Cat. No.: HY-130616

EGFR-IN-11

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Based on 1 Customer Validation

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

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

Purity: 98.76%
CAS No.: 2463200-44-2
Formula: C₂₉H₃₅N₉O₂S
Molecular Weight:573.71

Storage:

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

EGFR-IN-11 Chemical Structure

CAS No.: 2463200-44-2

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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
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR^{L858R/T790M/C797S}

18 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	>10 μM Compound: D9	Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
A549	IC₅₀	2.91 μM Compound: D9	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
HCC827	IC₅₀	0.00088 μM Compound: D9	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
HCC827	IC₅₀	0.88 nM Compound: D9	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
NCI-H1975	IC₅₀	0.2 μM Compound: D9	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]

In Vitro

EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC₅₀s of 0.88 nM and 0.20 µM, respectively^[1].
EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line^[1].
EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.^[1]
EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Human lung cancer cell lines HCC827 (EGFR^{Del E746-A750}), H1975 (EGFR^L858R/T790M) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT)
Concentration:

0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 µM
Incubation Time:

72 hours
Result:

Inhibited HCC827 H1975 A549 cells proliferation with IC₅₀s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

HCC827, H1975 and A549 cells
Concentration:

1.00, 0.10 and 0.01 µM for HCC827 cells; 10.00, 1.00 and 0.10 µM for H1975 and A549 cells
Incubation Time:

8 hours
Result:

Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines.

Apoptosis Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

1 µM
Incubation Time:

24 hours
Result:

The percentages of apoptotic cells is 56.91%.

Cell Cycle Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

1 µM
Incubation Time:

24 hours
Result:

The number of HCC827 cells in G0/G1 phase was increased significantly.

Chemical Information

CAS No. 2463200-44-2
Appearance Solid
Molecular Weight 573.71
Formula C₂₉H₃₅N₉O₂S
Color White to yellow
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C=N3)N=C(NC5=CC=CC=C5)N4[C@H]6CN(CC6)S(C7CC7)(=O)=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 : 125 mg/mL (217.88 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

1.7430 mL

8.7152 mL

17.4304 mL

5 mM

0.3486 mL

1.7430 mL

3.4861 mL

10 mM

0.1743 mL

0.8715 mL

1.7430 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: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)
- 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)

References

[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888. [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	1.7430 mL	8.7152 mL	17.4304 mL	43.5760 mL
	5 mM	0.3486 mL	1.7430 mL	3.4861 mL	8.7152 mL
	10 mM	0.1743 mL	0.8715 mL	1.7430 mL	4.3576 mL
	15 mM	0.1162 mL	0.5810 mL	1.1620 mL	2.9051 mL
	20 mM	0.0872 mL	0.4358 mL	0.8715 mL	2.1788 mL
	25 mM	0.0697 mL	0.3486 mL	0.6972 mL	1.7430 mL
	30 mM	0.0581 mL	0.2905 mL	0.5810 mL	1.4525 mL
	40 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0894 mL
	50 mM	0.0349 mL	0.1743 mL	0.3486 mL	0.8715 mL
	60 mM	0.0291 mL	0.1453 mL	0.2905 mL	0.7263 mL
	80 mM	0.0218 mL	0.1089 mL	0.2179 mL	0.5447 mL
	100 mM	0.0174 mL	0.0872 mL	0.1743 mL	0.4358 mL

Keywords

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EGFR-IN-11

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

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators 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

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-11 Related Classifications

HY-130616 Related Classifications