Perifosine (KRX-0401)

Name: Perifosine (KRX-0401)
Brand: Selleck Chemicals
SKU: S1037
Rating: 5 (118 reviews)

For research use only.

Catalog No.S1037 Synonyms: NSC639966

118 publications

Perifosine (KRX-0401) Chemical Structure

Molecular Weight(MW): 461.66

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

Selleck's Perifosine (KRX-0401) has been cited by 118 publications

Cancer Cell, 2013, 23(6):839-52

PubMed: 23684459 ( click the link to review the publication )

Cell, 2012, 149(3):656-70

PubMed: 22920938 ( click the link to review the publication )

Aging (Albany NY), 2020, 18;12(10):9489-9499

PubMed: 32421688 ( click the link to review the publication )

Cancer Cell Int, 2020, 25;20:134

PubMed: 32351328 ( click the link to review the publication )

J Cell Biochem, 2020, 121(1):723-734

PubMed: 31452248 ( click the link to review the publication )

Transl Oncol, 2020, 13(2):355-364

PubMed: 31887630 ( click the link to review the publication )

Cell Stress Chaperones, 2020, 9

PubMed: 32519137 ( click the link to review the publication )

Chin J Integr Med, 2020, 10.1007

PubMed: 31903532 ( click the link to review the publication )

Dev Cell, 2019, 50(2):229-246

PubMed: 31204173 ( click the link to review the publication )

Dev Cell, 2019, 51(2):236-254

PubMed: 31543445 ( click the link to review the publication )

Cancer Lett, 2019, 447:93-104

PubMed: 30660646 ( click the link to review the publication )

J Pathol, 2019, 10.1002/path.5334

PubMed: 31397884 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31769426 ( click the link to review the publication )

Cancers (Basel), 2019, 11(10)

PubMed: 31627436 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(2):356-363

PubMed: 30446585 ( click the link to review the publication )

Front Oncol, 2019, 9:422

PubMed: 31192127 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2019, 381:114729

PubMed: 31445927 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 511(3):559-565

PubMed: 30824188 ( click the link to review the publication )

Mol Med Rep, 2019, 20(1):33-40

PubMed: 31115502 ( click the link to review the publication )

Med Sci Monit, 2019, 25:7218-7227

PubMed: 31554782 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):911

PubMed: 30185800 ( click the link to review the publication )

Cell Death Dis, 2018, 9(7):747

PubMed: 29970878 ( click the link to review the publication )

Cell Death Dis, 2018, 9(7):739

PubMed: 29970892 ( click the link to review the publication )

Front Aging Neurosci, 2018, 10:378

PubMed: 30515090 ( click the link to review the publication )
Int J Oncol, 2018, 52(3):828-840

PubMed: 29344641 ( click the link to review the publication )

Chem Res Toxicol, 2018, 31(11):1219-1229

PubMed: 30265530 ( click the link to review the publication )

Acta Biochim Biophys Sin (Shanghai), 2018, 50(8):748-756

PubMed: 29961813 ( click the link to review the publication )

BMC Neurosci, 2018, 19(1):52

PubMed: 30189852 ( click the link to review the publication )

Mol Med Rep, 2018, 18(1):447-454

PubMed: 29749519 ( click the link to review the publication )

Transl Cancer Res, 2018, 7(6):1548-1560

PubMed: 30761266 ( click the link to review the publication )

Nat Cell Biol, 2017, 19(3):238-251

PubMed: 28218907 ( click the link to review the publication )

Nat Commun, 2017, 8:14091

PubMed: 28345588 ( click the link to review the publication )

Autophagy, 2017, 13(8):1364-1385

PubMed: 28598230 ( click the link to review the publication )

Sci Rep, 2017, 7:45136

PubMed: 28332584 ( click the link to review the publication )

Am J Pathol, 2017, 187(8):1736-1749

PubMed: 28627412 ( click the link to review the publication )

Mediators Inflamm, 2017, 2017:5706152

PubMed: 29056830 ( click the link to review the publication )

PLoS One, 2017, 12(1):e0169585

PubMed: 28081222 ( click the link to review the publication )

PLoS One, 2017, 12(3):e0173473

PubMed: 28291820 ( click the link to review the publication )

Med Sci Monit, 2017, 23:5637-5649

PubMed: 29176544 ( click the link to review the publication )

Biotechnol Lett, 2017, 39(9):1343-1349

PubMed: 28597147 ( click the link to review the publication )

Oncotarget, 2017, 8(38):63911-63922

PubMed: 28969040 ( click the link to review the publication )

Sci Rep, 2017, 7:42062

PubMed: 28165023 ( click the link to review the publication )

Nat Commun, 2016, 7:11363

PubMed: 27193833 ( click the link to review the publication )

J Clin Invest, 2016, 126(4):1300-10

PubMed: 26927669 ( click the link to review the publication )

Nucleic Acids Res, 2016, 45(6):3130-3145

PubMed: 27980063 ( click the link to review the publication )

Biomed Pharmacother, 2016, 84:305-313

PubMed: 27665476 ( click the link to review the publication )

Exp Cell Res, 2016, 340(1):81-90

PubMed: 26712518 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 479(1):54-60

PubMed: 27614310 ( click the link to review the publication )
Biochem Biophys Res Commun, 2016, 473(4):1170-6

PubMed: 27073162 ( click the link to review the publication )

J Mol Neurosci, 2016, 59(4):567-78

PubMed: 27412469 ( click the link to review the publication )

Anticancer Res, 2016, 36(11):5849-5858

PubMed: 27793908 ( click the link to review the publication )

NPJ Syst Biol Appl, 2016, 2:16027

PubMed: 28725479 ( click the link to review the publication )

Tumour Biol, 2016, 37(1):1025-33

PubMed: 26269112 ( click the link to review the publication )

Biochem Pharmacol, 2015, 10.1016/j.bcp.2015.04.015

PubMed: 25934232 ( click the link to review the publication )

Sci Rep, 2015, 5:12059

PubMed: 26154270 ( click the link to review the publication )

Oncol Rep, 2015, 33(2):875-84

PubMed: 25484022 ( click the link to review the publication )

Mol Cell Biochem, 2015, 398(1-2):105-13

PubMed: 25223639 ( click the link to review the publication )

Childs Nerv Syst, 2015, 31(2):221-6

PubMed: 25269544 ( click the link to review the publication )

Childs Nerv Syst, 2015, 31(4):557-62

PubMed: 25712742 ( click the link to review the publication )

Childs Nerv Syst, 2015, 31(2):221-6

PubMed: ( click the link to review the publication )

Tumour Biol, 2015, 10.1007/s13277-015-3244-2

PubMed: 25697899 ( click the link to review the publication )

Oncoscience, 2015,

PubMed: ( click the link to review the publication )

Oncotarget, 2015, 6(9):6597-610

PubMed: 25788264 ( click the link to review the publication )

Oncoscience, 2015, 10.1155/2015/8332

PubMed: ( click the link to review the publication )

Cancer Res, 2014, 74(16):4458-69

PubMed: 24934808 ( click the link to review the publication )

Oncogene, 2014, 10.1038/onc.2014.184.

PubMed: 24998847 ( click the link to review the publication )

FASEB J, 2014, 27(7):2584-99

PubMed: 23507869 ( click the link to review the publication )

Cardiovasc Diabetol, 2014, 35(7):450-4

PubMed: 24836459 ( click the link to review the publication )

Carcinogenesis, 2014, 35(10):2232-43

PubMed: 24942865 ( click the link to review the publication )

Biochim Biophys Acta, 2014, 1843(9):1851-64

PubMed: 24769208 ( click the link to review the publication )

Antimicrob Agents Chemother, 2014, 10.1128/AAC.02798-13

PubMed: 24752266 ( click the link to review the publication )

Anal Bioanal Chem, 2014, 406(15):3743-54

PubMed: 24817345 ( click the link to review the publication )
Biochem Biophys Res Commun, 2014, 455(3-4):256-61

PubMed: 25449280 ( click the link to review the publication )

Biomed Res Int, 2014, 2014:568693

PubMed: 25309914 ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.11.002

PubMed: ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 450(1):646-51

PubMed: 24946212 ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 453(3):362-7

PubMed: 25264192 ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 452(1):72-8

PubMed: 25152399 ( click the link to review the publication )

Vet J, 2014, 201(1):83-90

PubMed: 24881508 ( click the link to review the publication )

Cell Logist, 2014, 4(1):e27732

PubMed: 24843827 ( click the link to review the publication )

Oncotarget, 2014, 5(14):5295-303

PubMed: 24979463 ( click the link to review the publication )

Rostock University, 2014, Lange F

PubMed: ( click the link to review the publication )

Clin Cancer Res, 2013, 19(19):5413-22

PubMed: 23888070 ( click the link to review the publication )

Cancer Lett, 2013, 336(2):319-24

PubMed: 23528835 ( click the link to review the publication )

Gynecol Oncol, 2013, 131(1):207-12

PubMed: 23877012 ( click the link to review the publication )

Biochim Biophys Acta, 2013, 1831(8):1322-34

PubMed: 23707264 ( click the link to review the publication )

Biochim Biophys Acta, 2013, 1828(5):1384-9

PubMed: 23376656 ( click the link to review the publication )

Sci Rep, 2013, 3:1697

PubMed: 23603888 ( click the link to review the publication )

J Biol Chem, 2013, 288(31):22836-48

PubMed: 23788636 ( click the link to review the publication )

Mol Pharmacol, 2013, 84(4):562-71

PubMed: 23877009 ( click the link to review the publication )

Biochimie, 2013, 101:50-9

PubMed: 24394624 ( click the link to review the publication )

Oncol Rep, 2013, 29(6):2422-30

PubMed: 23588929 ( click the link to review the publication )

Biochemistry, 2013, 53(3):462-72

PubMed: 24383815 ( click the link to review the publication )

Dig Dis Sci, 2013, 58(10):2873-80

PubMed: 23912246 ( click the link to review the publication )

PLoS One, 2013, 8(5):e61896

PubMed: 23658701 ( click the link to review the publication )

PLoS One, 2013, 8(8): e74420

PubMed: 24009772 ( click the link to review the publication )
PLoS One, 2013, 8(8): e70804

PubMed: 23936469 ( click the link to review the publication )

Biochem Biophys Res Commun, 2013, 443(2):447-52

PubMed: 24316214 ( click the link to review the publication )

Mol Biol Rep, 2013, 40(10):5645-55

PubMed: 24065522 ( click the link to review the publication )

Mol Med Rep, 2013, 7(2):642-8

PubMed: 23175237 ( click the link to review the publication )

Cell Biochem Biophys, 2013, 65(2):217-27

PubMed: 23015227 ( click the link to review the publication )

Cell Biochem Biophys, 2013, 66(3):737-46

PubMed: 23397419 ( click the link to review the publication )

Helsinki Metropolia University, 2013, Jens Desloovere

PubMed: ( click the link to review the publication )

Cancer Res, 2012, 72(10):2622-33

PubMed: 22461507 ( click the link to review the publication )

J Clin Endocrinol Metab, 2012, 97(2):E173-82

PubMed: 22090271 ( click the link to review the publication )

Mol Cell Proteomics, 2012, 11(12):1898-912

PubMed: 23001822 ( click the link to review the publication )

J Biol Chem, 2012, 286(43):37389-98

PubMed: 21908616 ( click the link to review the publication )

Expert Opin Inv Drugs, 2012, 21(11):1597-606

PubMed: ( click the link to review the publication )

Mol Carcinog, 2012, 52(9):667-75

PubMed: 22488590 ( click the link to review the publication )

Surgery, 2012, 152(6):1218-24

PubMed: 23158188 ( click the link to review the publication )

Cancer Biol Ther, 2012, 13(11):1009-17

PubMed: 22825337 ( click the link to review the publication )

PLoS Biol, 2011, 9(9):e1001148

PubMed: 21931533 ( click the link to review the publication )

Cancer Lett, 2011, 310(1):118-28

PubMed: 21775054 ( click the link to review the publication )

J Pharmacol Exp Ther, 2011, 336(3):866-73

PubMed: 21148684 ( click the link to review the publication )

Radiat Oncol, 2011, 6:39

PubMed: 21496273 ( click the link to review the publication )

Cancer Res, 2010, 70(22):9106-17

PubMed: 21062988 ( click the link to review the publication )

Brit J Pharmacol, 2010, 160(2):355-66

PubMed: 20423345 ( click the link to review the publication )

Cytotechnology, 2010, 62(5):449-60

PubMed: 20842425 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

Targets

Akt ^[1]
(MM.1S cells)

4.7 μM

In vitro

Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. ^[1] Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (Erk) 1/2, induces cell cycle arrest in G1 and G2, and causes dose-dependent growth inhibition of mouse glial progenitors. ^[2] Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. ^[3] A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
T24 BC	M1HDXmZ2dmO2aX;uJGF{e2G7	MmTHNE42NzFxMj61JO69VQ>?	MV2zJIg>	MoLqdoVlfWOnczD0bIUh[mG\|YXygR2IhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	NXzlXlVNOjZyOUe4O\|M>
T24 BC	M2fweWNmdGxiVnnhZoltcXS7IFHzd4F6	M{LE[VAvPS9zL{KuOUDPxE1?	NF;OW4czPCCq	NGLOdXpmdmijbnPld{B{d3KjZnXubYIucW6mdXPl[EBk\WyuII\pZYJqdGm2eTDk[YNz\WG\|ZR?=	M{HuNlI3ODl5OEez
T24 BC	NF[4UI5CeG:ydH;zbZMhSXO\|c3H5	NVT1ZXQ2Oi53IN88US=>	NVfHVXZrOjRiaB?=	NYjk[Ydpe2Wwc3n0bZpmeyCEQzDj[YxteyC2bzDzc5Ji\mWwaXKtbY5lfWOnZDDhdI9xfG:2aXRCpC=>	M3zsRVI3ODl5OEez
HepG2	NH3qcYNHfW6ldHnvckBCe3OjeR?=	NGPrWIUzOMLizszN	NUfsdmhFOjUEoHi=	MnPBdJJw\HWlZYOgZY4hcW62ZX7z[UBkgXSxcHzhd41q[yC4YXP1c4xqgmG2aX;uJINwenKnc4DvcoRqdmdidH:gZUBvd3SjYnzlJIRqdGG2YYTpc44hd2ZidHjlJGVTKGOrc4Tldo5{	MVKyOVk{PDJ\|Mh?=
U-87 MG	M4[xdGZ2dmO2aX;uJGF{e2G7	Ml3WNlDDqM7:TR?=	NX3JSW85OjUEoHi=	MkPXbY5kemWjc3XzJIRwfWKuZT3t[Y1jemGwZTDic5Vv\CC\|dIL1Z5R2emW\|	MYCyOVk{PDJ\|Mh?=
HepG2	MU\GeY5kfGmxbjDBd5NigQ>?	MX:yNOKh\|ryP	NG\iXGU3NzJ2IHi=	Mme3bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZiTFOzMWlKKGOxdILlZZRm\CC5aYToJGNS	MknjNlU6OzR{M{K=
U-87 MG	NV3PenJ{TnWwY4Tpc44hSXO\|YYm=	M1\WbVIxyqEQvF2=	MWe2M\|I1KGh?	Mnj5bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZiTFOzMWlKKGOxdILlZZRm\CC5aYToJGNS	MkL5NlU6OzR{M{K=
HepG2	NX61WXBUTnWwY4Tpc44hSXO\|YYm=	MVGyNOKh\|ryP	NGDqN\|U3NzJ2IHi=	NHPMfHll\WO{ZXHz[ZMhVEN\|LVnJJIRm\3KjZHH0bY9vyqCocn;tJFYhcA>?	MWKyOVk{PDJ\|Mh?=
U-87 MG	MkfTSpVv[3Srb36gRZN{[Xl?	M4\NR\|IxyqEQvF2=	Moq5Ok8zPCCq	NGfjTGZqdmO{ZXHz[ZMhfGinIHH1eI9xcGGpaXOg[ox2gCBiYYSgOkBpKHeqaXzlJIlvcGmkaYTzJJRpcXNiZnz1fEBifCB{NHi=	MoG4NlU6OzR{M{K=
HepG2	MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH:4cI8zOC92MDFOwG0>	MYWyOE81QCCq	M3ziXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	NVHaR4JDOjV7M{SyN\|I>
U-87 MG	M{DaO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYmyNE81OCEQvF2=	NHuyZ\|MzPC92ODDo	MlrobY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	NEP2c2EzPTl\|NEKzNi=>
A549	NISxPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml64NE4{NTFyIN88US=>	NITQVWozPC95MjDo	MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	MlrGNlU3QTd6OUm=
H460	NYfIcFNkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{PYOFAvOy1zMDFOwG0>	NVeydINvOjRxN{KgbC=>	MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	MoDlNlU3QTd6OUm=
A549	M3XIVmFxd3C2b4Ppd{BCe3O\|YYm=	NWXhc4pSOS9\|IN88US=>	NVnzRol7PDhiaB?=	M1fRZYlv\HWlZYOgZZBweHSxc3nz	Mn3zNlU3QTd6OUm=
H460	NYnyW2JXSXCxcITvd4l{KEG\|c4PhfS=>	MYexM\|Mh\|ryP	MonVOFghcA>?	NHz4dpBqdmS3Y3XzJIFxd3C2b4Ppdy=>	M4nGXlI2Pjl5OEm5
A549	MVnGeY5kfGmxbjDBd5NigQ>?	NVKwdFF{OyEQvF2=	NFfQfGI5KGh?	MnvQZoxw[2u\|IFHLWEBi[3SrdnH0bY9v	NF\MR5gzPTZ7N{i5PS=>
H460	NF7UcY1HfW6ldHnvckBCe3OjeR?=	NEj3XoY{KM7:TR?=	NFzSfVg5KGh?	MmrOZoxw[2u\|IFHLWEBi[3SrdnH0bY9v	NFjtZm4zPTZ7N{i5PS=>
A549	M1Kyb2Z2dmO2aX;uJGF{e2G7	MYqzJO69VQ>?	NYf2OWY3QCCq	M3vmfoJtd2OtczDtWG9TSzFuIHHu[EBGWktvTVHQT{Bi[3SrdnH0bY9vKGOxbXLpcoVlKHerdHigUWVMNTF4Mh?=	NInNNHozPTZ7N{i5PS=>
H460	M3TJRmZ2dmO2aX;uJGF{e2G7	NUXt[FBzOyEQvF2=	NFr1NnU5KGh?	NI\4UZhjdG:la4OgcXRQWkNzLDDhcoQhTVKNLV3BVGsh[WO2aY\heIlwdiClb33ibY5m\CC5aYToJG1GUy1zNkK=	MnjhNlU3QTd6OUm=
RMG1	M1fHe2NmdGxiVnnhZoltcXS7IFHzd4F6	MVSxMVMxKM7:TR?=	NWn1e2VXPzJiaB?=	MkTT[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	M{DJU\|I2PTF7MUS4
RMG2	NX\ES4VES2WubDDWbYFjcWyrdImgRZN{[Xl?	NFTofpcyNTNyIN88US=>	Ml7aO\|IhcA>?	NYLQfpJC\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy	MYOyOVUyQTF2OB?=
KOC7C	M3rQSGNmdGxiVnnhZoltcXS7IFHzd4F6	NFfyUJcyNTNyIN88US=>	NVWz[YN7PzJiaB?=	M13weoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?=	MX[yOVUyQTF2OB?=
HAC2	NEfvZ2tE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	MkW1NU0{OCEQvF2=	M{LaVFczKGh?	NH7QWI5l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	M{T5blI2PTF7MUS4
RMG2	NWXoepZoS2WubDDWbYFjcWyrdImgRZN{[Xl?	MkDMNU0{OCEQvF2=	MnvKOFghcA>?	NG\2RpFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	NWfXWW17OjV3MUmxOFg>
OVISE	MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MWqxMVMxKM7:TR?=	M2K3d\|Q5KGh?	M3jrUYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?=	MmfnNlU2OTlzNEi=
SKOV3	Mlf3R4VtdCCYaXHibYxqfHliQYPzZZk>	MnnvNU0{OCEQvF2=	MWC0PEBp	MVvk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	NXLPeXRpOjV3MUmxOFg>
A2780	Mn30R4VtdCCYaXHibYxqfHliQYPzZZk>	NHPXfXgyNTNyIN88US=>	MWS0PEBp	NEjrepll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	NVHXcGs6OjV3MUmxOFg>
RMG1	MVTBdI9xfG:\|aYOgRZN{e2G7	NGeyUZQ{OCEQvF2=	Ml20NlQhcA>?	NGHHUZJqdmS3Y3XzJIFxd3C2b4Ppdy=>	M4GxUFI2PTF7MUS4
RMG2	M3X1fmFxd3C2b4Ppd{BCe3O\|YYm=	M1XtZ\|MxKM7:TR?=	NFv1b4EzPCCq	M3fkUolv\HWlZYOgZZBweHSxc3nz	MkHoNlU2OTlzNEi=
HCC1806	NVXlUWl1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MU[wMVExKM7:TR?=	NGfsVnc1QCCq	NVPEfndzTUN3ME2yMlg16oDLwsJihKkxNjB5IN88US=>	MmrPNlUzQTN3N{[=
MDA-MB-231	NFy3UGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUCwMVExKM7:TR?=	NYm2TI9UPDhiaB?=	MmS1SWM2OD1zLkGz5qCKyrIkgJmwMlA4KM7:TR?=	M1v1RlI2Ojl\|NUe2
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PANC-1	MX\GeY5kfGmxbjDBd5NigQ>?	NGfhepgxNjVizszN	NGPkNnEzPCCq	MljtbY5pcWKrdIOgRYt1NCCVNluxMEBidmRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvcuKh	MYiyOFUyQTd3MR?=
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A2780CP	NGT2Om1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVm1d5Q3UUN3ME23MlYh\|ryP	MlG4NlM5PzdyMUK=
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Kasumi-1	NFrjWJNE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NX\jTo5POC1{MDFOwG0>	MYOyOE81QCCq	NHHHXnNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[m:2aDDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI>	NHLwfoMzOjRyN{KyPC=>
HL-60	NVzvRpRwS2WubDDWbYFjcWyrdImgRZN{[Xl?	MnX1NE0zOCEQvF2=	NHfVe3UzPC92ODDo	M2HubIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=>	MXSyNlQxPzJ{OB?=
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HL-60	MofuRZBweHSxc3nzJGF{e3OjeR?=	NEPoVJUyOCEQvF2=	MVOyOEBp	NU\rWXN2cW6mdXPld{BieG:ydH;zbZM>	MXeyNlQxPzJ{OB?=
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HL-60	NWLKN4xXTnWwY4Tpc44hSXO\|YYm=	NF\Sd3UzNjVxNT:xNEDPxE1?	NIjkXIQzPCCq	MorD[IVkemWjc3XzJGFsfCCjbnSgdE1Cc3RibHX2[Yx{yqCmb4PlMYRmeGWwZHXueIx6	M{TBRlIzPDB5MkK4
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HepG2	MkfLRZBweHSxc3nzJGF{e3OjeR?=	NHvLOIs2NzFyL{KwJO69VQ>?	NEfG[Y4zPC92ODDo	NXG1SHRlcW6mdXPld{BieG:ydH;zbZMh[XRidHjlJIxwdmdvdHnt[UBmgHCxc4Xy[S=>	M3Oyb\|IxQDR{NEK1
Bel-7402	NXr4WYdTSXCxcITvd4l{KEG\|c4PhfS=>	M4O0cVUwOTBxMkCg{txO	NXfQbmRLOjRxNEigbC=>	NG\UNoxqdmS3Y3XzJIFxd3C2b4Ppd{BifCC2aHWgcI9v\y22aX3lJIV5eG:\|dYLl	M1XsPVIxQDR{NEK1
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MAVER	MlWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnvFNk0yOMLizszN	MoXmOFjDqGh?	M{W2PIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz	NIrtcG8zODF\|MEm2NC=>
BJAB	M{LPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoL6Nk0yOMLizszN	MVO0POKhcA>?	NFXh[ndqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	MYKyNFE{ODl4MB?=
OCI	MmS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFzZN3YzNTFywrFOwG0>	MmO1OFjDqGh?	MlnrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI>	MkTTNlAyOzB7NkC=
MOLM	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4TJZVIuOTEEoN88US=>	M1y5RlQ5yqCq	NU\sVmE6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	MWKyNFE{ODl4MB?=
HL-60	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlfINk0yOMLizszN	M1nXTFQ5yqCq	MYLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=>	Mn3SNlAyOzB7NkC=
SKW6.4	NFfuc3RCeG:ydH;zbZMhSXO\|c3H5	MVixNOKh\|ryP	NWH4[VY4OjRxNEigbC=>	MkfzbY5lfWOnczDhdI9xfG:\|aYOgeIlu\S2mZYDlcoRmdnSueR?=	M{i2NVIxOTNyOU[w
MAVER	MWDBdI9xfG:\|aYOgRZN{e2G7	MXmxNOKh\|ryP	NEnpO2UzPC92ODDo	NFHJNJhqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nLXTldIVv\GWwdHz5	MnrNNlAyOzB7NkC=
BJAB	MkDYRZBweHSxc3nzJGF{e3OjeR?=	NXnrW5BXOTEEoN88US=>	NVX2WHZiOjRxNEigbC=>	MULpcoR2[2W\|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7	M{nzNlIxOTNyOU[w
OCI	MWTBdI9xfG:\|aYOgRZN{e2G7	M3HpSFExyqEQvF2=	MU[yOE81QCCq	MUnpcoR2[2W\|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7	M4f3PVIxOTNyOU[w
MOLM	NGDHR2hCeG:ydH;zbZMhSXO\|c3H5	NVPh[FQxOTEEoN88US=>	MVGyOE81QCCq	MVzpcoR2[2W\|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7	MYiyNFE{ODl4MB?=
HL-60	NXy0XY9uSXCxcITvd4l{KEG\|c4PhfS=>	M3XmcFExyqEQvF2=	NEDvfI4zPC92ODDo	NXeyXpNrcW6mdXPld{BieG:ydH;zbZMhfGmvZT3k[ZBmdmSnboTsfS=>	M124O\|IxOTNyOU[w

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT / AKT / p-S6K1 / S6K1 ; PubMed: 25519148 Mol Cancer Res The effect of perifosine on AKT-mTOR activation in vitro. RMG1 and RMG2 cells were treated with 0, 3, 10, 30 or 50 μM perifosine for 6 h in the presence of 10% FBS. Cells were harvested, and equivalent amounts (30 μg) of protein were subjected to SDS-PAGE and blotted with anti-phospho-AKT (Ser473), anti-AKT, anti-phospho-S6K1 (Thr389), anti-S6K1, or anti-β-actin antibodies. PARP; PubMed: 25519148 Mol Cancer Res Perifosine induces apoptosis. RMG1 and RMG2 cells were treated with or without 30 μM perifosine for 24 h. Cells were harvested, and the effect of perifosine was evaluated by western blotting p-mTOR / mTOR / Raptor / Rictor / p-p70S6K / p70S6K / p-4EBP1 / 4EBP1 / c-Myc / Cyclin D1; PubMed: 19920197 Cancer Res The indicated cell lines were treated with the given concentrations of perifosine (PRFS) for 8 h. p-PDK1 / p-GSK3α/β / p-S6R ; PubMed: 17761832 Blood BCWM.1 cells were cultured with perifosine for 6 hours with doses that ranged from 2 to 20 μM. Whole cell lysates were subjecting to Western blotting using anti–p-Akt ser473, -Akt, –p-PDK1, –p-GSK3α/β, –p-S6R, and α-tubulin antibodies.	25519148 19920197 17761832
Growth inhibition assay	Cell viability; PubMed: 28332584 Sci Rep Cell survival measured by MTT assay and IC50 of perifosine in a panel of eleven human cancer cells.	28332584

In vivo

Perifosine combining with temozolomide reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. ^[2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. ^[3] Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. ^[5]

Protocol

Kinase Assay:^[3]	- Collapse Akt kinase assay: MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit.
Cell Research:^[2]	- Collapse Cell lines: Human glioma cell lines Concentrations: 0, 15, 30 and 45 μM Incubation Time: 48 hours Method: Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader. (Only for Reference)
Animal Research:^[3]	- Collapse Animal Models: MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old). Dosages: 250 mg/kg/wk or 36 mg/kg/d Administration: Oral gavage (Only for Reference)

References

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Solubility (25°C)

In vitro	Ethanol	15 mg/mL (32.49 mM)
	Water	8 mg/mL (17.32 mM)
	DMSO	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): water For best results, use promptly after mixing.	8mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Perifosine (KRX-0401) SDF

Molecular Weight	461.66
Formula	C₂₅H₅₂NO₄P
CAS No.	157716-52-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NSC639966
Smiles	CCCCCCCCCCCCCCCCCCO[P]([O-])(=O)OC1CC[N+](C)(C)CC1

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01224730	Completed	Drug: perifosine	Cancer	AEterna Zentaris	January 24 2012	Phase 1
NCT01049841	Completed	Drug: perifosine + temsirolimus	Pediatric Solid Tumors	Memorial Sloan Kettering Cancer Center\|University of Wisconsin Madison\|Duke University\|NATL COMP CA NETWORK\|Pfizer\|AEterna Zentaris	January 2010	Phase 1
NCT01048580	Completed	Drug: Perifosine\|Drug: Capecitabine	Colon Cancer	AEterna Zentaris\|SCRI Development Innovations LLC	October 2009	Phase 1
NCT00776867	Completed	Drug: perifosine	Solid Tumors	Memorial Sloan Kettering Cancer Center\|University of Wisconsin Madison\|Duke University\|AEterna Zentaris	October 2008	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

Selective Akt Inhibitor

CCT128930 : AKT2-selective, IC50=6 nM.
Most Potent Akt Inhibitor

AZD5363 : Akt1, IC50=3 nM; Akt2, IC50=8 nM; Akt3, IC50=8 nM.
Akt Inhibitor in Clinical Trial

Ipatasertib (GDC-0068) : Phase II for Prostate Cancer and Gastric Cancer.
Newest Akt Inhibitor

AZD5363 : Potent inhibitor of all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2.

Related Akt Products

Afuresertib (GSK2110183) ^New

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.
AT13148 ^New

AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
SC79 ^New

SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.
MK-2206 2HCl

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.
Capivasertib (AZD5363)

AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.

Features:Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.
Ipatasertib (GDC-0068)

Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.
GSK690693

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
A-674563

A-674563 is an Akt1 inhibitor with K_i of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.

Features:Orally bioavailable compound (achieved by replacing indole of A-443654 with phenyl moiety) and somewhat less selective for Akt over PKA than A-443654.
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Honokiol

Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.

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Perifosine (KRX-0401)