1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. 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。

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Axl-IN-3 Chemical Structure

Axl-IN-3 Chemical Structure

CAS No. : 2783991-34-2

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查看 TAM Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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

Axl

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
SK-OV-3 GI50
1.02 μM
Compound: 54
Antiproliferative activity against human SK-OV-3 cells as reduction in cell growth measured after 72 hrs by Celltiter-Glo luminescent assay
Antiproliferative activity against human SK-OV-3 cells as reduction in cell growth measured after 72 hrs by Celltiter-Glo luminescent assay
[PMID: 34600239]
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].

MCE 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

464.95

Formula

C24H25ClN6O2

CAS 号
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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Axl-IN-3
目录号:
HY-144706
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