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

Anticancer agent 109 Chemical Structure

CAS No. : 2097497-16-8

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Anticancer agent 109 相关抗体

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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

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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
4.2 μM
Compound: 6-15
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
CHO-K1 IC50
54.5 μM
Compound: 6-15
Cytotoxicity against CHO-K1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against CHO-K1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
DU-145 IC50
1.1 μM
Compound: 6-15
Cytotoxicity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
HEK293 IC50
26.2 μM
Compound: 6-15
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
HT-29 IC50
4.6 μM
Compound: 6-15
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
MCF7 IC50
2 μM
Compound: 6-15
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
MDA-MB-231 IC50
2.8 μM
Compound: 6-15
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
PANC-1 IC50
4 μM
Compound: 6-15
Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
U-937 IC50
6.7 μM
Compound: 6-15
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36921529]
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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