Structure of Perifosine
CAS No.: 157716-52-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Perifosine is an Akt inhibitor with IC50 of 4.7 μM, targets pleckstrin homology domain of Akt.
Synonyms: KRX-0401; NSC 639966; NKA17
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CAS No. : | 157716-52-4 |
Formula : | C25H52NO4P |
M.W : | 461.66 |
SMILES Code : | O=P(OC1CC[N+](C)(C)CC1)([O-])OCCCCCCCCCCCCCCCCCC |
Synonyms : |
KRX-0401; NSC 639966; NKA17
|
InChI Key : | SZFPYBIJACMNJV-UHFFFAOYSA-N |
Pubchem ID : | 148177 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Concentration | Treated Time | Description | References |
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. | PMC3158972 |
TB3 cells | 5 μM | 6 h | Pretreatment with perifosine blocked BDNF/TrkB-mediated rescue of TB3 cells from etoposide-induced cell death. | PMC3158972 |
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 | PMC3158972 |
PANC-1 | 1–500μM | 72 h | Perifosine significantly inhibited the growth of PANC-1 cells with an IC50 value of 5.1μM. | PMC5219723 |
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. | PMC5219723 |
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. | PMC5219723 |
U251 cells | 10 μM | 30 min | Inhibit AKT protein, reduce TNTs formation and mitochondrial transfer induced by nanomaterials | PMC10789074 |
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. | PMC2789206 |
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. | PMC2789206 |
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. | PMC2789206 |
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. | PMC2789206 |
MM.1S cells | 5 µM | 2 h | Perifosine inhibited Akt phosphorylation, enhancing rapamycin-induced cytotoxicity. | PMC3096071 |
MM.1S cells | 5 µM | 3 h | Perifosine augmented rapamycin-induced autophagy. | PMC3096071 |
In Vivo:
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 | PMC8254240 |
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 | PMC8214859 |
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. | PMC3158972 |
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 | PMC3158972 |
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. | PMC2789206 |
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. | PMC3096071 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT01555281 | Multiple Myeloma | Phase 1 Phase 2 | Active, not recruiting | December 2019 | Italy ... More >> 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 Less << |
NCT00055380 | Cancer | Phase 1 | Completed | - | United States, Maryland ... More >> National Institute of Dental And Craniofacial Research (NIDCR) Bethesda, Maryland, United States, 20892 Less << |
NCT00053794 | Endometrial Cancer ... More >> Sarcoma Less << | Phase 2 | Completed | - | Canada, Alberta ... More >> 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 Less << |
NCT00053781 | Melanoma (Skin) | Phase 2 | Completed | - | Canada, Alberta ... More >> Tom Baker Cancer Center - Calgary Calgary, Alberta, Canada, T2N 4N2 Canada, Nova Scotia Nova Scotia Cancer Centre Halifax, Nova Scotia, Canada, B3H 1V7 Canada, Ontario Cancer Care Ontario-London Regional Cancer Centre London, Ontario, Canada, N6A 4L6 Princess Margaret Hospital at University Health Network Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Centre Hospitalier de l'Universite de Montreal Montreal, Quebec, Canada, H2L-4M1 McGill University Montreal, Quebec, Canada, H2W 1S6 Less << |
NCT00019656 | Leukemia Lymp... More >>homa Myelodysplastic Syndromes Myelodysplastic/Myeloproliferative Neoplasms Unspecified Adult Solid Tumor, Protocol Specific Less << | Phase 1 | Completed | - | United States, Maryland ... More >> Warren Grant Magnuson Clinical Center - NCI Clinical Studies Support Bethesda, Maryland, United States, 20892-1182 NCI - Center for Cancer Research Bethesda, Maryland, United States, 20892 Less << |
NCT00054145 | Breast Cancer | Phase 2 | Completed | - | Canada, Ontario ... More >> Margaret and Charles Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Cancer Care Ontario-London Regional Cancer Centre London, Ontario, Canada, N6A 4L6 Ottawa Regional Cancer Centre Ottawa, Ontario, Canada, K1H 1C4 Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less << |
NCT00060437 | Prostate Cancer | Phase 2 | Completed | - | United States, Maryland ... More >> Warren Grant Magnuson Clinical Center - NCI Clinical Studies Support Bethesda, Maryland, United States, 20892-1182 Less << |
NCT00005794 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, Wisconsin ... More >> University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792-6164 Less << |
NCT00053924 | Pancreatic Cancer | Phase 2 | Completed | - | Canada, Ontario ... More >> Margaret and Charles Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Cancer Care Ontario-London Regional Cancer Centre London, Ontario, Canada, N6A 4L6 Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less << |
NCT00064324 | Recurrent Adult Soft Tissue Sa... More >>rcoma Stage III Adult Soft Tissue Sarcoma Stage IV Adult Soft Tissue Sarcoma Less << | Phase 2 | Completed | - | United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less << |
NCT00431054 | Ovarian Cancer | Phase 1 | Completed | - | United States, Texas ... More >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT01097018 | Colorectal Cancer | Phase 3 | Completed | - | - |
NCT00399126 | Neoplasms | Phase 1 | Completed | - | United States, Tennessee ... More >> AOI Pharmaceuticals Investigative Site Johnson City, Tennessee, United States, 37604 Less << |
NCT00399087 | Neoplasms | Phase 1 | Completed | - | United States, Tennessee ... More >> Investigative Site Johnson City, Tennessee, United States, 37604 Less << |
NCT00062387 | Head and Neck Cancer | Phase 2 | Terminated(Administratively co... More >>mplete.) Less << | - | United States, Illinois ... More >> University of Chicago Cancer Research Center Chicago, Illinois, United States, 60637-1470 Decatur Memorial Hospital Cancer Care Institute Decatur, Illinois, United States, 62526 Evanston Northwestern Health Care - Evanston Hospital Evanston, Illinois, United States, 60201-1781 Ingalls Memorial Hospital Harvey, Illinois, United States, 60426 LaGrange Memorial Hospital LaGrange, Illinois, United States, 60525 Cardinal Bernardin Cancer Center at Loyola University Medical Center Maywood, Illinois, United States, 60153 Oncology/Hematology Associates of Central Illinois, P.C. Peoria, Illinois, United States, 61602 Central Illinois Hematology Oncology Center Springfield, Illinois, United States, 62701 United States, Indiana Fort Wayne Medical Oncology and Hematology, Incorporated Fort Wayne, Indiana, United States, 46885-5099 CCOP - Northern Indiana CR Consortium South Bend, Indiana, United States, 46601 United States, Michigan Oncology Care Associates, P.L.L.C. Saint Joseph, Michigan, United States, 49085 United States, Wisconsin Medical College of Wisconsin Cancer Center Milwaukee, Wisconsin, United States, 53226 Less << |
NCT00301938 | Accelerated Phase Chronic Myel... More >>ogenous Leukemia Adult Acute Megakaryoblastic Leukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(15;17)(q22;q12) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Acute Promyelocytic Leukemia (M3) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Blastic Phase Chronic Myelogenous Leukemia Myelodysplastic/Myeloproliferative Neoplasms Previously Treated Myelodysplastic Syndromes Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Relapsing Chronic Myelogenous Leukemia Secondary Acute Myeloid Leukemia T-cell Adult Acute Lymphoblastic Leukemia Untreated Adult Acute Lymphoblastic Leukemia Untreated Adult Acute Myeloid Leukemia Less << | Phase 1 | Completed | - | United States, Maryland ... More >> University of Maryland Greenebaum Cancer Center Baltimore, Maryland, United States, 21201-1595 Less << |
NCT00415064 | Multiple Myeloma | Phase 1 | Completed | - | United States, Michigan ... More >> Ann Arbor, Michigan, United States, 48109 Less << |
NCT00398697 | Neoplasms | Phase 1 | Completed | - | United States, Tennessee ... More >> Johnson City, Tennessee, United States, 37604 Less << |
NCT02238496 | Brain Tumor, Recurrent ... More >> Glioblastoma Anaplastic Astrocytoma Anaplastic Oligodendroglioma Mixed Glioma Less << | Phase 2 | Unknown | December 2016 | United States, New York ... More >> Columbia University Medical Center New York City, New York, United States, 10032 Memorial Sloan-Kettering Cancer Center New York City, New York, United States, 10065 Less << |
NCT00059982 | Pancreatic Cancer | Phase 2 | Completed | - | United States, Illinois ... More >> CCOP - Carle Cancer Center Urbana, Illinois, United States, 61801 United States, Indiana CCOP - Northern Indiana CR Consortium South Bend, Indiana, United States, 46601 United States, Iowa CCOP - Iowa Oncology Research Association Des Moines, Iowa, United States, 50309-1016 United States, Massachusetts Tufts - New England Medical Center Boston, Massachusetts, United States, 02111 United States, Minnesota CCOP - Duluth Duluth, Minnesota, United States, 55805 Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 CCOP - Metro-Minnesota Saint Louis Park, Minnesota, United States, 55416 United States, New York MBCCOP-Our Lady of Mercy Cancer Center Bronx, New York, United States, 10466 United States, North Dakota CCOP - Merit Care Hospital Fargo, North Dakota, United States, 58122 United States, Texas CCOP - Scott and White Hospital Temple, Texas, United States, 76508 Less << |
NCT00399152 | Renal Cancer ... More >>GIST Less << | Phase 1 | Completed | - | - |
NCT00398814 | Renal Cancer ... More >>Tumors Less << | Phase 1 | Completed | - | - |
NCT00058214 | Adenocarcinoma of the Prostate... More >> Recurrent Prostate Cancer Stage IIB Prostate Cancer Stage III Prostate Cancer Stage IV Prostate Cancer Less << | Phase 2 | Terminated(Did not meet interi... More >>m stopping criteria for continuation to the second stage.) Less << | - | United States, California ... More >> UC Davis Cancer Center Sacramento, California, United States, 95817 Less << |
NCT00401388 | Chondrosarcomas ... More >> Alveolar Soft Part Sarcomas Extra Skeletal Myxoid Chondrosarcomas Less << | Phase 2 | Completed | - | - |
NCT00422656 | Waldenstrom's Macroglobulinemi... More >>a Less << | PHASE2 | COMPLETED | 2025-11-12 | Dana-Farber Cancer Institute, ... More >>Boston, Massachusetts, 02115, United States Less << |
NCT00422656 | Waldenstrom's Macroglobulinemi... More >>a Less << | PHASE2 | COMPLETED | 2025-11-12 | Dana-Farber Cancer Institute, ... More >>Boston, Massachusetts, 02115, United States Less << |
NCT01051557 | - | Terminated | - | - | |
NCT00399789 | Non Small Cell Lung Cancer | PHASE1|PHASE2 | COMPLETED | 2025-12-11 | AOI Pharmaceuticals Investigat... More >>ive Site, Tucson, Arizona, 85704, United States|AOI Pharmaceuticals Investigative Site, Pomona, California, 91767, United States|AOI Pharmaceuticals Investigative Site, Aventura, Florida, 33180, United States|AOI Pharmaceuticals Investigative Site, Hollywood, Florida, 33021, United States|AOI Pharmaceuticals Investigative Site, Lakeland, Florida, 33805, United States|AOI Pharmaceuticals Investigative Site, Ormond Beach, Florida, 32174, United States|AOI Pharmaceuticals Investigative Site, Lawrenceville, Georgia, 30045, United States|AOI Pharmaceuticals Investigative Site, Galesburg, Illinois, 61401, United States|AOI Pharmaceuticals Investigative Site, New Albany, Indiana, 47150, United States|AOI Pharmaceuticals Investigative Site, Grand Rapids, Michigan, 49546, United States|AOI Pharmaceuticals Investigative Site, Kalamazoo, Michigan, 49048, United States|AOI Pharmaceuticals Investigative Site, Billings, Montana, 59101, United States|AOI Pharmaceuticals Investigative Site, Albuquerque, New Mexico, 87109, United States|AOI Pharmaceuticals Investigative Site, Albany, New York, 12208, United States|AOI Pharmaceuticals Investigative Site, Armonk, New York, 10504, United States|AOI Pharmaceuticals Investigative Site, Greenville, South Carolina, 29605, United States|AOI Pharmaceuticals Investigative Site, Chattanooga, Tennessee, 37404, United States|AOI Pharmaceuticals Investigative Site, Nashville, Tennessee, 37203, United States|AOI Pharmaceuticals Investigative Site, Dallas, Texas, 75237, United States|AOI Pharmaceuticals Investigative Site, Dallas, Texas, 75246, United States|AOI Pharmaceuticals Investigative Site, Tyler, Texas, 75702, United States Less << |
NCT01051557 | Adult Anaplastic Astrocytoma ... More >> Adult Anaplastic Oligodendroglioma Adult Diffuse Astrocytoma Adult Giant Cell Glioblastoma Adult Glioblastoma Adult Gliosarcoma Adult Mixed Glioma Adult Oligodendroglioma Recurrent Adult Brain Neoplasm Less << | Phase 1 Phase 2 | Terminated | - | United States, New Jersey ... More >> Memorial Sloan Kettering Basking Ridge Basking Ridge, New Jersey, United States, 07920 United States, New York Memorial Sloan Kettering Commack Commack, New York, United States, 11725 Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00058214 | - | Terminated(Did not meet interi... More >>m stopping criteria for continuation to the second stage.) Less << | - | - | |
NCT00401011 | Multiple Myeloma ... More >> Multiple Myeloma in Relapse Less << | Phase 1 Phase 2 | Completed | - | - |
NCT00391560 | Leukemia | Phase 2 | Completed | - | - |
NCT00398879 | Colon Cancer | Phase 2 | Completed | - | - |
NCT00398710 | Waldenstr?m's Macroglobulinemi... More >>a Less << | PHASE2 | COMPLETED | 2025-10-11 | Dana-Farber Cancer Institute, ... More >>Boston, Massachusetts, 02115, United States Less << |
NCT00776867 | Solid Tumors | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00498966 | Kidney Cancer | PHASE2 | COMPLETED | 2025-10-11 | Investigative Site, Louisville... More >>, Kentucky, 40202, United States|Investigative Site, Morristown, New Jersey, 07962, United States|Investigative Site, Armonk, New York, 10504, United States Less << |
NCT00847366 | Non Small Cell Lung Cancer ... More >> Solid Tumors Metastatic Breast Cancer Sarcomas Less << | Not Applicable | Completed | - | - |
NCT01002248 | Multiple Myeloma | Phase 3 | Terminated | - | - |
NCT00455559 | Gastrointestinal Stromal Tumor... More >>s Less << | Phase 2 | Completed | - | - |
NCT00448721 | Renal Cell Carcinoma | PHASE2 | COMPLETED | 2025-10-11 | Investigative Site, Duarte, Ca... More >>lifornia, 91010, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Investigative Site, Philadelphia, Pennsylvania, 19104, United States|Investigative Site, Nashville, Tennessee, 37232, United States Less << |
NCT00375791 | Multiple Myeloma | Phase 2 | Completed | - | United States, California ... More >> Investigative Site Berkeley, California, United States, 94704 Investigative Site Duarte, California, United States, 91010 United States, Georgia Investigative Site Atlanta, Georgia, United States, 30322 United States, Illinois Investigative Site Chicago, Illinois, United States, 60611 United States, Massachusetts Investigative Site Boston, Massachusetts, United States, 02115 United States, Michigan Investigative Site Ann Arbor, Michigan, United States, 48103 United States, Virginia Investigative Site Charlottesville, Virginia, United States, 22908 Less << |
NCT00873457 | Chronic Lymphocytic Leukemia ... More >> Small Lymphocytic Lymphoma Less << | Phase 2 | Completed | - | United States, North Carolina ... More >> Duke University Medical Center Durham, North Carolina, United States, 27710 Less << |
NCT00389077 | Tumors|Lymphomas | PHASE2 | COMPLETED | 2025-09-11 | - |
NCT00873457 | - | Completed | - | - | |
NCT01224730 | Cancer | Phase 1 | Completed | - | United States, Texas ... More >> Dallas, Texas, United States, 75230 Houston, Texas, United States, 77030 Less << |
NCT01048580 | Colon Cancer | Phase 1 | Completed | - | - |
NCT00590954 | Malignant Gliomas|CNS|Brain Ca... More >>ncer|Cancer Less << | PHASE2 | COMPLETED | 2019-11-11 | Memorial Sloan-Kettering Cance... More >>r Center, New York, New York, 10065, United States Less << |
NCT01049841 | Pediatric Solid Tumors | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
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 |