货号:A140384 同义名: KRX-0401;NSC 639966
Perifosine is an Akt inhibitor with IC50 of 4.7 μM, targets pleckstrin homology domain of Akt.
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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 | ✔ | PI3K,PKC | 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 |
98+% | |||||||||||||||
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 | 98+% | ||||||||||||||
Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 98% | ||||||||||||||||
CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 98+% | ||||||||||||||||
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。 |
靶点 |
|
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. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
769-P | 0-40 μM | Growth Inhibition Assay | 72 h | IC50~5-10 μM | 21644050 |
769-P | 0-20 μM | Growth Inhibition Assay | 72 h | inhibits cell growth in a dose dependent manner | 21644050 |
786-0 | 0-40 μM | Growth Inhibition Assay | 72 h | IC50~5 μM | 21644050 |
786-O | 0-20 μM | Growth Inhibition Assay | 72 h | inhibits cell growth in a dose dependent manner | 21644050 |
Dose | Mice (p.o.): min = 36 mg/kg[4], max = 200 mg/kg[6] | ||||||||||||||||||
Administration | p.o. | ||||||||||||||||||
Pharmacokinetics |
|
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 << |
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 |
CAS号 | 157716-52-4 |
分子式 | C25H52NO4P |
分子量 | 461.659 |
别名 | KRX-0401;NSC 639966;NKA17;D21266 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
H2O: 100 mg/mL(216.61 mM),配合低频超声助溶 |
动物实验配方 |