4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt
Perifosine (KRX-0401)
CAS: 157716-52-4
Molecular Formula: C25H52NO4P
4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt - Names and Identifiers
4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt - Physico-chemical Properties
| Molecular Formula | C25H52NO4P |
| Molar Mass | 461.663 |
| Melting Point | 271-272° (dec) |
| Solubility | DMSO <1 mg/mL (<1 mM); Water 8 mg/mL (17.32 mM); Ethanol 15 mg/mL (32.49 mM) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| Use | An alkylphospholipid which inhibits Akt activation and the anti-apoptotic MAPK pathway. |
| In vitro study | Perifosine inhibits proliferation of immortalized keratinocytes (HaCaT cells) and head and neck squamous carcinoma cells with an IC50 of 0.6-8.9 μm. Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK)1/2, inducing cell cycle arrest in G1 and G2, and induced dose-dependent growth inhibition of glial progenitor cells in mice. Perifosine (10 μm) completely inhibited phosphorylation of Akt in MM.1S cells. A recent study showed that Perifosine induces cell cycle arrest and apoptosis in human hepatoma cells by blocking the phosphorylation of Akt. Perifosine inhibits proliferation of immortalized keratinocytes (HaCaT cells) and head and neck squamous carcinoma cells with an IC50 of 0.6-8.9 μm. Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK)1/2, inducing cell cycle arrest in G1 and G2, and induced dose-dependent growth inhibition of glial progenitor cells in mice. Perifosine (10 μm) completely inhibited phosphorylation of Akt in MM.1S cells. A recent study showed that Perifosine induces cell cycle arrest and apoptosis in human hepatoma cells by blocking the phosphorylation of Akt. |
| In vivo study | The combination of Perifosine and temozolomide reduces tumor proliferation in vivo (PDGF drives glioma development). The results suggest that Perifosine is an effective drug for inhibiting glioma and may be a candidate for the treatment of glioma in which Akt and the Ras-ERK1/2 pathway are frequently activated. Daily and weekly doses of Perifosine significantly reduced the growth of human MM tumors and improved survival compared to PBS-treated control animals. Perifosine induces thrombocytopenia and leukocytosis, increases bone marrow and spleen of myeloid mice, and it causes apoptosis in transplanted myeloma. The combination of Perifosine and temozolomide reduces tumor proliferation in vivo (PDGF drives glioma development). The results suggest that Perifosine is an effective drug for inhibiting glioma and may be a candidate for the treatment of glioma in which Akt and the Ras-ERK1/2 pathway are frequently activated. Daily and weekly doses of Perifosine significantly reduced the growth of human MM tumors and improved survival compared to PBS-treated control animals. Perifosine induces thrombocytopenia and leukocytosis, increases bone marrow and spleen of myeloid mice, and it causes apoptosis in transplanted myeloma. |
4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt - Risk and Safety
| WGK Germany | 3 |
4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt - Introduction
Perifosine (KRX-0401) is a new Akt inhibitor with IC50 of 4.7 μM, which targets the pleckstrin homology (PH) region of Akt. Phase 3.
Last Update：2022-10-16 17:41:28
4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt - Reference Information
| biological activity | Perifosine (KRX-0401) is a new type of Akt inhibitor with IC50 of 4.7 μM, targeting the pleckstrin homology (PH) region of Akt. Phase 3. Perifosine (KRX-0401, NSC639966, D21266) is a new Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targeting the pleckstrin homology domain of Akt. Phase 3. |
| in vitro study | Perifosine inhibit the proliferation of immortalized keratinocytes (HaCaT cells) and head and neck squamous cancer cells, IC50 is 0.6-8.9 μM. Perifosine tried to reduce the phosphorylation level of Akt and extracellular signal-regulated kinase (ERK)1/2, induced cell cycle arrest in G1 and G2, and induced dose-dependent growth inhibition of glial progenitor cells in mice. Perifosine (10 μM) completely inhibited the phosphorylation of Akt in MM.1S cells. A recent study showed that Perifosine induces cell cycle arrest and apoptosis in human liver cancer cells by blocking Akt phosphorylation. Perifosine inhibits the proliferation of immortalized keratinocytes (HaCaT cells) and head and neck squamous cancer cells with IC50 of 0.6-8.9 μM. Perifosine tried to reduce the phosphorylation level of Akt and extracellular signal-regulated kinase (ERK)1/2, induced cell cycle arrest in G1 and G2, and induced dose-dependent growth inhibition of glial progenitor cells in mice. Perifosine (10 μM) completely inhibited the phosphorylation of Akt in MM.1S cells. A recent study showed that Perifosine induces cell cycle arrest and apoptosis in human liver cancer cells by blocking Akt phosphorylation. |
| in vivo research | the combination of Perifosine and temozolomide can reduce tumor proliferation in vivo (PDGF drives glioma). The results show that Perifosine is an effective drug to inhibit glioma and may be a candidate drug for the treatment of glioma. Akt and Ras-ERK1/2 pathways in glioma are often activated. Compared with PBS-treated control animals, daily and weekly Perifosine significantly reduced the growth of human MM tumors and improved the survival rate. Perifosine induces platelets and leukocytosis, increases bone marrow and spleen of myeloid mice, and it will lead to apoptosis of transplanted myeloma. the combination of Perifosine and temozolomide can reduce tumor proliferation in vivo (PDGF drives glioma). The results show that Perifosine is an effective drug to inhibit glioma and may be a candidate drug for the treatment of glioma. Akt and Ras-ERK1/2 pathways in glioma are often activated. Compared with PBS-treated control animals, daily and weekly Perifosine significantly reduced the growth of human MM tumors and improved the survival rate. Perifosine induces platelets and leukocytosis, increases bone marrow and spleen of myeloid mice, and it will lead to apoptosis of transplanted myeloma. |
| target | TargetValue Akt (MM.1S cells) 4.7 μM |
| Target | Value |
| Akt (MM.1S cells) | 4.7 μM |
Last Update：2024-04-09 21:00:56
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Product Name: Perifosine (KRX-0401) Visit Supplier Webpage Request for quotationCAS: 157716-52-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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