GW768505A free base
Based on 1 Customer Validation
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity.
For research use only. We do not sell to patients.
- Purity: 99.26%
- CAS No.: 501693-25-0
- Formula: C27H19F4N5O3
- Molecular Weight:537.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All VEGFR Isoforms
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Biological Activity
|
KDR |
Tie2 |
Tie-2 |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HFF | IC50 |
0.79 μM
Compound: 7k
|
Cytotoxic concentration against HFF cells was determined
Cytotoxic concentration against HFF cells was determined
|
[PMID: 15837294] |
| HUVEC | IC50 |
0.045 μM
Compound: 7k
|
Concentration required for growth inhibition of human umbilical vein endothelial cells stimulated by VEGF
Concentration required for growth inhibition of human umbilical vein endothelial cells stimulated by VEGF
|
[PMID: 15837294] |
| NIH3T3 | IC50 |
0.0063 μM
Compound: 7k
|
Concentration required to inhibit autophosphorylation of tyrosine protein kinase receptor TIE-2 transfected in 3T3 cells
Concentration required to inhibit autophosphorylation of tyrosine protein kinase receptor TIE-2 transfected in 3T3 cells
|
[PMID: 15837294] |
GW768505A free base has inhibition for cancer cells growth in NCI-60 panel screening[2].
GW768505A free base is an inhibitor of KDR and TIE2, shows potent inhibition (71–88% inhibition at 100 nM) of the tropomysin-related kinases TRKA, TRKB and TRKC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 501693-25-0
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Appearance Solid
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Molecular Weight 537.47
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Formula C27H19F4N5O3
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=C(C4=CC=C(OC)C=C4)OC5=NC=NC(N)=C53)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 8.33 mg/mL (15.50 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. 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. 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 (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Miyazaki Y, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8. [Content Brief]
[2]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103. [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. 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 | 1.8606 mL | 9.3028 mL | 18.6057 mL | 46.5142 mL |
| 5 mM | 0.3721 mL | 1.8606 mL | 3.7211 mL | 9.3028 mL | |
| 10 mM | 0.1861 mL | 0.9303 mL | 1.8606 mL | 4.6514 mL | |
| 15 mM | 0.1240 mL | 0.6202 mL | 1.2404 mL | 3.1009 mL |