1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. EGFR-IN-12

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 EGFRL858R and EGFRL861Q 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.

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EGFR-IN-12 Chemical Structure

EGFR-IN-12 Chemical Structure

CAS No. : 879127-07-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 217 In-stock
Solution
10 mM * 1 mL in DMSO USD 217 In-stock
Solid
1 mg USD 94 In-stock
5 mg USD 198 In-stock
10 mg USD 330 In-stock
25 mg USD 660 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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 EGFRL858R and EGFRL861Q 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[1][2].

IC50 & Target[1]

EGFR (WT)

21 nM (IC50)

EGFRL858R

63 nM (IC50)

EGFRL861Q

4 nM (IC50)

HER4

7640 nM (IC50)

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.
Molecular Weight

413.40

Formula

C21H18F3N5O

CAS No.
Unlabeled CAS

Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4190 mL 12.0948 mL 24.1896 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
EGFR-IN-12
Cat. No.:
HY-17499
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