Antineoplaston A10
(Synonyms: 3-苯基乙酰氨基-2,6-哌啶二酮) 目录号 : GC35361
Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
Cas No.:91531-30-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
[1] Stanislaw R Burzynski, et al. Childs Nerv Syst. 2014 Dec;30(12):2051-61. [2] Xian-Jun Qu, et al. Anticancer Res. Jul-Aug 2007;27(4B):2427-31.
| Cas No. | 91531-30-5 | SDF | |
| 别名 | 3-苯基乙酰氨基-2,6-哌啶二酮 | ||
| Canonical SMILES | O=C(N[C@@H](CC1)C(NC1=O)=O)CC2=CC=CC=C2 | ||
| 分子式 | C13H14N2O3 | 分子量 | 246.26 |
| 溶解度 | DMSO: 250 mg/mL (1015.19 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0607 mL | 20.3037 mL | 40.6075 mL |
| 5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL |
| 10 mM | 0.4061 mL | 2.0304 mL | 4.0607 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。
Inhibitory effect of Antineoplaston A10 and AS2-1 on human hepatocellular carcinoma
Kurume Med J 1996;43(2):137-47.PMID:8755117DOI:10.2739/kurumemedj.43.137.
Antineoplastons, first described by Burzynski, are naturally occurring peptides and amino acid derivatives which control neoplastic growth. Antineoplaston A10 (3-pehnylacetylamino-2,6-piperidinedion) is the first chemically identified antineoplastons and when it is administered orally it is hydrolysed in pancreatic juice to phenylactylglutamine and phenylacetylisoglutamine in the ration of 4 to 1. These metabolites are water soluble and have antitumor effect, they are further degraded to pehnylacetic acid. The mixture of phenylacetylglutamine and phenylacetylisoglutamine in the ratio of 4 to 1 was formulated as Antineoplaston A10 injectable formulation. The mixture of phenylacetylglutamine and phenylacetic acid in the ratio of 1 to 4 was also shown to have antitumor effect in tissue culture study, then formulated as Antineoplaston AS2-1. The reported cytostatic inhibitory effect of A10 on human hepatocellular carcinoma cells and differentiation inducing effect of AS2-1 on various tumor cells suggest potential benefit for the treatment of human hepatocellular carcinoma since this tumor recurs frequently despite initial successful treatment. We report here the effects of Antineoplaston A10 and AS2-1 on cell proliferation, cell morphology, cell cycle, and DNA in human hepatocellular carcinoma cell lines. Both agents inhibited cell proliferation and increased the number of cells in G0 and G1 phases and Antineoplaston AS2-1 induced apoptosis, we also describe our clinical experience of a hepatocellula carcinoma (HCC) patient whose tumor, after incomplete trancathere arterial embolization (TAE) for a 7cm 7cm HCC, has been stable for more than 15 months during which time he has been taking Antineoplaston AS2-1 continuously without any serious adverse effects.
Induction of apoptosis in human hepatocellular carcinoma cells by synthetic Antineoplaston A10
Anticancer Res 2007 Jul-Aug;27(4B):2427-31.PMID:17695534doi
Antineoplaston A10 (3-phenylacetylamino-2,6-piperidinedion) is a naturally occurring substance and was the first antineoplaston in the human body to be chemically identified. The effect of Antineoplaston A10 on human hepatocellular carcinoma cell lines HepG2 and HLE has been examined. Antineoplaston A10 displayed anti-proliferative action inhibiting cell growth in a dose- and time-dependent manner in vitro as measured by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and clonogenic assays. Incubation with Antineoplaston A10 for 48 h induced apoptotic events such as a typical apoptotic morphology, formation of a characteristic ladder pattern of DNA migration and accumulation of sub-G1 phase cells. Next, hepatoma xenografts in nude mice were employed to study the antitumor effects of Antineoplaston A10 in vivo. Oral administration of Antineoplaston A10 delayed the growth of HepG2 and HLE cells in the mice without a reduction in body weight. A higher proportion of apoptotic cells in xenografts was observed by means of terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL) staining. In addition, the level of expression of apoptotic marker p53 increased while that of anti-apoptotic protein bcl-2 decreased, as evaluated with immunohistochemical staining in the xenografts. These results suggested that Antineoplaston A10 may inhibit the growth of human hepatoma cells through the induction of apoptosis.
Theoretical investigations on the structure and potential binding sites of Antineoplaston A10 and experimental findings
Drugs Exp Clin Res 1990;16(7):343-9.PMID:2092960doi
The essential biological importance of antineoplastons has motivated the present theoretical and experimental studies on the structure and potential binding sites of Antineoplaston A10, 3-phenylacetylamino-2,6-piperidinedione. Semi-empirical molecular orbital calculations SCF-LCAO-MO were performed using the MNDO method. The calculated molecular geometry of A10 is in very good agreement with the recently obtained X-ray structure of synthetic A10. Experimental investigations of the Raman spectra of A10 and its N,N-dideuterated derivative confirm the theoretical predictions concerning the structure and hydrogen bonding of A10. Analysis of calculated charge distribution reveals that the negative charges are localized on the ring nitrogen and on the exocyclic oxygen atoms of A10 and are similar to the corresponding charges computed for some pyrimidine bases. This indicates that Antineoplaston A10 may have similar binding sites. It is concluded that the mechanism of action of Antineoplaston A10 may in part be related to its structural and chemical resemblance with deoxythymidine and uridine. A10 may act as a nucleoside antagonist and interact very closely with adenosine units in nucleic acids and enzymes, which may interfere with protein synthesis in neoplastic cells.
Phase II study of Antineoplaston A10 and AS2-1 in patients with recurrent diffuse intrinsic brain stem glioma: a preliminary report
Drugs R D 2003;4(2):91-101.PMID:12718563DOI:10.2165/00126839-200304020-00002.
Objective: A phase II study of Antineoplaston A10 and AS2-1 was conducted to evaluate the antineoplastic activity in patients with recurrent diffuse intrinsic brain stem glioma. Patients and methods: This report describes the results of treatment of the first 12 patients admitted to the study. Patients received escalating doses of Antineoplaston A10 and AS2-1 by intravenous bolus injections. The median duration of treatment was 6 months and the average dosage of Antineoplaston A10 was 11.3 g/kg/day and of antineoplaston AS2-1 0.4 g/kg/day. Responses were assessed by gadolinium-enhanced magnetic resonance imaging of the head. Results: Of ten evaluable patients, complete response was determined in two cases (20%), partial response in three (30%), stable disease in three (30%) and progressive disease in two (20%). Survival at 2 years was 33.3%. Currently, of all 12 patients, two (17%) were alive and tumour free for over 5 years since initial diagnosis; one was alive for more than 5 years, and another for more than 4 years from the start of treatment. Only mild and moderate toxicities were observed, which included three cases of skin allergy, two cases of anaemia, fever and hypernatraemia, and single cases of agranulocytosis, hypoglycaemia, numbness, tiredness, myalgia and vomiting. Conclusion: The results of this study compared favourably with the responses of patients treated with radiation therapy and chemotherapy. The study continues with accrual of additional patients.
Antineoplaston treatment for advanced hepatocellular carcinoma
Oncol Rep 1998 Nov-Dec;5(6):1363-7.PMID:9769368DOI:10.3892/or.5.6.1363.
Antineoplaston A10 injection (Antineoplaston A10 I) exhibited cystostatic growth inhibition of human hepatocellular carcinoma (HCC) cells in vitro and showed minimum adverse effects in a phase I clinical trial. Advanced HCC is hard to control because the potent anticancer drugs or embolizations easily induce hepatic failure. We review herein 2 cases of advanced HCC treated with Antineoplaston A10 I. Both cases showed interesting responses to Antineoplaston A10 I. One showed massive coagulation necrosis of tumors after intra-arterial infusion of Antineoplaston A10 I and the other showed resolution of portal vein tumor thrombosis with systemic infusion of Antineoplaston A10 I. The usefulness of anti-neoplaston A10 I in terminal staged HCC is discussed.