LY294002

LY294002は初めての周知されたPI3Kα/δ/βを抑制する小分子で、無細胞試験でIC50値が0.5 μM/0.57 μM/0.97 μM に分かれることですが、溶液にの状態はWortmanninにの状態よりもっと安定になりって、自食体の形成も遮断できます。

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LY294002 化学構造
分子量: 307.34

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製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • LY294002のメカニズム

製品の説明

生物活性

製品説明 LY294002は初めての周知されたPI3Kα/δ/βを抑制する小分子で、無細胞試験でIC50値が0.5 μM/0.57 μM/0.97 μM に分かれることですが、溶液にの状態はWortmanninにの状態よりもっと安定になりって、自食体の形成も遮断できます。
ターゲット p110α p110δ p110β
IC50 0.5 μM 0.57 μM 0.97 μM[1]
In vitro試験 LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MDA-MB-231 cells Ml\3R4VtdCCrbo\hd4lwdiCjc4PhfS=> M{ewUVI1KGh? M4j0UmlvcGmkaYTpc44hd2ZiZYDpeIhmdGmjbDDndo94fGhiZnHjeI9zNWmwZIXj[YQh[2WubDDtbYdz[XSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCyOEBpenNiYomgZ4VtdCCrbo\hd4lwdiCjc4PhfUwhUUN3ME2wMlM5KM7:TT6= MYeyNlgxPDFyOB?=
Sf21 cells MmGwSpVv[3Srb36gZZN{[Xl? Mn6xTY5pcWKrdHnvckBw\iCvb4Xz[UB4cWymIIT5dIUhWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lIyKGOnbHzzJINwNWW6cILld5NqdmdiTj30[ZJucW6jbDDIbZMufGGpZ3XkJIh2dWGwIIC4OYEhfXOrbnegUE1idHCqYT3wbI9{eGijdHnkfYxqdm:|aYTvcEB{fWK|dILheIUh[nliVFzDJIJie2WmIIDoc5NxcG:{IHntZYdqdmduIFnDOVA:OC53IN88US=> M3jtSFIzPTJyNkOw
Sf21 cells NHLuTFVHfW6ldHnvckBie3OjeR?= NWXFRXVYUW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDQTVNM[WyyaHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmNlEh[2WubIOsJGlEPTB;MD61JO69VS5? NYHV[3JoOTl5NEiyOlk>
Sf9 cells Mn3lSox2d3Knc3PlcpQheG:uYYLpfoF1cW:wIHHzd4F6 M3rVWGlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxRTBwNUWg{txONg>? MYeyNVEzOTZ|MR?=
THP1 cells NVHB[HN4TnWwY4Tpc44h[XO|YYm= M334WmlvcGmkaYTpc44hd2ZiU1PGNU1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJHRJWDFiY3XscJMtKEmFNUC9NU4xOSEQvF2u NF\WbWgyPjd6OUe0Ni=>
human PC3 cells NHjGOHRHfW6ldHnvckBie3OjeR?= NH3KT2k{OCCvaX6= M3TMWWlvcGmkaYTpc44hd2ZiUFmzT{BqdiCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCC|ZYLpcoUhPDd|IHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEmFNUC9NU4{|ryPLh?= NV\YcG95OjN2MUCwNFU>
HeLa (human carcinoma) cells. M1q2fGZ2dmO2aX;uJIF{e2G7 NXnrSXBIUW5idnn0do8hcW6qaXLpeIlwdiCxZjDEUmEu\GWyZX7k[Y51KHC{b4TlbY4hc2mwYYPlLGRPSS2SSzmg[pJwdSCKZVzhJEhpfW2jbjDjZZJkcW6xbXGpJINmdGy|LDDJR|UxRTFwNDFOwG0v M4HEeFE2PjV6OEew
THP1 cells NWXYSm1rTnWwY4Tpc44h[XO|YYm= M2DibGlvcGmkaYTpc44hd2ZiTVPQNU1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJHRJWDFiY3XscJMtKEmFNUC9NU43PSEQvF2u NF71U4wyPjd6OUe0Ni=>
HeLa cells NYXsVmF5TnWwY4Tpc44h[XO|YYm= Ml;kTY5pcWKrdHnvckBw\iCvVF;SJJBzd3SnaX6gbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|LDDJR|UxRTJwNTFOwG0v MYixOVY2QDh5MB?=
human MCF7 cells NFf1eIFEgXSxdH;4bYPDqGG|c3H5 MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJO69VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLNUC9Nk43OyEQvF2u MV[xPFY6OTh7NB?=
HeLa cells M3;NUGZ2dmO2aX;uJIF{e2G7 NIDLSYdKdmirYnn0bY9vKG:oIFHYMVc2ODNiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBRdGt|IHX4dJJme3OnZDDpckBJ\UyjIHPlcIx{KGK7IGfld5Rmem5iYnzveEwhUUN3PUOg{txONg>? MmTONVcyOzV{NEi=
human MCF7 cells NHPhTnJEgXSxdH;4bYPDqGG|c3H5 M1L4SWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMhcW5icILld4Vv[2Vib3[gNVAhfU1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVMvODhizszNMi=> MkXnNVg3QTF6OUS=
human MCF7 cells MUjDfZRwfG:6aXRCpIF{e2G7 NFnmblZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k:Oy5zNjFOwG0v NGfKdXgyQDZ7MUi5OC=>
human MDA-MB-231 cells MkDDR5l1d3SxeHnjxsBie3OjeR?= NX3oUoJVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSU2zMlMzKM7:TT6= NFWwNY0yQDZ7MUi5OC=>
human MDA-MB-231 cells M4LyfWN6fG:2b4jpZ:Kh[XO|YYm= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD12LkO1JO69VS5? NH2w[GIyQDZ7MUi5OC=>
human MDA-MB-468 cells M3jSWmN6fG:2b4jpZ:Kh[XO|YYm= NIm0V|ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4Phfg+9lCCLQ{WwQVQvPzZizszNMi=> NHK1d2syQDZ7MUi5OC=>
human HCT116 cells NUPDdVdpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXryb|Q4PDhiaB?= NGCwe5lIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKEhzMES3VkBufXSjboSgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13LkOg{txO Mkm1NlIzOTJ5MkG=
human HCT116 cells NXTu[2NtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlnBOFghcA>? NGnVc|VIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02NjhizszNMi=> MYmyNlIyOjd{MR?=
HeLa cells M3;INmJqdmSrbnegZYZncW6rdImgZZN{[Xl? NIX4eG9DcW6maX7nJIFn\mmwaYT5JIZweiCSSUOtb4lv[XOnIHnzc4xifGWmIH\yc40hUGWOYTDj[YxteyxiS3m9OkDPxE1? MWCxOVY2QDh5MB?=
human HCT116 cells M1PYcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW[0PEBp NFW5To1Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9Ok44KM7:TT6= NGfrW4szOjJzMkeyNS=>
MDA-MB-231 cells NES3PWVEgXSxdH;4bYPDqGG|c3H5 MlzxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok44OSEQvF2u MVmxPFY6OTh7NB?=
Sf9 cells MV\GeY5kfGmxbjDhd5NigQ>? M{KwT2lvcGmkaYTpc44hd2ZiQ1uyJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:Pi57IN88UU4> M1zjXFE5OzJzN{G2
human U87MG cells M2\Q[GZ2dmO2aX;uJIF{e2G7 M2L1cGlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIGW4O21IKGOnbHzzJIJ6KEWOSWPBMEBKSzVyPUiuNUDPxE1w NImyfZQyQDN2NU[wPS=>
human MDA-MB-468 cells MXfDfZRwfG:6aXRCpIF{e2G7 MorVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDpckBxemW|ZX7j[UBw\iBzMDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKPTB;OD6yJO69VS5? NVHSW2dXOTh4OUG4PVQ>
human A375 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 M3e0S|Q3KGh? M{P4WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB2NjDodpMtKEmFNUC9PE41KM7:TT6= NUW0V5dbOTdyNEmyOFg>
human A375 cells MkH1VJJwdGmoZYLheIlwdiCjc4PhfS=> MW\Jcohq[mm2aX;uJI9nKHOncoXtMYlv\HWlZXSgdJJwdGmoZYLheIlwdiCxZjDoeY1idiCDM{e1JINmdGy|LDDJR|UxRThwNDFOwG0v M{H1RVE4PjBzN{O5
human HL60 cells MVzDfZRwfG:6aXRCpIF{e2G7 MljNO|IhcA>? NULLeGttS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvQTRizszNMi=> MV2yNlQ5ODh3MR?=
mouse Raw264 macrophage NXiyfXA3TnWwY4Tpc44h[XO|YYm= NYfsTnVzUW6qaXLpeIlwdiCxZjDDOYEudWWmaXH0[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgVoF4OjZ2IH3hZ5JweGijZ3WsJGlEPTB;MUCg{txONg>? Ml7zNVY4QDl5NEK=
Sf9 cells M{\3WGZ2dmO2aX;uJIF{e2G7 NXu4cVh1UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJIJwfmmwZTDQTVNMKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MUCg{txONg>? MnzmNVA6QTh|NUG=
human MDA-MB-468 cells MkXuR5l1d3SxeHnjxsBie3OjeR?= NVj4S41FS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{BjgSCVUlKgZZN{[XluIFnDOVA:OTBwNDFOwG0v MUCxPFY6OTh7NB?=
human PC3 cell M1jwWHBzd2yrZnXyZZRqd25iYYPzZZk> Mn;jO|IhcA>? NFzkUIlKdmirYnn0bY9vKG:oIHj1cYFvKFCFMzDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrczygTWM2OD1zMj6xJO69VS5? NF\kdYszOzRzMECwOS=>
human HL60 cells MYTQdo9tcW[ncnH0bY9vKGG|c3H5 MWG3NkBp M1viXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zOD60N{DPxE1w MXOyOVY6Ozd6Nx?=
human BT474 cell NVH4Z4JIWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFz3TYw4OiCq NILhTllKdmirYnn0bY9vKG:oIHj1cYFvKEKWNEe0JINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgd5Bm[3S{b4Doc5RwdWW2cnnjJIFv[Wy7c3nz89yNKEmFNUC9NlAvPyEQvF2u MYeyN|QyODByNR?=
THP1 cells M3naNWZ2dmO2aX;uJIF{e2G7 NIH0R|NKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KG:oIGTIVFEh[2WubIOsJGlEPTB;M{eg{txONg>? MX:xOlc5QTd2Mh?=
human 184B5 cells NFXnS2VEgXSxdH;4bYPDqGG|c3H5 NEXkeWlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyQDSENTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{muN|ch|ryPLh?= NUG1XmdEOTh4OUG4PVQ>
human KB cells MkP6R5l1d3SxeHnjxsBie3OjeR?= NEO0elc4OiCq M3vNbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NESuO|Yh|ryPLh?= NEPDZlAzOTl2NUK1NC=>
mouse RAW264.7 cells MXHGeY5kfGmxbjDhd5NigQ>? NXK3O5hVOjVizszN MYmyNEBp NGXqZWtKdmirYnn0bY9vKG:oIGDJN2swSUuWIHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRiaV7PV{Bxem:2ZXnuJIV5eHKnc4Ppc44h[XRiMkWg{txOKGGodHXyJFIxKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NWT4cYo3OjR{OUm2NVY>
human A2780 cells M1S3VGFxd3C2b4Ppd{Bie3OjeR?= MmLtNkDPxE1? M3ryc|EzKGh? M1jGUWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gZ4l{eGyjdHnuMZJme2m|dHHueEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDa4SgcIV3\WxiYYSgNkB2VSCjZoTldkAyOiCqcoOgZpkhcW2vdX7vZoxwfCCjbnHsfZNqey5? M2nHUFE4Pjh2MEG4
human SW480 cells NUT4eHV3TnWwY4Tpc44h[XO|YYm= NGjnfJYzOCEQvF2= NFH3O5AzPCCq MkLOSIVkemWjc3WgbY4he3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCVV{S4NEBk\WyuczDheEAzOCC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= NF;lWnMyPzR5Mkm2Ni=>
mouse mast cells MWPGeY5kfGmxbjDhd5NigQ>? MknzNlAh|ryP M{LQRmlvcGmkaYTpc44hd2ZiU1PGMYlv\HWlZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gcY92e2VibXHzeEBk\WyuczDheEAzOCEQvF2= MlXzNVY4QDl5NEK=
human BJ cells MmjVSpVv[3Srb36gZZN{[Xl? NHrZRowzPSEQvF2= NXjObYg3OiCq M2LQWGlvcGmkaYTpc44hd2ZiUFmzT{B{cWewYXzpcochcW5iUFTHSk1{fGmvdXzheIVlKHOncoXtJJN1[XK4ZXSgbJVu[W5iQlqgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCybHHzcYllKEWJRmCvVGgh\G:vYXnuJI9nKEGtdDDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDQTE1GT0[SIILl[Il{fHKrYoX0bY9vKHSxIIDsZZNu[SCvZX3idoFv\SCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDjc45nd2OjbDDtbYNzd3Olb4D5 MV6xOlc3PzB6NR?=
human IGROV1 cells MlnSSpVv[3Srb36gZZN{[Xl? NGjmdIMzPC92ODDo NULEPXR6UW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1\WRiQVvUJIxmfmWuIHH0JFEhfG9iNTD0bY1meyCLQ{WwJIFnfGW{IEK0JJRwKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NVfZNZdZOjF{MU[xOVE>
human IGROV1 cells MkDlSpVv[3Srb36gZZN{[Xl? NVK2R2pXOjRxNEigbC=> Mn\UTY5pcWKrdHnvckBw\iCSSUPLM2FsfCCrbjDoeY1idiCLR2LPWlEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY4njcIlvKERzIHzleoVtKGG2IEGgeI8hPSC2aX3ld{BKSzVyIHHmeIVzKDJ2IITvJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M3ewNVIyOjF4MUWx
rat RBL2H3 cells NY\vVIhxTnWwY4Tpc44h[XO|YYm= MorQTY5pcWKrdHnvckBw\iCDMkOxPFcucW6mdXPl[EBl\We{YX71cIF1cW:wIHnuJJJifCCUQlyyTFMh[2WubIO= NYDTc|RIOTh|Mki3NVY>
human BJ cells MmnVSpVv[3Srb36gZZN{[Xl? Ml7ENlUh|ryP NIe4To0zKGh? NF;xXmJC[3SrdnH0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gZZQhXGi{M{C4JIlvKFCGR1[td5RqdXWuYYTl[EB{\XK3bTDzeIFzfmWmIHj1cYFvKEKMIHPlcIx{KGG2IEK1JJVOKHS{ZXH0[YQhOiCqcoOgZoVnd3KnIGDES2Yh[2ijbHzlcodmKGK7IHntcZVvd2Kub4T0bY5o NFnobHcyPjd4N{C4OS=>
human HCT116 cells M{n4eWZ2dmO2aX;uJIF{e2G7 NYTpNJF2OTBizszN MYOxNEBucW5? M1fOcGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHnuJIh2dWGwIFjDWFEyPiClZXzsd{B2e2mwZzDbN|JRZUGWUDDheEAyOCC3TTDh[pRmeiBzMDDtbY5{ NIjWXWQzOjJzMkeyNS=>
human HCT116 cells MYnGeY5kfGmxbjDhd5NigQ>? MoDNNVAh|ryP NVi3c|l3OTBibXnu MoW4TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNidYPpcochYzN{UG3BWHAh[XRiMUCgeW0h[W[2ZYKgNVAhdWmwcx?= M33wblIzOjF{N{Kx
human HCT116 cells MVLGeY5kfGmxbjDhd5NigQ>? MW[xNEDPxE1? MUfJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDifUBqdW23bn;icI91KGGwYXz5d4l{ NHu1Vo4zOjJzMkeyNS=>
human HCT116 cells NIq5ZYlHfW6ldHnvckBie3OjeR?= MWWxNEDPxE1? M1zxOmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFixNFQ4WiCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iYYSgNVAhfU1iYomgbY1ufW6xYnzveEBidmGueYPpdy=> NVTvS2FzOjJ{MUK3NlE>
human PC3 cells NF;admZHfW6ldHnvckBie3OjeR?= NYTRUo9nPTBizszN NWfWTZU2QCCq Ml7jTY5lfWO2aX;uJI9nKHB{MTDwdo91\WmwIHX4dJJme3Orb36gbY4hcHWvYX6gVGM{KGOnbHzzJIF1KDVyIIXNJIlv[3WkYYTl[EBnd3JiODDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yC{ZXzheIl3\SC2bzD1cpRz\WG2ZXSgZ49vfHKxbB?= MWOyNlk6QDR5Mh?=
human LNCAP cells MUfGeY5kfGmxbjDhd5NigQ>? MlTPNE4yNTNyIN88US=> NFiyTlE{OCCvaX6= NYPvc40xUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGxPS0GSIHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCzNEBucW6|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NHTwS40zOjh|MkOxOi=>
human LNCAP cells NV\p[2VLTnWwY4Tpc44h[XO|YYm= NYXSNlFkOC5zLUOwJO69VQ>? MojlNlQhcA>? NV3YNIh5TG:5boLl[5Vt[XSrb36gc4Yhe3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCOTlPBVEBk\WyuczDheEAxNjFidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= Ml\DNlI5OzJ|MU[=
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human H1299 cells NVPQ[XVCTnWwY4Tpc44h[XO|YYm= M37yTVAvOS1|MDFOwG0> NVrPSFZGOjRiaB?= MVzEc5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M4rXO|IzPjJ{ME[5
human H1299 cells Mnu3SpVv[3Srb36gZZN{[Xl? NUm5VoFkOC5zLUOwJO69VQ>? NHyxUIEzPCCq M2PZRmRwf25icnXneYxifGmxbjDv[kBkUUGSMjDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJFExOCC3Zz;tcEBVWkGLTDDhcoQhWEl|SzDpcohq[mm2b4KgUHkzQTRyMEK= NVHjbIdQOjJ4MkKwOlk>
human H1299 cells MX\GeY5kfGmxbjDhd5NigQ>? NIn6OWUxNjFvM{Cg{txO NHnaW|kzPCCq MYnJcoR2[3Srb36gc4YhTFJ3IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MYeyNlYzOjB4OR?=
human H1299 cells NWLD[5RbTnWwY4Tpc44h[XO|YYm= NETzZocxNjFvM{Cg{txO M3y5d|I1KGh? M{nZbGlv\HWldHnvckBw\iCMTlutcYVlcWG2ZXSgR2hQWCCneIDy[ZN{cW:wIHnuJIh2dWGwIFixNlk6KGOnbHzzJIF1KDBwMTD0c{A{OCC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz Mke2NlI3OjJyNkm=
HEK293 cells MWDGeY5kfGmxbjDhd5NigQ>? MWixMlUhcA>? NXvRZVRqTGm|cHzhZ4Vu\W62IH;mJHs{UF2OU1Sg[pJwdSCqdX3hckA2UFR4IILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOS53IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZx?= M2rid|IzPTN5MUWz
human U251HRE cells MoPESpVv[3Srb36gZZN{[Xl? M4\4WGlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBWOjVzSGLFJINmdGy|IHL5JINmdGxiYnHz[YQhemWyb4L0[ZIh\2WwZTDhd5NigQ>? NW[1UYxmOTh3MEG2NFE>
human HCT116 cells NXLldVNHTnWwY4Tpc44h[XO|YYm= NH\mVZcyOCEQvF2= MXLJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MUOyNlIyOjd{MR?=
Sf9 cells NUT5[HNP\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 MYDJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHL5JIZtfW:{ZYPj[Y51KHCxbHHybZpifGmxbjDhd5NigQ>? MmHqNlEyOjF4M{G=
human HCT116 cells M4\m[XBzd2yrZnXyZZRqd25iYYPzZZk> MUG3NkBp M1TMO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWxMlgzKM7:TT6= M2XTdVI2Pjl|N{i3
human HCT116 cells NWT6So9xS3m2b4TvfIlkyqCjc4PhfS=> MUC3NkBp NYLBfWNYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PTZwMEGg{txONg>? MnLyNlE6PDV{NUC=
human PC3 cells NUjWcFIxS3m2b4TvfIlkyqCjc4PhfS=> MYW3NkBp M1j1NmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[xMlM2KM7:TT6= M1vBeFIzPDhyOEWx
human HuH7 cells NFzMNXlRem:uaX\ldoF1cW:wIHHzd4F6 NVv3cJU4PzJiaB?= NXLtW204SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[3MlE5KM7:TT6= M1HDU|I2Pjl|N{i3
human A549 cells MkPWVJJwdGmoZYLheIlwdiCjc4PhfS=> NGTzT2g4OiCq MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QDJwM{Kg{txONg>? NIHEbIczPTZ7M{e4Oy=>
human A549 cells MnriR5l1d3SxeHnjxsBie3OjeR?= NWP4ZVJSPzJiaB?= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= NEf5THAzOjR6MEi1NS=>
human PC3 cells NHq1fohRem:uaX\ldoF1cW:wIHHzd4F6 M1X2V|I2KM7:TR?= Ml3DNVIxKGh? NHjtRVdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDheEAzPSC3TTDh[pRmeiBzMkCgbJJ{KGK7IF3UWEBie3OjeTDy[YxifGm4ZTD0c{BFVVOR MlTBNVY3QDBzNUm=
human H460 cells NX3HNFVUTnWwY4Tpc44h[XO|YYm= Mo\IN|Ah|ryP NIPaXYlKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFOncjC0O|MhfXBidH:gN|AhfU1? MlHiNVg2ODF4MEG=
human IGROV1 cells M3mxcGZ2dmO2aX;uJIF{e2G7 MlTMNlQhcA>? MYHD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNmKGG2IEGg[o9t\CCLQ{WwJIFnfGW{IEK0JIhzeyCkeTDmcI94KGO7dH;t[ZRzgQ>? MYmyNVIyPjF3MR?=
human IGROV1 cells MVTGeY5kfGmxbjDhd5NigQ>? MkK0NlQhcA>? M1PT[GNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgOUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 M3nNU|IyOjF4MUWx
human H4 cells Ml21SpVv[3Srb36gZZN{[Xl? M1KzXVIhcA>? M{D0[2Rm[3KnYYPlJIlvKE[\VlWtVmZRMyC4ZYPpZ4xmKGmwdHXud4l1gSCyZYKgZ4VtdCCrbjDoeY1idiCKNDDj[YxteyCjZoTldkAzKGi{czDy[YxifGm4ZTD0c{Bkd262cn;s NHS0eHQyQDB{NEW4OC=>
human MGC803 cells M3rY[WZ2dmO2aX;uJIF{e2G7 M1ywTFI2KM7:TR?= M2jlWlQ5KGh? NGTvRZNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOT0N6MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZZQhOjVidV2gZYZ1\XJiNEigbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZYZ1\XJiNEigbJJ{KGK7IH\sc5ch[3m2b33leIVzKHKnbHH0bZZmKHSxIHPvcpRzd2x? NIjS[nEzPDFzOUi2PS=>

... Click to View More Cell Line Experimental Data

In vivo試験 LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]
臨床試験 LY294002 is currently in Phase I clinical trials in patients with cancers.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [4]

kinase assays PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.

細胞アッセイ: [2]

細胞株 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
反応時間 0–48 hours
実験の流れ 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.

動物実験: [3]

動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
製剤 Dissolved in DMSO plus 0.25 ml of PBS
投薬量 0–100 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download LY294002 SDF
分子量 307.34
化学式

C19H17NO3

CAS No. 154447-36-6
保管 3年-20℃
2年-80℃in solvent
別名 SF 1101, NSC 697286
溶解度 (25°C) * In vitro DMSO 36 mg/mL (117.13 mM)
Ethanol 21 mg/mL (68.32 mM)
Water <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 2-morpholino-8-phenyl-4H-chromen-4-one

文献中の引用 (70)

Frequently Asked Questions

  • Question 1
    I want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of LY294002 (catalog no. s1105) says it will inactivates Akt/PKB. Is LY294002 available for Akt/PI3K inhibition?

    Answer: LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. It can inhibit PI3K/AKT. PKB is the alternative name of AKT.

  • Question 2
    What is the suggested formulation of this compound for mouse injection(i.p.)?

    Answer: It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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