2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. GW2974

GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research.

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

GW2974 Chemical Structure

GW2974 Chemical Structure

CAS No. : 202272-68-2

Size Price Stock Quantity
5 mg USD 120 In-stock
10 mg USD 195 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

GW2974 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research[1][2].

IC50 & Target[2]

EGFRL858R/T790M

0.007 μM (IC50)

HER2

0.016 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
50.1 μM
Compound: 17; GW2974
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
[PMID: 31260312]
In Vitro

GW2974 (0.5-50 μM, 3 h) has an obvious cytotoxicity appeared at 10 μM or above and inhibits cell proliferation of U87MG and U251MG cells at 0.5-5 μM after 24 h treatment[1].
GW2974 (0.5-5 μM, 24 h) has a dose-related role in GBM cell invasion and migration[1].
GW2974 (0.001-100 μM, 24 h) inhibits BT474, HN5, N87 cells growth[2].

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

GW2974 Related Antibodies

Cell Viability Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-50 μM
Incubation Time: 3 h
Result: Reduced U87MG and U251MG cells viability to 89.4% and 86.3% in 0.5 μM and 5 μM compared with control.

Cell Proliferation Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Inhibited U87MG and U251MG cells proliferation in 0.5 μM and 5μM.

Cell Invasion Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Reduced the percentage to 55.6% and 48.6% of U87MG and U251MG cells in 0.5 μM, respectively.

Cell Migration Assay [1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Decreased the relative migration distances (percentage) of U87MG and U251MG cells to 40.2% and 51.6% in 0.5 μM, respectively.
Resulted in a relative migration distances of U87MG and U251MG cells in 5 μM compared with control.

Cell Proliferation Assay[2]

Cell Line: BT474, HN5, N87
Concentration: 0.001-100 μM
Incubation Time: 24 h
Result: Inhibited cell growth by 50% at concentrations > 1.0 μM with IC50s < 0.4 μM.
In Vivo

GW2974 (30 mg/kg, 100 mg/kg for Oral gavage, once a day) inhibits GBM growth, invasion, and angiogenesis in dose of 30 mg/kg but abrogated the inhibitory effect of low-dose GW2974 on tumor invasion in dose of 100 mg/kg in GBM xenograft mice model[1].
GW2974 (10 mg/kg, 30 mg/kg, Oral gavage, twice a day) inhibits the growth of tumor in CD-1 nude mice (HN5) and C.B-17 SCID mice (BT474) models in a dosed dependent manner[2].

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

Animal Model: GBM xenograft mice model[1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Oral gavage (p.o.)
Result: Decelerated tumor growth at dose of 30 mg/kg and 100 mg/kg.
Inhibited the invasion to peritumor areas of tumors in 30 mg/kg group but augmented tumor invasion in 100 mg/kg group of brain tissues.
Inhibited angiogenesis in doses of 30 mg/kg and 100 mg/kg.
Animal Model: CD-1 nude mice (HN5), C.B-17 SCID mice (BT474)[2]
Dosage: 10 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Inhibited tumor growth in the HN5 model by treatment dose with 30 mg/kg.
Inhibited tumor growth in the HN5 model about 95% inhibition and BT474 model about 50% inhibition by treatment dose with 10 mg/kg.
Molecular Weight

395.46

Formula

C23H21N7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN(C)C1=CC2=C(NC3=CC4=C(N(CC5=CC=CC=C5)N=C4)C=C3)N=CN=C2C=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (50.57 mM; Need ultrasonic and warming; 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 2.5287 mL 12.6435 mL 25.2870 mL
5 mM 0.5057 mL 2.5287 mL 5.0574 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 2.5287 mL 12.6435 mL 25.2870 mL 63.2175 mL
5 mM 0.5057 mL 2.5287 mL 5.0574 mL 12.6435 mL
10 mM 0.2529 mL 1.2644 mL 2.5287 mL 6.3218 mL
15 mM 0.1686 mL 0.8429 mL 1.6858 mL 4.2145 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1609 mL
25 mM 0.1011 mL 0.5057 mL 1.0115 mL 2.5287 mL
30 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5804 mL
50 mM 0.0506 mL 0.2529 mL 0.5057 mL 1.2644 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GW2974 Related Classifications

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.

Keywords:

GW2974202272-68-2GW 2974GW-2974EGFREpidermal growth factor receptorErbB-1HER1HER2glioblastomaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GW2974
Cat. No.:
HY-112293
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.