Apogossypolone (ApoG2)
(Synonyms: ApoG2) 目录号 : GC14080
Apogossypolone (ApoG2) (ApoG2) 是一种具有口服活性的 Bcl-2 家族蛋白抑制剂，对 Bcl-2、Mcl-1 和 Bcl-XL 的 Ki 值分别为 35、25 和 660 nM。
Cas No.:886578-07-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment[1]: | |
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Cell lines |
human prostate cancer cell lines PC-3 and LNCaP |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
24-96 h, 5-20 mg/L |
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Applications |
Apogossypolone is a novel inhibitor of Bcl-2 family proteins. Apogossypolone inhibited PC-3 and LNCaP cell growth in a dose-dependent manner. Treating PC-3 and LNCaP cells with apogossypolone induced autophagy, for the appearance of membranous vacuoles in the cytoplasm and the formation of acidic vesicular organelles. Expression of autophagy-associated beclin-1 and LC3-II were also increased in both cell lines after apogossypolone treatment. |
| Animal experiment [2]: | |
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Animal models |
Male 4-week-old Balb/c nu/nu mice |
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Dosage form |
2.5, 5, 10 mg/kg, intraperitoneal administration daily for 10 days. |
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Application |
Apogossypolone can significantly inhibit the growth of subcutaneous prostatic carcinoma implant. Apogossypolone decreased the expression of PCNA and CD31, enhanced the expression of caspases-3, caspase-8 in tumor tissues, indicating an induction of apoptosis and inhibition of tumor proliferation and angiogenesis. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| Cas No. | 886578-07-0 | SDF | |
| 别名 | ApoG2 | ||
| 化学名 | 6,6',7,7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-1,1',4,4'-tetraone | ||
| Canonical SMILES | CC1=C(C2=C(C(=O)C(=O)C=C2C(=C1C3=C(C4=CC(=O)C(=O)C(=C4C(=C3C)O)C(C)C)O)O)C(C)C)O | ||
| 分子式 | C28H26O8 | 分子量 | 490.501 |
| 溶解度 | ≥ 24.55 mg/mL in DMSO, ≥ 51.2 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0387 mL | 10.1937 mL | 20.3873 mL |
| 5 mM | 0.4077 mL | 2.0387 mL | 4.0775 mL |
| 10 mM | 0.2039 mL | 1.0194 mL | 2.0387 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet