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

EGFR-IN-12 

Cat. No.: HY-17499 Purity: 99.49%
Handling Instructions

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.

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

EGFR-IN-12 Chemical Structure

EGFR-IN-12 Chemical Structure

CAS No. : 879127-07-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
25 mg USD 600 In-stock
Estimated Time of Arrival: December 31
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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].

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.

879127-07-8

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (604.74 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.2419 mL 1.2095 mL 2.4190 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

EGFR-IN-12EGFRApoptosisEpidermal growth factor receptorErbB-1HER1Tyrosinekinases4,6-disubstitutedpyrimidineautophosphorylationanti-proliferationantitumorAKTInhibitorinhibitorinhibit

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