Reparixin L-lysine salt
(Synonyms: REPERTAXINL-赖氨酸盐,Repertaxin L-lysine salt) 目录号 : GC13813
Perifosine is an orally active alkyl phospholipid analogue that has shown antitumor activity in a variety of cancers by interfering .
Cas No.:266359-93-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
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Preparation Method |
Cells were incubated with increasing concentrations of perifosine for 24h, 48h and 72h and the number of viable cells was determined by crystal violet staining. |
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Reaction Conditions |
10µM-40µM;24h, 48h and 72h |
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Applications |
AKT phosphorylation was dose-dependently inhibited by perifosine. Concomitantly, perifosine displayed anti-tumor activity in both cell lines. |
| Animal experiment [2]: | |
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Animal models |
Five-week-old male BALB/c nude mice |
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Preparation Method |
DU 145 or H1915 cells were subcutaneously inoculated into the right flank of mice and allowed to form a palpable tumor. |
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Dosage form |
45 and 180 mg/kg;p.o |
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Applications |
Perifosine Preferably Accumulates in H1915 Tumor Xenografts. Perifosine Reduced Cell Proliferation and Induced Apoptosis Preferentially in H1915 Tumor Xenografts. |
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References: [1]. Engel JB, Honig A, et,al. Perifosine inhibits growth of human experimental endometrial cancers by blockade of AKT phosphorylation. Eur J Obstet Gynecol Reprod Biol. 2008 Nov;141(1):64-9. doi: 10.1016/j.ejogrb.2008.06.007. Epub 2008 Aug 6. PMID: 18687514. | |
Perifosine is an orally active alkyl phospholipid analogue that has shown antitumor activity in a variety of cancers by interfering with Akt membrane translocation targeting Akt activity and inhibiting AKT phosphorylation[1-3].
Perifosine (0.5 µM) blocked Akt activation in all three pancreatic cancer cell lines(PANC-1, MIA and AsPC-1)[6]. AKT phosphorylation was dose-dependently inhibited by perifosine(10µM-40µM;24h, 48h and 72h). Concomitantly, perifosine displayed anti-tumor activity in both cell lines[4].
Perifosine(45 and 180 mg/kg;p.o) Accumulates in H1915 Tumor Xenografts. Perifosine Reduced Cell Proliferation and Induced Apoptosis Preferentially in H1915 Tumor Xenografts[5]. In vivo, perifosine (1 mg/kg; i.g;once daily for 20 days) and ABT-737 co-administration strikingly inhibited A549 lung cancer xenograft growth in nude mice[7].
References:
[1]. Holohan B, Hagiopian MM, et,al Perifosine as a potential novel anti-telomerase therapy. Oncotarget. 2015 Sep 8;6(26):21816-26. doi: 10.18632/oncotarget.5200. PMID: 26307677; PMCID: PMC4673128.
[2]. Fensterle J, Aicher B, et,al. Current view on the mechanism of action of perifosine in cancer. Anticancer Agents Med Chem. 2014 May;14(4):629-35. doi: 10.2174/1871520614666140309225912. PMID: 24628236.
[3]. Chen MB, Wu XY, et,al. Perifosine sensitizes curcumin-induced anti-colorectal cancer effects by targeting multiple signaling pathways both in vivo and in vitro. Int J Cancer. 2012 Dec 1;131(11):2487-98. doi: 10.1002/ijc.27548. Epub 2012 Jul 3. PMID: 22438101.
[4]. Engel JB, Honig A, et,al. Perifosine inhibits growth of human experimental endometrial cancers by blockade of AKT phosphorylation. Eur J Obstet Gynecol Reprod Biol. 2008 Nov;141(1):64-9. doi: 10.1016/j.ejogrb.2008.06.007. Epub 2008 Aug 6. PMID: 18687514.
[5]. Taniguchi K, Suzuki T, et,al. Perifosine, a Bioavailable Alkylphospholipid Akt Inhibitor, Exhibits Antitumor Activity in Murine Models of Cancer Brain Metastasis Through Favorable Tumor Exposure. Front Oncol. 2021 Nov 4;11:754365. doi: 10.3389/fonc.2021.754365. PMID: 34804943; PMCID: PMC8600181.
[6]. Xin Y, Shen XD, et,al. Perifosine inhibits S6K1-Gli1 signaling and enhances gemcitabine-induced anti-pancreatic cancer efficiency. Cancer Chemother Pharmacol. 2014 Apr;73(4):711-9. doi: 10.1007/s00280-014-2397-9. Epub 2014 Feb 12. PMID: 24519751.
[7]. Shen J, Xu L, et,al. Perifosine and ABT-737 synergistically inhibit lung cancer cells in vitro and in vivo. Biochem Biophys Res Commun. 2016 May 13;473(4):1170-1176. doi: 10.1016/j.bbrc.2016.04.035. Epub 2016 Apr 9. PMID: 27073162.
| Cas No. | 266359-93-7 | SDF | |
| 别名 | REPERTAXINL-赖氨酸盐,Repertaxin L-lysine salt | ||
| 化学名 | (2S)-2,6-diaminohexanoic acid;(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide | ||
| Canonical SMILES | CC(C)CC1=CC=C(C=C1)C(C)C(=O)NS(=O)(=O)C.C(CCN)CC(C(=O)O)N | ||
| 分子式 | C20H35N3O5S | 分子量 | 429.57 |
| 溶解度 | ≥ 21.5 mg/mL in DMSO, ≥ 66.67 mg/mL in EtOH, ≥ 16.67 mg/mL in Water with gentle warming | 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 | 2.3279 mL | 11.6395 mL | 23.2791 mL |
| 5 mM | 0.4656 mL | 2.3279 mL | 4.6558 mL |
| 10 mM | 0.2328 mL | 1.164 mL | 2.3279 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。