2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Axl-IN-17

Axl-IN-17（compound 13c）是一种口服有效的，具有选择性的 AXL 抑制剂，IC50 值为 3.0 nM。Axl-IN-17 展现出抗肿瘤活性。

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Axl-IN-17 Chemical Structure

Axl-IN-17 Chemical Structure

CAS No. : 3048409-80-6

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Axl-IN-17 相关抗体

Top Publications Citing Use of Products

查看 TAM Receptor 亚型特异性产品:

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Axl Mer Tyro3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy[1].

IC50 & Target

Axl

 

Axl

3.23 nM (IC50)

Mer

 

Tyro3

 

体外研究
(In Vitro)

Axl-IN-17 在1 μM 的浓度下可以抑制 TYRO3，MER，MET，RON 等多种激酶[1]。
Axl-IN-17 在 BaF3/TEL-AXL 细胞中展现出抗增殖活性，IC50 值＜1 nM[1]。
Axl-IN-17 (1 nM，2 h) 抑制 AXL 磷酸化和其下游信号通路[1]。

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

Axl-IN-17 相关抗体:

Cell Proliferation Assay[1]

Cell Line: BaF3/TEL-AXL
Concentration: 1 nM
Incubation Time: 72 h
Result: Inhibited proliferation activity in BaF3/TEL-AXL cells.

Western Blot Analysis[1]

Cell Line: BaF3/TEL-AXL
Concentration: 1 nM
Incubation Time: 2 h
Result: Inhibited phosphorylation of AXL and its downstream signaling
体内研究
(In Vivo)

Axl-IN-17 （口服，3 mg/kg，每天一次）具有良好的药代动力学特性，半衰期是10.09 小时，AUC 值是59815 ng•h/mL[1]。
Axl-IN-17（p.o.，25，50，100 mg/kg，每天一次，共七天）在 AXL 驱动的肿瘤异种小鼠中表现出抗肿瘤效应[1]。

AXL-IN-17在雄性Sprague-Dawley鼠体内的药代动力学分析[1]

Route Dose (mg/kg) AUC0→∞ (ng·h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) MRT0→∞(h)
p.o. 3 mg/kg 59815 10.09 2 2906 16.5

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

Animal Model: Male Sprague-Dawley rats /pharmacokinetic[1]
Dosage: 3 mg/kg (p.o.), once daily
Administration: Oral gavage
Result: Revealed a T1/2 value of 10.09 h and an AUC value of 59815 ng•h/mL.
Animal Model: BaF3/TEL-AXL xenograft mice[1]
Dosage: 25, 50 or 100 mg/kg, once daily for 7 days
Administration: Oral gavage
Result: Induced tumor regression.
分子量

563.60

Formula

C32H27F2N7O
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

Axl-IN-17 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

Axl-IN-173048409-80-6TAM ReceptorTyro3AxlMerreceptor tyrosine kinase AXLBaF3/TEL-AXLantitumorTYRO3MERMETRONInhibitorinhibitorinhibit

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目录号：
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