Cat. No.: HY-18213

EGFR-IN-9

Customer Review

Based on 1 Customer Validation

EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC₅₀s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.

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

Purity: 98.84%
CAS No.: 1226549-39-8
Formula: C₂₉H₂₄N₄O₃
Molecular Weight:476.53

Storage:

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

EGFR-IN-9 Chemical Structure

CAS No.: 1226549-39-8

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Top Publications Citing

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
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR (WT)

7 nM (IC₅₀)

EGFR^L858R/T790M

28 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	CC₅₀	>1 μM Compound: 12	Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay	[PMID: 36749735]
HCC827	CC₅₀	24 nM Compound: 2	Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
HCC827	IC₅₀	8 nM Compound: 8	Antiproliferative activity against human HCC827 cells after 96 hrs by MTS assay Antiproliferative activity against human HCC827 cells after 96 hrs by MTS assay	[PMID: 20550212]
NCI-H1975	CC₅₀	>1 μM Compound: 12	Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay	[PMID: 36749735]
NCI-H1975	CC₅₀	1258 nM Compound: 2	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]

In Vitro

EGFR-IN-9 (Compound 8) shows antiproliferative activity in HCC827 lung cancer cell line with an IC₅₀ of 8 nM.

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

Chemical Information

CAS No. 1226549-39-8
Appearance Solid
Molecular Weight 476.53
Formula C₂₉H₂₄N₄O₃
Color Off-white to light yellow
SMILES

C=CC(NC1=CC=CC(C2=C(C3=CC=CC=C3)OC4=NC=NC(N[C@@H](C5=CC=CC=C5)CO)=C42)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (209.85 mM; Need ultrasonic; 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

2.0985 mL

10.4925 mL

20.9850 mL

5 mM

0.4197 mL

2.0985 mL

4.1970 mL

10 mM

0.2099 mL

1.0493 mL

2.0985 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)
- 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)

References

[1]. Coumar MS, et al. Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor leadidentification. J Med Chem. 2010 Jul 8;53(13):4980-8. [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	2.0985 mL	10.4925 mL	20.9850 mL	52.4626 mL
	5 mM	0.4197 mL	2.0985 mL	4.1970 mL	10.4925 mL
	10 mM	0.2099 mL	1.0493 mL	2.0985 mL	5.2463 mL
	15 mM	0.1399 mL	0.6995 mL	1.3990 mL	3.4975 mL
	20 mM	0.1049 mL	0.5246 mL	1.0493 mL	2.6231 mL
	25 mM	0.0839 mL	0.4197 mL	0.8394 mL	2.0985 mL
	30 mM	0.0700 mL	0.3498 mL	0.6995 mL	1.7488 mL
	40 mM	0.0525 mL	0.2623 mL	0.5246 mL	1.3116 mL
	50 mM	0.0420 mL	0.2099 mL	0.4197 mL	1.0493 mL
	60 mM	0.0350 mL	0.1749 mL	0.3498 mL	0.8744 mL
	80 mM	0.0262 mL	0.1312 mL	0.2623 mL	0.6558 mL
	100 mM	0.0210 mL	0.1049 mL	0.2099 mL	0.5246 mL

Keywords

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EGFR-IN-9

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening 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

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-9

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening 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

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-9 Related Classifications

Cat. No.: HY-18213