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

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规格 是否有货
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Customer Review

  • 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

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.

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

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.

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产品名称:
Axl-IN-17
目录号:
HY-162085
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