EGFR-IN-61

Cat. No.: HY-147860: FAQs
Data Sheet Handling Instructions

Molarity Calculator

EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC₅₀ values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC₅₀ values of 2.14 and 1.82 μM, respectively.

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

EGFR-IN-61 Chemical Structure

CAS No. : 2890261-81-9

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EGFR^L858R/T790M

42 ± 2 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

137 ± 6 nM (IC₅₀)

EGFR (WT)

743 ± 20 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.14 μM Compound: 22a	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
NCI-H1975	IC₅₀	1.82 μM Compound: 22a	Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]

In Vitro

EGFR-IN-61 (compound 22a) shows excellent kinase selectivity against the L858R/T790M/C797S mutant EGFR kinase rather than the wild-type, which reached 5.4 times^[1].

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

Molecular Weight

629.15

Formula

C₃₃H₃₇ClN₈O₃

CAS No.

2890261-81-9

SMILES

COC1=CC(N(CCN(C)C)C)=C(C=C1NC2=NC(C3=CN(C4=C3C=CC=C4)CCCO)=CC=N2)NC(C5=CC(Cl)=NC=C5)=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]. Ding S, et al. Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors. Eur J Med Chem. 2022 Aug 5;238:114492. [Content Brief]

EGFR-IN-61 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-612890261-81-9EGFREpidermal growth factor receptorErbB-1HER1A549H1975osimertinib derivativesreversible EGFR kinase InhibitorsL858R/T790M/C797S mutationantitumor activityInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks