AAL993

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AAL993 

AAL993 是一种有效的、选择性的、具有口服活性的 VEGFR 抑制剂,对 VEGFR1、VEGFR2 和 VEGFR3 的 IC50 分别为 130 nM、23 nM 和 18 nM。AAL993 对其他酪氨酸激酶的抑制作用较弱。AAL993 具有有效的抗血管生成和抗肿瘤特性。

AAL993

AAL993 Chemical Structure

CAS No. : 269390-77-4

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生物活性

IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties[1].

IC50 & Target[1]

VEGFR1

130 nM (IC50)

VEGFR2

23 nM (IC50)

VEGFR3

18 nM (IC50)

体外研究
(In Vitro)

AAL993 suppresses HIF-1α expression through ERK inhibition without affecting Akt phosphorylation[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AAL993 (compound 5) potently inhibits VEGF-induced angiogenesis in an implant model, with an ED50 value of 7 mg/kg[1].
In B16 melanoma xenograft model, AAL993 (24-100 mg/kg; p.o.; daily; for 14days) inhibits both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

371.36

Formula

C20H16F3N3O

CAS 号

269390-77-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Paul W Manley , et al. Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.

    [2]. Hyun Seung Ban, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26.

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