EGFR/ErbB-2/ErbB-4 inhibitor-3
Based on 1 Customer Validation
EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively. EGFR/ErbB-2/ErbB-4 inhibitor-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity: 96.78%
- CAS No.: 881001-19-0
- Formula: C17H11ClFN5O
- Molecular Weight:355.75
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
All EGFR Isoforms
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Biological Activity
|
ErbB2 1.1 nM (IC50) |
ErbB1 0.3 nM (IC50) |
ErbB4 0.5 nM (IC50) |
EGFR 2.5 nM (IC50) |
HER 24 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-453 | IC50 |
24 nM
Compound: 29
|
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
|
[PMID: 16480284] |
| NIH3T3 | IC50 |
2.5 nM
Compound: 29
|
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
|
[PMID: 16480284] |
Chemical Information
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CAS No. 881001-19-0
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Appearance Solid
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Molecular Weight 355.75
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Formula C17H11ClFN5O
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Color Off-white to light yellow
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SMILES
O=C(C#CC)NC1=CC(C(NC(C=C2)=CC(Cl)=C2F)=NC=N3)=C3C=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 25 mg/mL (70.27 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (271 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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Handling Instructions (2659 KB)
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 (protect from light). 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 | 2.8110 mL | 14.0548 mL | 28.1096 mL | 70.2741 mL |
| 5 mM | 0.5622 mL | 2.8110 mL | 5.6219 mL | 14.0548 mL | |
| 10 mM | 0.2811 mL | 1.4055 mL | 2.8110 mL | 7.0274 mL | |
| 15 mM | 0.1874 mL | 0.9370 mL | 1.8740 mL | 4.6849 mL | |
| 20 mM | 0.1405 mL | 0.7027 mL | 1.4055 mL | 3.5137 mL | |
| 25 mM | 0.1124 mL | 0.5622 mL | 1.1244 mL | 2.8110 mL | |
| 30 mM | 0.0937 mL | 0.4685 mL | 0.9370 mL | 2.3425 mL | |
| 40 mM | 0.0703 mL | 0.3514 mL | 0.7027 mL | 1.7569 mL | |
| 50 mM | 0.0562 mL | 0.2811 mL | 0.5622 mL | 1.4055 mL | |
| 60 mM | 0.0468 mL | 0.2342 mL | 0.4685 mL | 1.1712 mL |