AAL-993 是口服有效的VEGFR选择性抑制剂，抑制 VEGFR1、VEGFR2 和 VEGFR3 的IC50分别为 130 nM、23 nM 和 18 nM，对其他酪氨酸激酶的抑制作用较弱。AAL-993 具有抗血管生成和抗肿瘤的活性。

AAL-993 is a potent VEGFR inhibitor with IC50s of 130 nM, 23 nM and 18 nM for VEGFR1, VEGFR2 and VEGFR3, respectively. AAL993 has a weak inhibitory effect on other tyrosine kinases. AAL993 also shows potent antiangiogenic and antitumor activities.

AAL993 suppressed HIF-1α expression through the inhibition of ERK without affecting Akt phosphorylation[1].

AAL993 (24-100 mg/kg; p.o.) inhibited both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases in B16 melanoma xenograft model[2]. AAL993 potently inhibited VEGF-induced angiogenesis with an ED50 value of 7 mg/kg in an implant model[2].

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371.356

(< 1 mg/ml refers to the product slightly soluble or insoluble )
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In solvent: -80°C for 2 years