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Cat. No.: HY-147860

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EGFR-IN-61

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.

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CAS No.: 2890261-81-9
Formule: C₃₃H₃₇ClN₈O₃
Masse moléculaire:629.15

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

Data Sheet (273 KB)

EGFR-IN-61 Chemical Structure

CAS No.: 2890261-81-9

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Antibody-Drug Conjugates

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target

EGFR^L858R/T790M

42 ± 2 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

137 ± 6 nM (IC₅₀)

EGFR (WT)

743 ± 20 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

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]
A549	IC₅₀	2.14 μM Compound: 150	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]
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]
NCI-H1975	IC₅₀	1.82 μM Compound: 150	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]

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.

Chemical Information

CAS No. 2890261-81-9
Masse moléculaire 629.15
Formule C₃₃H₃₇ClN₈O₃
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 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)
Instruction de manipulation (2659 KB)

Références

[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]

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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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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EGFR-IN-61

Voir tous les produits spécifiques à Isoform EGFR