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.
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).
Average Rating: 5
(Based on Reviews and 10 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *