC50	8.44 μM	Antiproliferative activity against human U87 MG cells harboring EGFRWT assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human U87 MG cells harboring EGFRWT assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42561559
BaF3	IC50	2.25 μM	Antiproliferative activity against Ba/F3-EGFRL858R/T790M/C797S cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against Ba/F3-EGFRL858R/T790M/C797S cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.	42561559

In Vitro

OthersAnti-cancerCell Cycle Regulation

Others

EGFR-IN-218 (compound 8m) (0.45-1000 nM) inhibits EGFRWT, EGFRL858R/T790M, and EGFRL858R/T790M/C797S kinase activity with IC50 values of 3.85, 0.40, and 140.5 nM, respectively^[1].
EGFR-IN-218 (1 μM) shows inhibition rates of 102.23%, 99.97%, 97.29%, 90.84%, and 73.53% against HER2, EGFR, HER4, FRK, and BRK, respectively, in a 76-tyrosine kinase panel screen^[1].
EGFR-IN-218 (1-100 nM; 48 h) dose-dependently decreases EGFR and ERK1/2 phosphorylation in H1975 and PC-9 cells; at 10 nM, it inhibits p-EGFR and p-ERK1/2 more potently than Osimertinib^[1].

Anti-cancer

EGFR-IN-218 (0.03-100 μM; 72 h) reduces the viability of A431, H1975, U87 MG, and U87-EGFRvIII cells with IC₅₀ values of 2.53, 0.61, 8.44, and 10.35 μM, respectively^[1].
EGFR-IN-218 (72 h) reduces Ba/F3-EGFRL858R/T790M/C797S cell viability with an IC₅₀ of 2.25 μM, superior to Osimertinib (HY-15772) at 12.03 μM^[1].

Cell Cycle Regulation

EGFR-IN-218 (48 h) increases the G0/G1 phase proportion in H1975 cells from 66.46% to 84.18% and 85.19%, respectively, and decreases the S phase proportion from 27.06% to 6.24% and 6.56%, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

H1975, PC-9
Concentration:

1, 10, 100 nM
Incubation Time:

48 h
Result:

Dose-dependently decreased EGFR phosphorylation.
Decreased phospho-ERK1/2 levels.
At 10 nM, suppressed EGFR phosphorylation more strongly than Osimertinib.
At 10 nM, suppressed ERK1/2 phosphorylation more strongly than Osimertinib.

Parmacokinetics

Species	Dose	Route	F	C_max	T_max	MRT_0-t	MRT_0-∞	T_1/2	AUC_0-t	AUC_0-∞	V_z	CL
Rat^[1]	4 mg/kg	i.v.	/	481.36 μg/L	0.46 h	9.90 h	12.29 h	10.23 h	4790.42 μg/L·h	5058.05 μg/L·h	40511.82 L/kg	2313.12 L/h/kg
Rat^[1]	20 mg/kg	p.o.	31.5 %	1317.18 μg/L	2.90 h	6.75 h	6.82 h	7.94 h	7971.30 μg/L·h	7977.94 μg/L·h	6865.66 L/kg	643.00 L/h/kg

In Vivo

Anti-cancerOthers

Anti-cancer

EGFR-IN-218 (compound 8m) (5, 10 mg/kg; p.o.; once daily; 14 days) inhibits tumor growth in H1975 subcutaneous xenograft BALB/c nude mice, with TGI of 94.18% and 96.10%, respectively, comparable to 94.84% for 5 mg/kg Osimertinib^[1].
EGFR-IN-218 (30 mg/kg/day; 15 days) inhibits intracranial tumor growth in intracranial H1975-Luc brain metastasis BALB/c nude mice; supplementary bioluminescence imaging on day 7 and day 15 both shows suppressed tumor burden; and it prolongs the survival of H1975-Luc brain metastasis model mice^[1].

Others

EGFR-IN-218 (5, 10 mg/kg; p.o.; once daily; 14 days) reduces EGFR phosphorylation in H1975 subcutaneous xenograft tumor tissues, with a greater degree of inhibition than 5 mg/kg Osimertinib^[1].

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

Animal Model:

BALB/c nude mice (female, 5-7 weeks old)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Inhibited tumor growth with TGI rates of 94.18% at 5 mg/kg and 96.10% at 10 mg/kg.
Suppressed EGFR phosphorylation relative to vehicle controls.

Related Protocols :

Chemical Information

CAS No. 2410789-80-7
Molecular Weight 610.72
Formula C₃₄H₃₉FN₈O₂
SMILES

FC(C=C1)=CC=C1C2=NC=CN2C3=CC(NC4=C(OC)C=C(N5CCC(N6CCN(C)CC6)CC5)C(NC(C=C)=O)=C4)=NC=C3
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]. Zhang T, et al. Novel 2-amino-4-(1H-imidazol)pyridine derivatives as potent brain-penetrant EGFR mutant inhibitors: Design, synthesis, biological evaluation, and molecular modeling study. Bioorg Chem. 2026;181:110311.

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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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EGFR-IN-218

All EGFR Isoforms

All ERK Isoforms