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Cat. No.: HY-146136

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EGFR-IN-56

EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC₅₀ values of 541.7 nM and 132.1 nM against EGFR^T790M and EGFR^T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis.

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

CAS No.: 2477726-83-1
Formula: C₂₃H₂₂N₄O₃S
Molecular Weight:434.51

Storage:

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

Data Sheet (267 KB)

EGFR-IN-56 Chemical Structure

CAS No.: 2477726-83-1

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Use of MCE Products

Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

EGFR^L858R/T790M

132.1 nM (IC₅₀)

EGFR^T790M

541.7 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4.22 μM Compound: 13a	Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
HeLa	IC₅₀	20.91 μM Compound: 13a	Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
L02	IC₅₀	>50 μM Compound: 13a	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
MCF7	IC₅₀	0.66 μM Compound: 64	Anticancer activity against human MCF7 cells incubated for 48 hrs by MTT assay Anticancer activity against human MCF7 cells incubated for 48 hrs by MTT assay	[PMID: 33992931]
MCF7	IC₅₀	11.69 μM Compound: 13a	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
NCI-H1975	IC₅₀	2.19 μM Compound: 13a	Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]

Chemical Information

CAS No. 2477726-83-1
Molecular Weight 434.51
Formula C₂₃H₂₂N₄O₃S
SMILES

C=CC(NC1=CC=CC(OC2=C(CSCC3)C3=NC(NC4=CC=C(OC)C=C4)=N2)=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xiao Z, et al. Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. Bioorg Med Chem. 2020 Oct 1;28(19):115669. [Content Brief]

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.

Keywords

100 mg

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