Perifosine
(Synonyms: 哌立福新; KRX-0401; NSC 639966; D21266) 目录号 : GC15680
Perifosine 是 Akt 的抑制剂 。
Cas No.:157716-52-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
CRW22RV1 cells |
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Preparation method |
Cells (1.2×105) were seeded in 6-cm diameter dishes and incubated overnight to allow the cells to attach. Cells were then treated with perifosine and immediately thereafter with 6 Gy of radiation. To assess the effect of perifosine on radiation-induced apoptosis, the Annexin-FITC based flow cytometry analysis was used. Both nuclear fragmentations with PI staining and translocated membrane phosphatidylserine (PS) with Annexin V staining were measured. |
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Reaction Conditions |
10 μM, 24 hours |
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Applications |
Both perifosine and radiation induced significant apoptotic responses as shown by the increase of apoptotic cells. When radiation (6Gy) and perifosine (10 μM) were combined, the number of apoptotic cells was significantly increased. Perifosine alone did not induce cell cycle arrest at the G2/M phases and perifosine did not affect the IR-induced G2/M checkpoint. |
| Animal experiment: [1] | |
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Animal models |
Male Athymic Nude-Foxn1nu mice injected with CRW22RV1 cells |
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Dosage form |
Oral administration, in a loading dose of 300 mg/kg (2 × 150 mg/kg separated by 12 hours) followed by daily maintenance doses of 35 mg/kg for 5 days |
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Applications |
Mice were separated into 4 groups: control, perifosine, radiotherapy and combined therapy. Perifosine alone did not have a significant effect on tumor growth. However, perifosine can significantly increase radiation induced tumor growth delay. To reach the 10-fold size of tumor volume to the initial volume in the control, it took 15, 19, 41 and 59 days in control, perifosine only, radiation only and combined treatment groups, respectively. It is noted that the combined treatment led to a complete remission of the CWR22RV1 tumor. |
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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] Gao Y, Ishiyama H, Sun M, et al. The alkylphospholipid, perifosine, radiosensitizes prostate cancer cells both in vitro and in vivo. Radiation oncology (London, England), 2011, 6: 39. |
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Perifosine is an inhibitor of Akt [1].
Perifosine is a synthetic antitumor alkylphospholipid. It induces cell apoptosis through inhibiting the activity of Akt. Perifosine shows antitumor activity in various cell lines including NSCLC, MM, epithelial carcinoma, prostate carcinoma and leukemia cells. In H460 cells, perifosine decreased cell survival and induced apoptosis with IC50 values of 1μM and 10 μM, respectively. The treatment of perifosine was also found to induce cleavage of caspase-8, caspase-9, caspase-3 and PARP in this cell line. In MM.1S cells, perifosine induced sub-G1 phase population increase from 15% to 57% at 10 μM and induced cleavage of caspase-8, caspase-9 and PARP in a dose-dependent manner. In mice inoculated with MM.1S cells, oral administration of perifosine significantly reduced MM tumor growth and increased survival [1, 2].
References:
[1] Elrod H A, Lin Y D, Yue P, et al. The alkylphospholipid perifosine induces apoptosis of human lung cancer cells requiring inhibition of Akt and activation of the extrinsic apoptotic pathway. Molecular cancer therapeutics, 2007, 6(7): 2029-2038.
[2] Hideshima T, Catley L, Yasui H, et al. Perifosine, an oral bioactive novel alkylphospholipid, inhibits Akt and induces in vitro and in vivo cytotoxicity in human multiple myeloma cells. Blood, 2006, 107(10): 4053-4062.
Perifosine 是 Akt 的抑制剂 [1]。
Perifosine 是一种合成的抗肿瘤烷基磷脂。它通过抑制 Akt 的活性来诱导细胞凋亡。 Perifosine 在多种细胞系中表现出抗肿瘤活性，包括 NSCLC、MM、上皮癌、前列腺癌和白血病细胞。在 H460 细胞中，perifosine 降低细胞存活率并诱导细胞凋亡，IC50 值分别为 1μM 和 10 μM。还发现哌立福新处理可诱导该细胞系中 caspase-8、caspase-9、caspase-3 和 PARP 的裂解。在 MM.1S 细胞中，perifosine 在 10 μM 时诱导亚 G1 期细胞群从 15% 增加到 57%，并以剂量依赖的方式诱导 caspase-8、caspase-9 和 PARP 的裂解。在接种 MM.1S 细胞的小鼠中，口服哌立福新可显着降低 MM 肿瘤的生长并提高存活率 [1, 2]。
| Cas No. | 157716-52-4 | SDF | |
| 别名 | 哌立福新; KRX-0401; NSC 639966; D21266 | ||
| 化学名 | (1,1-dimethylpiperidin-1-ium-4-yl) octadecyl phosphate | ||
| Canonical SMILES | CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C | ||
| 分子式 | C25H52NO4P | 分子量 | 461.67 |
| 溶解度 | Water : ≥ 153.33 mg/mL (332.13 mM); Ethanol : 92 mg/mL (199.28 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 | 2.166 mL | 10.8302 mL | 21.6605 mL |
| 5 mM | 0.4332 mL | 2.166 mL | 4.3321 mL |
| 10 mM | 0.2166 mL | 1.083 mL | 2.166 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。