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AAL-993 Sale

(Synonyms: VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253) 目录号 : GC10938

Inhibitor of VEGFR1, 2, and 3

AAL-993 Chemical Structure

Cas No.:269390-77-4

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1mg
¥420.00
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5mg
¥714.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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
别名 VEGFR Tyrosine Kinase Inhibitor VI,ZK 260253
化学名 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
分子式 C20H16F3N3O 分子量 371.4
溶解度 ≤1mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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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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