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Apogossypolone (ApoG2)

现货
Catalog No.
A4200
Bcl-2的非肽类小分子抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 7,000.00
现货
25mg
¥ 20,000.00
现货

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Background

Apogossypolone is an inhibitor of Bcl-2, Mcl-1 and Bcl-XL with Ki values of 35nM, 25nM and 660nM, respectively [1].

The MTT-based cell cytotoxicity assay shows that apogossypolone has an anticancer activity with IC50 values of 1, 2 and 3μM, respectively in PC-3, DU-145 (human prostate cancer cell lines) and MDA-MB-231(human breast cancer cell line). Apogossypolone is also found to inhibit the colony formation of DU-145 cells. The mechanism is that apogossypolone binds to Bcl-2 and prevents its association with BH3-only pro-apoptotic proteins, leading the pro-apoptotic proteins to participate in the apoptotic response [2].

Besides prostate cancer and breast cancer, apogossypolone is also potent in follicular lymphoma. Apogossypolone significantly inhibits the cell growth via inducing apoptosis in WSU-FSCCL cell line with IC50 value of 109.2nM at 72h [3].

References:
[1] Zhang XQ, Huang XF, Hu XB, Zhan YH, An QX, Yang SM, Xia AJ, Yi J, Chen R, Mu SJ, Wu DC. Apogossypolone, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces autophagy of PC-3 and LNCaP prostate cancer cells in vitro. Asian J Androl. 2010 Sep;12(5):697-708.
[2] Zhan Y, Jia G, Wu D, Xu Y, Xu L. Design and synthesis of a gossypol derivative with improved antitumor activities. Arch Pharm (Weinheim). 2009 Apr;342(4):223-9.
[3] Arnold AA, Aboukameel A, Chen J, Yang D, Wang S, Al-Katib A, Mohammad RM. Preclinical studies of Apogossypolone: a new nonpeptidic pan small-molecule inhibitor of Bcl-2, Bcl-XL and Mcl-1 proteins in Follicular Small Cleaved Cell Lymphoma model. Mol Cancer. 2008 Feb 14;7:20.

文献引用

1. Lin D, Wang X, et al. "Apogossypolone acts as a metastasis inhibitor via up-regulation of E-cadherin dependent on the GSK-3/AKT complex." Am J Transl Res. 2019 Jan 15;11(1):218-232. PMID:30787981
2. Lin D, Li X, et al. "Apogossypolone (ApoG2) induces ROS-dependent apoptosis and reduces invasiveness of PC12 cells in vitro and in vivo." Am J Transl Res. 2017 Sep 15;9(9):3990-4002. eCollection 2017. PMID:28979675

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt490.501
Cas No.886578-07-0
FormulaC28H26O8
Solubility≥24.55 mg/mL in DMSO, ≥51.2 mg/mL in EtOH with ultrasonic, <2.47 mg/mL in H2O
Chemical Name1,1',4,4'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-6,6',7,7'-tetraone
SDFDownload SDF
Canonical SMILESOC(C(C1=C(C2=O)C(C)C)=CC2=O)=C(C(C)=C1O)C(C(C)=C3O)=C(C(C3=C(C4=O)C(C)C)=CC4=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人前列腺癌PC-3和LNCaP细胞系

溶解方法

在DMSO中的溶解度大于10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

24-96 h,5-20 mg/L

应用

Apogossypolone是一种新型的Bcl-2家族蛋白抑制剂,它以剂量依赖的方式抑制PC-3和LNCaP细胞的生长。用Apogossypolones处理PC-3和LNCaP细胞可诱导自噬,细胞质中出现膜空泡,有酸性自噬泡形成。Apogossypolones处理后两种细胞系的自噬相关蛋白beclin-1和LC3-II表达增加。

动物实验[2]:

动物模型

4周龄的雄性Balb/c nu/nu裸鼠

剂量

2.5, 5, 10 mg/kg的剂量腹腔给药,每天1次,持续10天

应用

Apogossypolone能够显著抑制前列腺癌皮下种植体的生长。Apogossypolone可降低肿瘤组织内PCNA和CD31的表达,上调caspases-3和caspase-8的表达,表明Apogossypolone可诱导细胞凋亡,抑制肿瘤增殖和血管生成。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Zhang X Q, Huang X F, Hu X B, et al. Apogossypolone, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces autophagy of PC-3 and LNCaP prostate cancer cells in vitro[J]. Asian journal of andrology, 2010, 12(5): 697.

[2]. Xianqing Z, Xiaofeng H, Shijie M, et al. Inhibitory effect of a new gossypol derivative apogossypolone (ApoG2) on xenograft of human prostate cancer cell line PC-3[J]. Journal of Medical Colleges of PLA, 2009, 24(5): 274-282.

生物活性

Description Apogossypolone是一种Bcl-2的非肽类小分子抑制剂。
靶点 Bcl-2          
IC50            

质量控制

化学结构

Apogossypolone (ApoG2)

相关生物数据

Apogossypolone (ApoG2)

相关生物数据

Apogossypolone (ApoG2)