AAL993
Based on 1 Customer Validation
IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.14%
- No. CAS: 269390-77-4
- Fòrmula: C20H16F3N3O
- Peso molecular:371.36
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Ver todos los productos específicos de isoformas VEGFR
More
Actividad biológica
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VEGFR1 130 nM (IC50) |
VEGFR2 23 nM (IC50) |
VEGFR3 18 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>10 μM
Compound: AAL993
|
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
|
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
|
[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
|
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
>5.5 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
0.013 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
0.019 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
2.9 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
5.6 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| BaF3 | IC50 |
8.4 μM
Compound: AAL993
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Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
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[PMID: 26629594] |
| CHO | IC50 |
0.0012 μM
Compound: C
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Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
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[PMID: 19124243] |
| CHO | IC50 |
1.24 nM
Compound: 5
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Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells
Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells
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[PMID: 12477352] |
| HEK293 | IC50 |
0.09 μM
Compound: C
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Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
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[PMID: 16460936] |
| HEK293 | IC50 |
0.09 μM
Compound: C
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Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
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[PMID: 19124243] |
| HUVEC | IC50 |
>3 μM
Compound: AAL993
|
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
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[PMID: 26629594] |
| HUVEC | IC50 |
1 nM
Compound: AAL993
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Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
|
[PMID: 26629594] |
In B16 melanoma xenograft model, AAL993 (24-100 mg/kg; p.o.; daily; for 14days) inhibits both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 269390-77-4
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Appearance Solid
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Peso molecular 371.36
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Fòrmula C20H16F3N3O
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2NCC3=CC=NC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 125 mg/mL (336.60 mM; Need ultrasonic; 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 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]. Paul W Manley , et al. Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. [Content Brief]
[2]. Hyun Seung Ban, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26. [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 (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 | 2.6928 mL | 13.4640 mL | 26.9280 mL | 67.3201 mL |
| 5 mM | 0.5386 mL | 2.6928 mL | 5.3856 mL | 13.4640 mL | |
| 10 mM | 0.2693 mL | 1.3464 mL | 2.6928 mL | 6.7320 mL | |
| 15 mM | 0.1795 mL | 0.8976 mL | 1.7952 mL | 4.4880 mL | |
| 20 mM | 0.1346 mL | 0.6732 mL | 1.3464 mL | 3.3660 mL | |
| 25 mM | 0.1077 mL | 0.5386 mL | 1.0771 mL | 2.6928 mL | |
| 30 mM | 0.0898 mL | 0.4488 mL | 0.8976 mL | 2.2440 mL | |
| 40 mM | 0.0673 mL | 0.3366 mL | 0.6732 mL | 1.6830 mL | |
| 50 mM | 0.0539 mL | 0.2693 mL | 0.5386 mL | 1.3464 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4488 mL | 1.1220 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8415 mL | |
| 100 mM | 0.0269 mL | 0.1346 mL | 0.2693 mL | 0.6732 mL |
AAL993 Related Classifications
HY-19986 Related Classifications
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