EGFR ligand-2

Cat. No.: HY-150905: FAQs
Data Sheet Handling Instructions

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EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC₅₀s of 21 nM and 48 nM for EGFR^L858R and EGFR^L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC.

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

EGFR ligand-2 Chemical Structure

CAS No. : 2737283-20-2

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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^L858R

21 nM (IC₅₀)

EGFR^L858R/T790M

48 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	7090 nM Compound: C4	Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
HCC827	IC₅₀	0.33 nM Compound: C4	Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
NCI-H1975	IC₅₀	12 nM Compound: C4	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]

Molecular Weight

537.66

Formula

C₃₀H₃₅N₉O

CAS No.

2737283-20-2

SMILES

C=CC(N1CCC[C@@H](C1)N2C(NC3=CC=CC=C3)=NC4=CN=C(N=C42)NC5=CC=C(C=C5)N6CCN(CC6)C)=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]. Hong-Yi Zhao, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022 Mar 24;65(6):4709-4726. [Content Brief]

EGFR ligand-2 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 ligand-22737283-20-2EGFR ligand2EGFR ligand 2EGFREpidermal growth factor receptorErbB-1HER1EGFR ligandEGFR mutantPROTACInhibitorinhibitorinhibit

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