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/ Akt / Perifosine/哌立福新

Perifosine/哌立福新 {[allProObj[0].p_purity_real_show]}

货号：A140384 同义名： KRX-0401; NSC 639966

Perifosine是一种Akt抑制剂，IC50为4.7 μM，其作用于Akt的Pleckstrin同源域。

Perifosine/哌立福新 化学结构 CAS号：157716-52-4
Perifosine/哌立福新 化学结构
CAS号：157716-52-4
Perifosine/哌立福新 3D分子结构
CAS号：157716-52-4
Perifosine/哌立福新 化学结构 CAS号：157716-52-4
Perifosine/哌立福新 3D分子结构 CAS号：157716-52-4
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Perifosine/哌立福新 纯度/质量文件 产品仅供科研

货号：A140384 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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产品名称 Akt ↓ Akt1 ↓ Akt2 ↓ Akt3 ↓ 其他靶点 纯度
Honokiol ✔ MEK 98%
PF-04691502 ++++

P-Akt (S473), IC50: 3.8 nM

P-Akt (T308), IC50: 7.5 nM

 		98+%
PHT-427 +

Akt, Ki: 2.7 μM

 		99%+
Deguelin ✔ PI3K 99%+
TIC10 isomer ✔ ERK 98+%
Perifosine +

Akt, IC50: 4.7 μM

 		98%
Miltefosine ✔ PKC,PI3K 98%
Triciribine +

Akt, IC50: 130 nM

 		99%+
Uprosertib +

Akt1, IC50: 180 nM

 		+

Akt2, IC50: 328 nM

 		++

Akt3, IC50: 38 nM

 		99%+
Afuresertib ++++

Akt1, Ki: 0.08 nM

 		++++

Akt2, Ki: 2 nM

 		++++

Akt3, Ki: 2.6 nM

 		99%+
Miransertib ++++

Akt1, IC50: 5 nM

 		++++

Akt2, IC50: 4.5 nM

 		++

Akt3, IC50: 16 nM

 		98+%
GSK-690693 ++++

Akt1, IC50: 2 nM

 		+++

Akt2, IC50: 13 nM

 		+++

Akt3, IC50: 9 nM

 		99%+
AT7867 ++

Akt1, IC50: 32 nM

 		++

Akt2, IC50: 17 nM

 		++

Akt3, IC50: 47 nM

 		PKA 99%+
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

 		+

Akt2, IC50: 210 nM

 		+

Akt3, IC50: 2119 nM

 		97%
MK-2206 2HCl +++

Akt1, IC50: 8 nM

 		+++

Akt2, IC50: 12 nM

 		+

Akt3, IC50: 65 nM

 		99%+
Ipatasertib ++++

Akt1, IC50: 5 nM

 		++

Akt2, IC50: 18 nM

 		+++

Akt3, IC50: 8 nM

 		99%+
AT13148 ++

Akt1, IC50: 38 nM

 		+

Akt2, IC50: 402 nM

 		++

Akt3, IC50: 50 nM

 		PKA 95%
Capivasertib ++++

Akt1, IC50: 3 nM

 		+++

Akt2, IC50: 8 nM

 		+++

Akt3, IC50: 8 nM

 		99%+
A-674563 HCl +++

Akt1, Ki: 11 nM

 		PKA 99%
CCT128930 +++

Akt2, IC50: 6 nM

 		PKA 95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Perifosine/哌立福新 生物活性

靶点

  • Akt

    Akt, IC50:4.7 μM
描述 AKT is the central node of PI3K/AKT/mTOR pathway. It has three functional domains -- a PH domain, a-helical linker domain and central kinase domain. The PH domain can interact with phospholipids produced by the actions of PI3K which serve to home AKT to the cell membrane and transfer to an active conformation[1]. Perifosine (KRX-0401) is an alkylphospholipid-kind inhibitor of AKT. It can inhibit the binding of the AKT-PH domain to artificial membranes containing 3% PI(3,4)P2 with IC50 value of ~10 μM (measured by SPR) [2]. Treatment of perifosine on concentration of 5uM can decrease level of p-AKT-S473 and p-AKT-T308 in PC-3 cells. Stimulated Akt phosphorylation by serum, insulin, IGF-I, EGF, and PDGF was strongly inhibited by 5 μM perifosine for 30 min. Treatment of perifosine (5 μM) can inhibit the membrane localization of the PH domain of Akt[3]. In vivo study shows that either oral daily (36 mg/kg/d) or weekly (250 mg/kg/week) administration of perifosine can significantly reduce MM tumor growth and increase survival compared with control group in mice[4]. Clinical trials of perifosine treatment for cancer, including a phase 3 study for colorectal cancer, have been done (see in https://clinicaltrials.gov/).
作用机制 Perifosine inhibits AKT by preventing its translocation from the cytosol to the inner leaflet of the plasma membrane.

Perifosine/哌立福新 细胞实验

Cell Line
Concentration Treated Time Description References
MM.1S cells 5 µM 3 h Perifosine augmented rapamycin-induced autophagy. Mol Cancer Ther. 2010 Apr;9(4):963-75.
TB3 cells 2.5 μM, 5 μM 6 h or 24 h Pretreatment with perifosine blocked BDNF/TrkB-induced Akt phosphorylation and inhibited BDNF's protection of TB3 cells from etoposide treatment. Cancer. 2011 Dec 1;117(23):5412-22.
TB3 cells 5 μM 6 h Pretreatment with perifosine blocked BDNF/TrkB-mediated rescue of TB3 cells from etoposide-induced cell death. Cancer. 2011 Dec 1;117(23):5412-22.
TB3 cells 2.5 μM, 5 μM 6 h, 24 h Perifosine inhibited BDNF/TrkB-induced Akt phosphorylation and blocked BDNF's protection of TB3 cells Cancer. 2011 Dec 1;117(23):5412-22.
PANC-1 1–500μM 72 h Perifosine significantly inhibited the growth of PANC-1 cells with an IC50 value of 5.1μM. J Hematol Oncol. 2017 Jan 6;10(1):9.
LPC028 1–500μM 72 h Perifosine significantly inhibited the growth of LPC028 cells and synergistically enhanced the antiproliferative activity of gemcitabine with a CI value of 0.2. J Hematol Oncol. 2017 Jan 6;10(1):9.
LPC006 1–500μM 72 h Perifosine showed weaker growth inhibition in LPC006 cells with an IC50 value of 22.5μM, and the combination with gemcitabine was antagonistic. J Hematol Oncol. 2017 Jan 6;10(1):9.
U251 cells 10 μM 30 min Inhibit AKT protein, reduce TNTs formation and mitochondrial transfer induced by nanomaterials Part Fibre Toxicol. 2024 Jan 15;21(1):1.
H460 1 µM to 20 µM 24 h To evaluate the effect of Perifosine on cell survival, the results showed that Perifosine inhibited the survival of H460 cells. Cancer Res. 2009 Dec 1;69(23):8967-76.
H157 1 µM to 20 µM 24 h To evaluate the effect of Perifosine on cell survival, the results showed that Perifosine inhibited the survival of H157 cells. Cancer Res. 2009 Dec 1;69(23):8967-76.
H358 1 µM to 20 µM 24 h To evaluate the effect of Perifosine on cell survival, the results showed that Perifosine inhibited the survival of H358 cells. Cancer Res. 2009 Dec 1;69(23):8967-76.
H226 1 µM to 20 µM 24 h To evaluate the effect of Perifosine on cell survival, the results showed that Perifosine inhibited the survival of H226 cells. Cancer Res. 2009 Dec 1;69(23):8967-76.
MM.1S cells 5 µM 2 h Perifosine inhibited Akt phosphorylation, enhancing rapamycin-induced cytotoxicity. Mol Cancer Ther. 2010 Apr;9(4):963-75.

Perifosine/哌立福新 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Radiation-induced lung injury model Not specified 250 mg/kg Once per week for 3, 7, and 14 days Suppressed the regenerative effects of Sox9-expressing cells, leading to thickened alveolar septa and aggravated pulmonary fibrosis Stem Cell Res Ther. 2021 Jul 2;12(1):381
BALB/c nude mice Osteosarcoma xenograft model Oral 36 mg/kg Once daily for 2 weeks Perifosine inhibits tumor proliferation and promotes apoptosis of osteosarcoma cells Clin Transl Med. 2021 Jun;11(6):e377
Nude mice TB3 tumor model Oral gavage 15 mg/kg Once daily for 30 days Perifosine treatment inhibited Akt phosphorylation in tumor tissues and increased the sensitivity of TB3 neuroblastoma tumors to etoposide treatment. Cancer. 2011 Dec 1;117(23):5412-22.
Nude mice TB3 tumor model Oral 15 mg/kg Once daily for 30 days Perifosine inhibited Akt phosphorylation and increased the sensitivity of TB3 tumors to etoposide Cancer. 2011 Dec 1;117(23):5412-22.
Nude mice H460 xenograft model Oral 15–10 mg/kg Once daily for 14 days To evaluate the inhibitory effect of Perifosine alone or in combination with chloroquine on H460 xenografts, the results showed that Perifosine combined with chloroquine significantly inhibited tumor growth. Cancer Res. 2009 Dec 1;69(23):8967-76.
CB-17 SCID mice Multiple myeloma mouse xenograft model Oral gavage 125 mg/kg Once weekly for 4 weeks Perifosine combined with nab-rapamycin significantly inhibited tumor growth and prolonged survival. Mol Cancer Ther. 2010 Apr;9(4):963-75.

Perifosine/哌立福新 动物研究

Dose Mice (p.o.): min = 36 mg/kg[4], max = 200 mg/kg[6]
Administration p.o.
Pharmacokinetics
Animal Nude mice[7]
Dose 40 mg/kg
Administration p.o.
Cmax 5.7 μg/ml
T1/2 137 ± 20 h
CL 0.057 l/h/kg
Tmax 22 h
AUC 698 ± 19 μg/ml·h
Vd 11.3 l/kg

Perifosine/哌立福新 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01555281 Multiple Myeloma Phase 1 Phase 2 Active, not recruiting December 2019 Italy ... 展开 >> Istituto Europeo di Oncologia IEO Milano, Italy, 20141 University of Torino Torino, Italy, 10127 Switzerland Kantonsspital Aarau Aarau, Switzerland, 5001 Kantonsspital Baden Baden, Switzerland, 5404 Istituto Oncologico Svizzera Italiana IOSI Bellinzona, Switzerland, 6500 Inselspital Bern Bern, Switzerland, 3010 Kantonsspital Graubünden Chur, Switzerland, 7000 Kantonsspital Olten Olten, Switzerland, 4600 Kantonsspital St. Gallen St. Gallen, Switzerland, 9007 Regionalspital Thun, Switzerland, 3600 UniversitätsSpital Zürich Zürich, Switzerland, 8091 收起 <<
NCT00055380 Cancer Phase 1 Completed - United States, Maryland ... 展开 >> National Institute of Dental And Craniofacial Research (NIDCR) Bethesda, Maryland, United States, 20892 收起 <<
NCT00053794 Endometrial Cancer ... 展开 >> Sarcoma 收起 << Phase 2 Completed - Canada, Alberta ... 展开 >> Tom Baker Cancer Center - Calgary Calgary, Alberta, Canada, T2N 4N2 Canada, British Columbia British Columbia Cancer Agency - Vancouver Island Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Margaret and Charles Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Cancer Care Ontario-London Regional Cancer Centre London, Ontario, Canada, N6A 4L6 Mount Sinai Hospital - Toronto Toronto, Ontario, Canada, M5G 1X5 Canada, Quebec Maisonneuve-Rosemont Hospital Montreal, Quebec, Canada, H1T 2M4 收起 <<

Perifosine/哌立福新 参考文献

[1]Keane NA, Glavey SV, et al. AKT as a therapeutic target in multiple myeloma. Expert Opin Ther Targets. 2014 Aug;18(8):897-915.

[2]Perifosine selectively inhibits binding of Akt PH domain to PtdIns(3,4)P2

[3]Kondapaka SB, Singh SS, et al. Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation. Mol Cancer Ther. 2003 Nov;2(11):1093-103.

[4]Hideshima T, Catley L, 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 May 15;107(10):4053-62. Epub 2006 Jan 17.

[5]Meuillet EJ, et al. Novel inhibitors of AKT: assessment of a different approach targeting the pleckstrin homology domain. Curr Med Chem. 2011;18(18):2727-42.

[6]Hennessy BT, Lu Y, et al. Pharmacodynamic markers of perifosine efficacy. Clin Cancer Res. 2007 Dec 15;13(24):7421-31.

[7]Vink SR, Schellens JH, et al. Tumor and normal tissue pharmacokinetics of perifosine, an oral anti-cancer alkylphospholipid. Invest New Drugs. 2005 Aug;23(4):279-86.

Perifosine/哌立福新 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.66mL

4.33mL

2.17mL

Perifosine/哌立福新 技术信息

CAS号157716-52-4
分子式C25H52NO4P
分子量 461.66
SMILES Code O=P(OC1CC[N+](C)(C)CC1)([O-])OCCCCCCCCCCCCCCCCCC
MDL No. MFCD00927554
别名 KRX-0401; NSC 639966; NKA17; D21266
运输蓝冰
InChI Key SZFPYBIJACMNJV-UHFFFAOYSA-N
Pubchem ID 148177
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

H2O: 100 mg/mL(216.61 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Perifosine | KRX-0401;NSC 639966;NKA17;D21266 | Akt | AmBeed-信号通路专用抑制剂 | Perifosine/哌立福新 纯度/质量文件 | Perifosine/哌立福新 亚型比较 | Perifosine/哌立福新 生物活性 | Perifosine/哌立福新 动物研究 | Perifosine/哌立福新 临床数据 | Perifosine/哌立福新 参考文献 | Perifosine/哌立福新 实验方案 | Perifosine/哌立福新 技术信息

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