Axl-IN-3

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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。

Axl-IN-3 

Axl-IN-3 是一种有效的、选择性的、具有口服活性的 AXL 激酶抑制剂，IC50 为 41.5 nM。Axl-IN-3 对其他激酶的抑制作用较低。

Axl-IN-3

Axl-IN-3 Chemical Structure

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生物活性

Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases[1].

IC50 & Target

IC50: 41.5 nM (AXL kinase)[1]
体外研究
(In Vitro)

Axl-IN-3 (Compound 54) shows anti-proliferative activity in SKOV3 cells with a GI50 of 1.02 μM[1].
Axl-IN-3 (Compound 54; 1-10 μM; pretreated 1 h) inhibits AXL signaling in SKOV3 cells. Axl-IN-3 shows a dose dependent reduction of phosphorylated AXL (pAXL) levels compared to untreated cells. Additionally, the reduction of pAXL levels also lead to the concomitant reduction in downstream pERK1/2 levels[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Pharmacokinetic studies of Axl-IN-3 (Compound 54) at 5 mg/kg reveal rapid oral absorption with a Tmax of 0.25 hr, Cmax of 460 ng/mL, T1/2 of 2.46 hr, and area under the curve (AUC) values of 1620 (ng*hr/mL)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

464.95

Formula

C24H25ClN6O2
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]. Pearly Shuyi Ng, et al. Fragment-based lead discovery of indazole-based compounds as AXL kinase inhibitors. Bioorg Med Chem. 2021 Nov 1;49:116437.

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