2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Anticancer agent 109

Anticancer agent 109 (compound 6-15)是 Gas6-Axl 轴的抑制剂，具有抑癌活性。Anticancer agent 109 抑制 Gas6和 Axl 的表达，抑制 p-PI3K 和 p-AKT 的表达，导致肿瘤细胞周期 G1 期阻滞进而促进细胞凋亡 ( apoptosis ) 并在裸鼠荷瘤模型中显著抑制肿瘤生长。

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Anticancer agent 109 Chemical Structure

Anticancer agent 109 Chemical Structure

CAS No. : 2097497-16-8

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Anticancer agent 109 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models[1].

IC50 & Target[1]

Axl

 

体外研究
(In Vitro)

Anticancer agent 109 (10 μM，48 小时) 抑制 A549 细胞 Gas6 和 Axl，抑制 PANC-1 细胞 Gas6-Axl 轴相关蛋白，诱导 G1 期阻滞并促进晚期凋亡，但不改变 DNA 合成[1]。

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

Anticancer agent 109 相关抗体:

Cell Viability Assay[1]

Cell Line: MCF-7; PANC-1; MDA-MB-231 ; HT-29 ; DU145 ; U937 ; A549 ; PANC-1
Concentration: 30 μM
Incubation Time: 48 h
Result: Inhibited the growth of cancer cells, and was up to 20-fold safer against normal cells and up to 5.4-fold more active than Sunitinib against the cancer cells.
Inhibited growth with IC50s of 2.0 μM (MCF-7); 2.8 μM (MDA-MB-231); 4.6 μM (HT-29); 1.1 μM (DU145); 6.7 μM (U937); 4.2 μM (A549); 4.0 μM (PANC-1).

Apoptosis Analysis[1]

Cell Line: PANC-1
Concentration: 1 μM , 5 μM , 10 μM
Incubation Time: 48 h
Result: Increased the sub-G1 fraction and induced late apoptosis.

Western Blot Analysis[1]

Cell Line: A549; PANC-1
Concentration: 10 μM
Incubation Time: 48 h
Result: Inhibited Gas6 and Axl in A549 and PANC-1 cell, increased the expression ratio of Bax/Bcl-2 and inhibited p-PI3K and p-AKT in PANC-1 cell.

RT-PCR[1]

Cell Line: PANC-1
Concentration: 3 μM ;5 μM 10 μM
Incubation Time: 48 h
Result: Inhibited Gas6 and Axl.
体内研究
(In Vivo)

Anticancer agent 109 (3 mg/kg，腹腔注射，A549 肿瘤模型 3 1天，PANC-1 肿瘤模型 85 天，每周 6 次) 在裸鼠异种移植模型中显著降低肿瘤的大小和重量[1]。

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

Animal Model: A549 or PANC-1 xenografted in BALB/c-nu mice[1].
Dosage: 1 mg/kg; 3 mg/kg
Administration: Intraperitoneal injection (i.p.) 6 times a week
Result: Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models.
Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models.
分子量

317.34

Formula

C19H15N3O2
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

Anticancer agent 109 相关分类

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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.

Keywords:

Anticancer agent 1092097497-16-8Anticancer agent109Anticancer agent-109TAM ReceptorTyro3AxlMerA549PANC-1xenograftanticancerInhibitorinhibitorinhibit

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