Cat. No.: HY-17499

EGFR-IN-12

Customer Review

Based on 1 Customer Validation

EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC₅₀of 21 nM. EGFR-IN-12 also inhibits mutant EGFR^L858R and EGFR^L861Q with IC₅₀s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC₅₀ = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.

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

Purity: 99.60%
CAS No.: 879127-07-8
Formula: C₂₁H₁₈F₃N₅O
Molecular Weight:413.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

EGFR-IN-12 Chemical Structure

CAS No.: 879127-07-8

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

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
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR (WT)

21 nM (IC₅₀)

EGFR^L858R

63 nM (IC₅₀)

EGFR^L861Q

4 nM (IC₅₀)

HER4

7640 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	84.1 nM Compound: 3	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]
B16-F10	IC₅₀	60.7 nM Compound: 3	Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]
HeLa	IC₅₀	83.4 nM Compound: 3	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]
HepG2	IC₅₀	28.5 nM Compound: 3	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]
MDA-MB-231	IC₅₀	45.3 nM Compound: 3	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]
SK-OV-3	IC₅₀	63.2 nM Compound: 3	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36621138]

In Vitro

EGFR-IN-12 (EGFR inhibitor 324674; 0-2 μM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations^[2].
EGFR-IN-12 (EGFR inhibitor 324674; 0-3 μM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner^[2].
EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 μM and 1.04 μM, respectively^[2].
Pretreatment of cells with EGFR-IN-12 (compound 1; 10 μM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12^[1].

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

Apoptosis Analysis^[1]

Cell Line:

HT29 and SW480 cells
Concentration:

0 µM, 1 µM, 2 µM
Incubation Time:

48 hours
Result:

Induced apoptosis in HT29 cells and SW480 cells.

Western Blot Analysis^[1]

Cell Line:

HT29 and SW480 cells
Concentration:

0 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM
Incubation Time:

3 hours
Result:

Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.

Chemical Information

CAS No. 879127-07-8
Appearance Solid
Molecular Weight 413.40
Formula C₂₁H₁₈F₃N₅O
Color Off-white to light yellow
SMILES

O=C(C1CC1)NC2=CC=CC(NC3=NC=NC(NC4=CC=CC(C(F)(F)F)=C4)=C3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (604.74 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

2.4190 mL

12.0948 mL

24.1896 mL

5 mM

0.4838 mL

2.4190 mL

4.8379 mL

10 mM

0.2419 mL

1.2095 mL

2.4190 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Qiong Zhang, et al. Discovery of EGFR Selective 4,6-disubstituted Pyrimidines From a Combinatorial Kinase-Directed Heterocycle Library. J Am Chem Soc. 2006 Feb 22;128(7):2182-3. [Content Brief]

[2]. Zhiwei Yu, et al. Novel Irreversible EGFR Tyrosine Kinase Inhibitor 324674 Sensitizes Human Colon Carcinoma HT29 and SW480 Cells to Apoptosis by Blocking the EGFR Pathway. Biochem Biophys Res Commun. 2011 Aug 12;411(4):751-6. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4190 mL	12.0948 mL	24.1896 mL	60.4741 mL
	5 mM	0.4838 mL	2.4190 mL	4.8379 mL	12.0948 mL
	10 mM	0.2419 mL	1.2095 mL	2.4190 mL	6.0474 mL
	15 mM	0.1613 mL	0.8063 mL	1.6126 mL	4.0316 mL
	20 mM	0.1209 mL	0.6047 mL	1.2095 mL	3.0237 mL
	25 mM	0.0968 mL	0.4838 mL	0.9676 mL	2.4190 mL
	30 mM	0.0806 mL	0.4032 mL	0.8063 mL	2.0158 mL
	40 mM	0.0605 mL	0.3024 mL	0.6047 mL	1.5119 mL
	50 mM	0.0484 mL	0.2419 mL	0.4838 mL	1.2095 mL
	60 mM	0.0403 mL	0.2016 mL	0.4032 mL	1.0079 mL
	80 mM	0.0302 mL	0.1512 mL	0.3024 mL	0.7559 mL
	100 mM	0.0242 mL	0.1209 mL	0.2419 mL	0.6047 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

EGFR-IN-12

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

Human Metabolite 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

Multi-Target 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

Mass Spectrometry Human Metabolite 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-12 Related Classifications

HY-17499 Related Classifications