AAL-993 (Synonyms: VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253) |
| رقم الكتالوجGC10938 |
IC50s من 130 نانومتر و 23 نانومتر و 18 نانومتر لـ VEGFR1 و VEGFR2 و VEGFR3 ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 269390-77-4
Sample solution is provided at 25 µL, 10mM.
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IC50: 130, 23, and 18 nM for VEGFR1, 2, and 3, respectively
AAL-993 is a VEGF receptor inhibitor.
A key pro-angiogenic cytokine released by tumor is vascular endothelial growth factor (VEGF). The angiogenic activity of the VEGF family of proteins is mediated by two high affinity receptors, VEGFR-1 and VEGFR-2 located on vascular endothelial cells.
In vitro: AAL-993 was found to be a highly potent and selective inhibitor of the recombinant VEGFR-2 and VEGFR-3 kinases. At 3- to 5-fold higher concentration, AAL-993 also inhibited VEGFR-1 and, although it possessed some activity against other members of the PDGFR kinase family at submicromolar concentrations, AAL-993 did not significantly inhibit any of the other kinases tested at concentrations <10 μM. In addition, AAL-993 was capable of penetrating cells and inhibit the VEGF-stimulated tyrosine autophosphorylation of human VEGFR-2 in CHO cells [1].
In vivo: Animal efficacy study found that AAL-993 was able to potently inhibit VEGF-induced angiogenesis in an implant model, with ED50 values of 7 mg/kg. Moreover, in a mouse orthotopic model of melanoma, AAL-993 could potently inhibit both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Manley, P. W.,Furet, P.,Bold, G., et al. Anthranilic acid amides: A novel class of antiangiogenic VEGF receptor kinase inhibitors. Journal of Medicinal Chemistry 45(26), 5687-5693 (2002).
| Cas No. | 269390-77-4 | SDF | |
| المرادفات | VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253 | ||
| Chemical Name | 2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]-benzamide | ||
| Canonical SMILES | O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2NCC3=CC=NC=C3 | ||
| Formula | C20H16F3N3O | M.Wt | 371.4 |
| الذوبان | ≤1mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6925 mL | 13.4626 mL | 26.9251 mL |
| 5 mM | 0.5385 mL | 2.6925 mL | 5.385 mL |
| 10 mM | 0.2693 mL | 1.3463 mL | 2.6925 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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