GW2974
Based on 1 Customer Validation
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.
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- Pureza : 99.16%
- No. CAS: 202272-68-2
- Fòrmula: C23H21N7
- Peso molecular:395.46
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
EGFRL858R/T790M 0.007 μM (IC50) |
HER2 0.016 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
0.07 μM
Compound: 3B
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Inhibition of erbB2 overexpressing BT 474 cell proliferation
Inhibition of erbB2 overexpressing BT 474 cell proliferation
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[PMID: 11378364] |
| Calu-3 | IC50 |
0.39 μM
Compound: 3B
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Inhibition of erbB2 overexpressing Calu3 cell proliferation
Inhibition of erbB2 overexpressing Calu3 cell proliferation
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[PMID: 11378364] |
| HB4a | IC50 |
30 μM
Compound: 3B
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Inhibition of RAS overexpressing HB4a.R4.2 cell proliferation
Inhibition of RAS overexpressing HB4a.R4.2 cell proliferation
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[PMID: 11378364] |
| HEK293 | IC50 |
50.1 μM
Compound: 17; GW2974
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Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
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[PMID: 31260312] |
| HN5 | IC50 |
0.21 μM
Compound: 3B
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Inhibition of EGF receptor overexpressing HN5 cell proliferation
Inhibition of EGF receptor overexpressing HN5 cell proliferation
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[PMID: 11378364] |
| MRC5 | IC50 |
>50 μM
Compound: 3B
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Inhibition of MRC5 cell proliferation
Inhibition of MRC5 cell proliferation
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[PMID: 11378364] |
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. .
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Cell Line:U87MG, U251MG
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Concentration:0.5-50 μM
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Incubation Time:3 h
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Result:Reduced U87MG and U251MG cells viability to 89.4% and 86.3% in 0.5 μM and 5 μM compared with control.
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Cell Line:U87MG, U251MG
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Concentration:0.5-5 μM
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Incubation Time:24 h
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Result:Inhibited U87MG and U251MG cells proliferation in 0.5 μM and 5μM.
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Cell Line:U87MG, U251MG
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Concentration:0.5-5 μM
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Incubation Time:24 h
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Result:Reduced the percentage to 55.6% and 48.6% of U87MG and U251MG cells in 0.5 μM, respectively.
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Cell Line:U87MG, U251MG
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Concentration:0.5-5 μM
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Incubation Time:24 h
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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.
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Cell Line:BT474, HN5, N87
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Concentration:0.001-100 μM
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Incubation Time:24 h
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Result:Inhibited cell growth by 50% at concentrations > 1.0 μM with IC50s < 0.4 μM.
In Vivo
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.
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Animal Model:GBM xenograft mice model[1]
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Dosage:30 mg/kg, 100 mg/kg
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Administration:Oral gavage (p.o.)
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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.
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Animal Model:CD-1 nude mice (HN5), C.B-17 SCID mice (BT474)[2]
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Dosage:10 mg/kg, 30 mg/kg
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Administration:Oral gavage (p.o.)
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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.
Chemical Information
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No. CAS 202272-68-2
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Appearance Solid
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Peso molecular 395.46
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Fòrmula C23H21N7
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Color Light yellow to yellow
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SMILES
CN(C)C1=CC2=C(NC3=CC4=C(N(CC5=CC=CC=C5)N=C4)C=C3)N=CN=C2C=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wang L, et al. Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. J Neurosci Res. 2013 Jan;91(1):128-37. [Content Brief]
[2]. Rusnak DW, et al. The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer. Cancer Res. 2001 Oct 1;61(19):7196-20. [Content Brief]
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 |
GW2974 Related Classifications
HY-112293 Related Classifications
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