Art. -Nr.: HY-143337

EGFR-IN-47

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EGFR-IN-47 is a potent and orally active EGFR^{L858R/T790M/C797S} inhibitor with an IC₅₀ of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.

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Reinheit: 96.01%
CAS. Nr.: 3034649-73-2
Formel: C₂₉H₃₅N₇
Molecular Weight:481.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

EGFR-IN-47 Chemical Structure

CAS. Nr.: 3034649-73-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR^{L858R/T790M/C797S}

0.07 μM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	2.972 μM Compound: 14aj	Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
A549	IC₅₀	1.031 μM Compound: 14aj	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
PC-9	IC₅₀	0.013 μM Compound: 14aj	Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
PC-9	IC₅₀	0.013 μM Compound: 36	Antiproliferative activity against human PC-9 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as cell growth inhibition Antiproliferative activity against human PC-9 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as cell growth inhibition	[PMID: 36417820]

In Vitro

EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC₅₀s of 0.013 μM, 2.972 μM, 1.031 μM for PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells, respectively^[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM; 24 h) induces cell cycle attest at the G0/G1-phase^[1].
EGFR-IN-47 (0.01, 0.05, 0.25 μM) induces cell deathvia apoptosis in a concentration-dependent manner^[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM) inhibits phosphorylation of the EGFR downstream mediators^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells
Concentration:
Incubation Time:

72 h
Result:

Showed anti-proliferative effects with IC₅₀s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:

0.01, 0.05, 0.25, 1 µM
Incubation Time:

24 h
Result:

Cells were arrest at the G0/G1-phase.

Apoptosis Analysis^[1]

Cell Line:

PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:

0.01, 0.05, 0.25 µM
Incubation Time:

24 h
Result:

Induced cell deathvia apoptosis in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:

PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:

0.01, 0.05, 0.25, 1 µM
Incubation Time:
Result:

Inhibited phosphorylation of the EGFR downstream mediators.

In Vivo

EGFR-IN-47 (10, 20, 40 mg/kg; i.g.) shows anti-tumor effect with low toxicity^[1].
EGFR-IN-47 (20 mg/kg for i.v.; 20 mg/kg for p.o.) shows an ideal oral bioavailability of 66.05%^[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats^[1].

parameter	iv (20 mg/kg)	po (20 mg/kg)
AUC_0-∞ (mg/Lh)	15.889	10.494
C_max (mg/L)	6.845	0.77
T_max (h)	0.083	6
F (%)		66.05
MRT_0-∞ (h)	16.439	16.791
V_ss (L/kg)	16.015	28.101
CL (L/h/kg)	1.272	2.151
t_(1/2) (h)	8.922	11.154

Male Sprague-Dawley rats; 20 mg/kg for i.v.; 20 mg/kg for p.o.^[1]

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

Animal Model:

6-8 weeks, BALB/c nude mice (PC-9 EGFR^{L858R/T790M/C797S} cells )^[1]
Dosage:

10, 20, 40 mg/kg (dissolved in 25% (v/v) PEG400 plus 5% DMSO)
Administration:

I.g.
Result:

Showed anti-tumor effect with low toxicity.

Animal Model:

Male Sprague-Dawley rats^[1]
Dosage:

20 mg/kg
Administration:

I.v.; p.o.
Result:

Showed an ideal oral bioavailability of 66.05%.

Chemical Information

CAS. Nr. 3034649-73-2
Appearance Solid
Molecular Weight 481.64
Formel C₂₉H₃₅N₇
Color Light yellow to yellow
SMILES

CN(CC1)CCN1C2=CC=C(C=C2)NC3=NC=C4C=C(N(C4=N3)C5CCCC5)CNC6=CC=CC=C6
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (41.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0762 mL

10.3812 mL

20.7624 mL

5 mM

0.4152 mL

2.0762 mL

4.1525 mL

10 mM

0.2076 mL

1.0381 mL

2.0762 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Wang C, et al. Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. Eur J Med Chem. 2022; 237:114381. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0762 mL	10.3812 mL	20.7624 mL	51.9060 mL
	5 mM	0.4152 mL	2.0762 mL	4.1525 mL	10.3812 mL
	10 mM	0.2076 mL	1.0381 mL	2.0762 mL	5.1906 mL
	15 mM	0.1384 mL	0.6921 mL	1.3842 mL	3.4604 mL
	20 mM	0.1038 mL	0.5191 mL	1.0381 mL	2.5953 mL
	25 mM	0.0830 mL	0.4152 mL	0.8305 mL	2.0762 mL
	30 mM	0.0692 mL	0.3460 mL	0.6921 mL	1.7302 mL
	40 mM	0.0519 mL	0.2595 mL	0.5191 mL	1.2976 mL

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EGFR-IN-47

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-47

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-47 Related Classifications

HY-143337 Related Classifications