| CAS NO: | 269390-77-4 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 371.4 |
| Cas No. | 269390-77-4 |
| Formula | C20H16F3N3O |
| Synonyms | VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253 |
| Solubility | ≤1mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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).
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