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AAL-993 (Synonyms: VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253)

Catalog No.GC10938

IC50 de 130 nM, 23 nM et 18 nM pour VEGFR1, VEGFR2 et VEGFR3, respectivement.

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AAL-993 Chemical Structure

Cas No.: 269390-77-4

Taille Prix Stock Qté
1mg
41,00 $US
En stock
5mg
70,00 $US
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 269390-77-4 SDF
Synonymes 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
Solubility ≤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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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