PI-103

Catalog No.S1038

PI-103 Chemical Structure

Molecular Weight(MW): 348.36

PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

Size Price Stock Quantity  
In DMSO USD 134 In stock
USD 147 In stock
USD 270 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 55 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
Features The first potent, synthetic mTOR inhibitor.
Targets
p110α [3]
(Cell-free assay)
p110β [3]
(Cell-free assay)
p110δ [3]
(Cell-free assay)
p110γ [3]
(Cell-free assay)
DNA-PK [3]
(Cell-free assay)
2 nM 3 nM 3 nM 15 nM 23 nM
In vitro

PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. [2] PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from insulin-stimulated decline in blood glucose. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-BE M13nfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu5NE05KM7:TR?= NIHoZZczPC92OD:3NkBp MXHpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq M{fLV|I3OjJ2Nkix
SH-SY5Y NXTOSm5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[4N4JXOC16IN88US=> NHjkTpMzPC92OD:3NkBp Ml:4bY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= NEDjTGMzPjJ{NE[4NS=>
SH-SY5Y  M1TNVGFxd3C2b4Ppd{BCe3OjeR?= Ml7ENUDPxE1? MUOwMlUuOjRiaB?= M3zWW5NmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NETzNWMzPjJ{NE[4NS=>
G 35 SC MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTLZ|cxNjB3LUKwJO69VQ>? NVL2XY1xOjRxN{KgbC=> MWXEUXNQ NVfKS4xQcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NITTTJkzPjF{MUK1NS=>
G 38 SC M3nyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3xSHBMOC5yNT2yNEDPxE1? NWPZWHRtOjRxN{KgbC=> M{DmfGROW09? MVrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M{HMTlI3OTJzMkWx
G 40 SC NUTid5J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmwMlA2NTJyIN88US=> NVzn[4M4OjRxN{KgbC=> NF;0eo1FVVOR NW\ubGFLcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NEexU5ozPjF{MUK1NS=>
G 35 DC M{LXUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDScIIzOC5yNT2yNEDPxE1? MXKyOE84OiCq NIfQ[5BFVVOR MlnlbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NVHEO4RxOjZzMkGyOVE>
G 38 DC M1Py[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3MNE4xPS1{MDFOwG0> MVuyOE84OiCq NYPodldQTE2VTx?= MnzkbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NVLsclF7OjZzMkGyOVE>
G 40 DC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPoboZkOC5yNT2yNEDPxE1? MnjWNlQwPzJiaB?= NIr4SGFFVVOR MoPMbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MVGyOlEzOTJ3MR?=
RD M4LYNWFxd3C2b4Ppd{BCe3OjeR?= MYKxM|EvPS9{IN88US=> M1r2SVczKGh? MojjbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MnrJNlU4PDl|N{i=
TE381.T MnznRZBweHSxc3nzJGF{e2G7 NHPj[2wyNzFwNT:yJO69VQ>? NEm2d|g4OiCq M3vqe4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NE\VOoQzPTd2OUO3PC=>
RMS13 NYiyWVNbSXCxcITvd4l{KEG|c3H5 MUexM|EvPS9{IN88US=> NFjxeZk4OiCq MX\pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NY\5bnFWOjV5NEmzO|g>
RH30  MmDnRZBweHSxc3nzJGF{e2G7 MlrENU8yNjVxMjFOwG0> NYrOeHhyPzJiaB?= NGiyc4FqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MVWyOVc1QTN5OB?=
VJ MWLBdI9xfG:|aYOgRZN{[Xl? MoDFNU8yNjVxMjFOwG0> MkTWO|IhcA>? MXjpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MmH0NlU4PDl|N{i=
HS578T NIrTOYFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NITGRYQxNTNizszN NGLoUGc4OiCq MX\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYmyOVczOTRzOR?=
BT549 M33oSWNmdGxiVnnhZoltcXS7IFHzd4F6 MofnNE0{KM7:TR?= NI\RcHM4OiCq NUK5OZk{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M2XKT|I2PzJzNEG5
MDA-MB-231 MoHDR4VtdCCYaXHibYxqfHliQYPzZZk> NU\QSVA6OC1|IN88US=> MXy3NkBp M1nZV4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{XseFI2PzJzNEG5
MDA-MB-468 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NInmfowxNTNizszN MYC3NkBp MV7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MVGyOVczOTRzOR?=
MDA-MB-436 MoPGR4VtdCCYaXHibYxqfHliQYPzZZk> MUOwMVMh|ryP MXO3NkBp NXL5N3E5cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NV\xUW4zOjV5MkG0NVk>
SUM149PT MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYHMOmdtOC1|IN88US=> MXO3NkBp MonwbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MWeyOVczOTRzOR?=
MDA-MB-468 Ml[0SpVv[3Srb36gRZN{[Xl? NHPwfIQxNjBzLUGwJO69VQ>? NHP6[YUzPCCq MoDh[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MlHvNlU4OjF2MUm=
MDA-MB-231 M3;uR2Z2dmO2aX;uJGF{e2G7 Mk\HNE4xOS1zMDFOwG0> M{Ww[FI1KGh? MVrkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh NW\4NVBCOjV5MkG0NVk>
HS578T MmqxSpVv[3Srb36gRZN{[Xl? NIT1O|IxNjBzLUGwJO69VQ>? NXvtPZlrOjRiaB?= MljM[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MXKyOVczOTRzOR?=
SW872 MWDGeY5kfGmxbjDBd5NigQ>? NUnMOJViOC5yMT2wMlUh|ryP M2PjWlI1KGh? NGnqZphz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> M1;5NFI1Pjl3NkOy
SW982 MUDGeY5kfGmxbjDBd5NigQ>? M4\BdVAvODFvMD61JO69VQ>? MWCyOEBp M3n5e5Jm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg Mk[5NlQ3QTV4M{K=
SW872 NWCxXnBHSXCxcITvd4l{KEG|c3H5 M4jNUlAvODFvMD61JO69VQ>? NUD1XY1PPDhiaB?= NHS1VYFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVGwS3k{OjR4OUW2N|I>
SW982 NG\6V3FCeG:ydH;zbZMhSXO|YYm= MnXxNE4xOS1yLkWg{txO MkXDOFghcA>? NYjRSWhKcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MmrlNlQ3QTV4M{K=
AGS HG NF3PbZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjMcIpmUUN3ME2wMlY5KMLzIECuNFMyKM7:TR?= NXTjPVZ2OjR3OUe0O|g>
AGS LG NFTnTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnK[lZKSzVyPUCuNFUhyrFiMD6wNFEh|ryP NXj1SY1GOjR3OUe0O|g>
HGC27 HG NUmxW2ZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPDSohKSzVyPUCuN|ghyrFiMD6wNlIh|ryP Mm\pNlQ2QTd2N{i=
HGC27 LG MlfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfMTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? MnnpNlQ2QTd2N{i=
MKN45 HG NWjselU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMEGgxtEhOC5yNUGg{txO M3;SV|I1PTl5NEe4
MKN45 LG NGLpcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwOEegxtEhOC5yM{Cg{txO Mk\LNlQ2QTd2N{i=
NUGC4 HG NUfNRWxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXyTWpKSzVyPUG0MlAhyrFiMz65NVMh|ryP MWSyOFU6PzR5OB?=
NUGC4 LG Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TYWWlEPTB;MUSuNEDDuSB3LkOyNUDPxE1? NVTjOoVPOjR3OUe0O|g>
A549 NH\NRVJHfW6ldHnvckBCe3OjeR?= MoH4NE4zPS9yLkWvNUDPxE1? NHLMc|UzPCCq MmG4bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NV;mWnNGOjR|NUG0NlU>
H460 MXrGeY5kfGmxbjDBd5NigQ>? M3jXWVAvOjVxMD61M|Eh|ryP M3HuXlI1KGh? MnrmbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> M{jiVFI1OzVzNEK1
H661 NXTnbJZtTnWwY4Tpc44hSXO|YYm= Mo[yNE4zPS9yLkWvNUDPxE1? M4\mZVI1KGh? NXTtcZdtcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MlznNlQ{PTF2MkW=
SAS MWXGeY5kfGmxbjDBd5NigQ>? NVrkWnZyOC5{NT:wMlUwOSEQvF2= NH3MTlczPCCq MknPbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NXrBe3RxOjR|NUG0NlU>
UT5 NVXCOHFFTnWwY4Tpc44hSXO|YYm= MkjDNE4zPS9yLkWvNUDPxE1? M{TIS|I1KGh? MnnUbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NUK3VHZkOjR|NUG0NlU>
FaDu NEixPWVHfW6ldHnvckBCe3OjeR?= MYOwMlI2NzBwNT:xJO69VQ>? NWTtWnJ6OjRiaB?= MWXpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MYmyOFM2OTR{NR?=
RD M4TI[WFxd3C2b4Ppd{BCe3OjeR?= M3rrWFEwOS53L{Kg{txO NEHHNmQ4OiCq M1zxWGROW09? MWLpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 M4Pp[|I{Pjh2OUK1
TE671 M33Lc2Fxd3C2b4Ppd{BCe3OjeR?= NHjycngyNzFwNT:yJO69VQ>? Ml7FO|IhcA>? NHrUOJVFVVOR M{f4Xolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NH7BbZozOzZ6NEmyOS=>
RH30  MlqyRZBweHSxc3nzJGF{e2G7 MYCxM|EvPS9{IN88US=> Mnj0O|IhcA>? M3LDSWROW09? MknEbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NFzhdokzOzZ6NEmyOS=>
RMS13 MXXBdI9xfG:|aYOgRZN{[Xl? MUexM|EvPS9{IN88US=> MoOzO|IhcA>? MnvCSG1UVw>? M1nvOYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MUKyN|Y5PDl{NR?=
SUM149PT MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1;GOlAvOyEQvF2= M2rpcFczKGh? M3nYXIVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? M1XjV|I{PjBzMEe0
MDA-MB-468 MmL5R4VtdCCYaXHibYxqfHliQYPzZZk> NHuwRYsxNjNizszN MWq3NkBp NV;aW|Fk\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| Ml;sNlM3ODFyN{S=
MDA-MB-231 M{nQfmNmdGxiVnnhZoltcXS7IFHzd4F6 NEXJOocxNjNizszN NXrTdYpiPzJiaB?= M3jjVYVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? MljINlM3ODFyN{S=
SY5Y NFLzT4JHfW6ldHnvckBCe3OjeR?= MV[xMlUwOi53L{Wg{txO MlnHNlQhcA>? Mn3jbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= NFX1Z2MzOzN5OEO0NS=>
SKNBE(2c) M{jFd2Z2dmO2aX;uJGF{e2G7 NY\rT2tXOS53L{KuOU82KM7:TR?= NGLCZoEzPCCq NW\4UmVHcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MVOyN|M4QDN2MR?=
RD NWnncHdISXCxcITvd4l{KEG|c3H5 NIDMe3Y{KML3TR?= M{DVN|EzKGh? NV;sTY5{TE2VTx?= M4nwRpNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NFTIN4gzOzNyMEiwPS=>
TP5014 NVK0dmZESXCxcITvd4l{KEG|c3H5 MnjNN{DDvU1? NVTZSZRkOTJiaB?= NVT6SlhkTE2VTx?= NWPMVY5Oe2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> NFT4R|MzOzNyMEiwPS=>
HT1080 MXvBdI9xfG:|aYOgRZN{[Xl? NYHYOFU2OyEEtV2= MWixNkBp NVPuT|VSTE2VTx?= M2\TUZNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NX\6SHB6OjN|MEC4NFk>
A549 MnqxSpVv[3Srb36gRZN{[Xl? NVXTZ2VFOC1|LkOg{txO M1izR|czKGh? NILpbGVqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M4TvcVI{OjV7NUmx
HCC827 MoWwSpVv[3Srb36gRZN{[Xl? MY[wMVMvOyEQvF2= NVrZWVZzPzJiaB?= MVHpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MnPTNlMzPTl3OUG=
H3122 M1\ZR2Z2dmO2aX;uJGF{e2G7 NUXhZ3pnOC1|LkOg{txO NWDBbIp7PzJiaB?= Mmm4bY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV MnL6NlMzPTl3OUG=
TALL-1 NYi3RppuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HpblHjiIoQvF2= MX63JIQ> MYjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MkLYNlMxOzh{N{O=
HPB-ALL NH;VW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXuyW3RCOeLCid88US=> NV\FOXlNPyCm NHjmSnpl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M{XkSlI{ODN6Mkez
DND41 M17KVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHyNgKBkc7:TR?= NFu3[nI4KGR? M{XWcIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NFLFPG8zOzB|OEK3Ny=>
SUP-T1 NFPIWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLRNgKBkc7:TR?= MkGyO{Bl MmfY[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NEDIbFYzOzB|OEK3Ny=>
PEER NIPtdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGmwbWky6oDLzszN M4O3WVch\A>? MX\k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M{PnWFI{ODN6Mkez
ALL-SIL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWix5qCK|ryP M2rodVch\A>? MWrk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MorvNlMxOzh{N{O=
KE37 M36yOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrlU4pjOeLCid88US=> M2rydFch\A>? M1X2WoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NHjufo8zOzB|OEK3Ny=>
Karpas-45 MlTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOx5qCK|ryP NXPFO5ZGPyCm MWnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MYKyN|A{QDJ5Mx?=
RPMI-8402 M4jEdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzr[4xXOeLCid88US=> NGDXV2I4KGR? MUnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M1j1Z|I{ODN6Mkez
Jurkat M2PHNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWex5qCK|ryP MnjPO{Bl NGLJWnJl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NHexfIMzOzB|OEK3Ny=>
MOLT-4 NUXIWlFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD1RXZLOeLCid88US=> MVu3JIQ> NYrCW3Rb\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MkDnNlMxOzh{N{O=
PF-382 NWrmWYNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuybY0y6oDLzszN MXW3JIQ> Mn[x[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MVuyN|A{QDJ5Mx?=
CCRF-CEM M3;mdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fVbFHjiIoQvF2= NF6wdoc4KGR? NXzlW3d1\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NWDZdlZLOjNyM{iyO|M>
LOUCY NFfnZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHPNXAy6oDLzszN M1SxVFch\A>? NH7Kfodl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M4f0UlI{ODN6Mkez
MOLT-16 NV7QOWR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfZUnUy6oDLzszN M2HndVch\A>? NFTxRm5l\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M2r4RlI{ODN6Mkez
MM1S NVXmOVEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fleFAuOiEQvF2= NH31TXczPCCq NIrIUZlKSzVyPUCuOUDPxE1? NUDncGUyOjJ6MkmyN|Q>
NCI-H929 NUnEbW9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMVIh|ryP NYXxNHZ2OjRiaB?= NWHqc25EUUN3ME2wMlI2KM7:TR?= M33wSFIzQDJ7MkO0
KMS12-BM  M33TO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XuN|AuOiEQvF2= MnS0NlQhcA>? NY\sOVRtUUN3MP-8olIh|ryP M13ENlIzQDJ7MkO0
MDA-MB-436 MorYSpVv[3Srb36gRZN{[Xl? NWTWTW9OOSEQvF2= Mnv2NlQhcA>? Mn3GdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= M3\DWlIzPDh6NUmw
SUM149PT M4jTPGZ2dmO2aX;uJGF{e2G7 M1fVfVEh|ryP MXOyOEBp MUny[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M1WwT|IzPDh6NUmw
SUM1315MO2 MY\GeY5kfGmxbjDBd5NigQ>? Ml3ZNUDPxE1? MWeyOEBp NYDTXmpremWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> MX:yNlQ5QDV7MB?=
HCC1937 MX\GeY5kfGmxbjDBd5NigQ>? M33ROVEh|ryP NYHVblZ7OjRiaB?= NFfNfXBz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU Mk\5NlI1QDh3OUC=
HCC827 NF;sU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PwNVAuOyEQvF2= M4DJTVczKGh? NGj3OYhKSzVyPUCuN{DPxE1? M3\HW|IyOjJyNEe0
PC-9  NFfYd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO2cGcxNTNizszN NEfKS4U4OiCq Ml2zTWM2OD1yLkig{txO MUOyNVIzODR5NB?=
LN229 M2CwXWZ2dmO2aX;uJGF{e2G7 NHy4R|MyKM7:TR?= NUnlUVJNPDhiaB?= NIDIW|ZqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NHXNe5UzOTB4Mkm5Ny=>
U87 MWDGeY5kfGmxbjDBd5NigQ>? MkXoNUDPxE1? MXe0PEBp M2WxWYlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NG\6TXMzOTB4Mkm5Ny=>
U373 M17JNGZ2dmO2aX;uJGF{e2G7 NGXndWIyKM7:TR?= MUO0PEBp Mlf4bY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NHLScFUzOTB4Mkm5Ny=>
SF767 MVLGeY5kfGmxbjDBd5NigQ>? MYexJO69VQ>? MVe0PEBp MVnpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v M{fn[FIyODZ{OUmz
Mel-Juso NXzhbm92S2WubDDWbYFjcWyrdImgRZN{[Xl? NIfHNZoxNjBz4pETNVDjiIoQvF2= NFnCfVc4OiCq M2\xSYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIrSTHQzOTB2OEe4OS=>
518A2  MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXGwMlAy6oDVMUFihKnPxE1? M2TYOlczKGh? M1Tt[4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlvLNlExPDh5OEW=
Mel-Juso  M4TCUGZ2dmO2aX;uJGF{e2G7 NIHGWngxNjByMfMAl|HjiIoQvF2= Ml;nNlQhcA>? MX7zeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| M1m4flIyODR6N{i1
518A2 M3\6N2Z2dmO2aX;uJGF{e2G7 NETRT3ExNjByMfMAl|HjiIoQvF2= MnTPNlQhcA>? NX;mUGw5e3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> MmLLNlExPDh5OEW=
PC3  NYLMU2F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSyOIg> MXvHTVUxyqB;IEGwNEBvVQ>? NGTqTFMzODV3MUC2NS=>
U87MG NHO0RoJHfW6ldHnvckBCe3OjeR?= MY[wMlEuOSEQvF2= NFjsfGYzPOLCiXlCpC=> Ml3ZSG1UVw>? MlflbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MUKxPVY{OzZ6Mx?=
U138MG NU\tTnF[TnWwY4Tpc44hSXO|YYm= NHLHZ2MxNjFvMTFOwG0> NX74bpJKOjUkgJnoxsA> M3HJO2ROW09? MUjpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NG\hOIYyQTZ|M{[4Ny=>
U118MG NGi3XmFHfW6ldHnvckBCe3OjeR?= NFrUXosxNjFvMTFOwG0> NHnYbmgzPOLCiXlCpC=> MkHwSG1UVw>? MoXmbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MnywNVk3OzN4OEO=
U87MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XKfWlEPTB;MD6xOEDPxE1? NX\SVnU4OTl3OESyNlc>
IGROV-1 M1rET2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjTPFROUUN3ME2wMlA3KM7:TR?= NXvLUFBzOTl3OESyNlc>
DETROIT562 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfHTWM2OD1yLkGzJO69VQ>? NH;kb5EyQTV6NEKyOy=>
PC3  NU\lN3RGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMUCg{txO NW\kNVZWOTl3OESyNlc>
SKOV-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j3Z2lEPTB;MD6xNkDPxE1? MYmxPVU5PDJ{Nx?=
HUVEC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\ONnRKSzVyPUCuNFgh|ryP MVWxPVU5PDJ{Nx?=
UCH-1  MlixSpVv[3Srb36gRZN{[Xl? M1PDfVAuPSEQvF2= NUe1XIs1cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Mnr0NVk2Ojh2NEG=
UCH-1  M4DuVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DPXFAvODFvMUCg{txO NEXl[VY3KGR? M1Szc4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? NFTYNlcyQTV{OES0NS=>
UCH-1  NEXHcXlCeG:ydH;zbZMhSXO|YYm= M4\iNlAvOS1zMDFOwG0> MlK0NlQhcA>? M4jLc2ROW09? M3XR[Ylv\HWlZYOgZZBweHSxc3nz MknyNVk2Ojh2NEG=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-S6K, S6K, P-S6, S6, P-p38 or p38 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 ; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-GSK3, GSK3, P-BAD BAD, P-Mdm2, Mdm2, P-p27 or p27 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

β-TrCP1 / p-mTOR; 

PubMed: 25721419     


PI-103 reduced the level of β-TrCP1 protein in TNBC cells. Cells were treated with 3 μm of PI-103 for 24 h and subjected to western blot analysis with indicated antibodies. HSP90 or β-actin was used as a loading control.

18922908 25721419
Immunofluorescence
autophagosomes / autolysosomes; 

PubMed: 26814436     


mRFP-GFP-LC3 stably expressing HeLa cells were treated with vehicle, PI (1uM), Baf (100nM) or PI (1uM)+Baf (100nM) for 20 hours. Cells were then fixed and confocal images were acquired. The numbers of autophagosomes (green vesicles) and autolysosomes (red vesicles minus green vesicles) were assessed with automated Cellomics microscopy (n = 12). Data are shown as mean ±sd. ***: P < 0.001. Scale bar: 20um.

26814436
Growth inhibition assay
Cell viability; 

PubMed: 25721419     


PI-103 reduced the viable TNBC cells in a dose-dependent manner. Cells were treated with increasing amounts of PI-103 up to 72 h and the viable cells were measured by MTT assay. Data from two independent experiments performed in triplicate are shown as mean±s.e.m.

25721419
In vivo When tumors reach 50-100 mm3, animals are randomized and treated with vehicle or PI-103. PI-103 exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. [2] Mice treated with PI-103 have no obvious signs of toxicity premorbidly (based on body weight, food and water intake, activity, and general exam) or at necropsy. Treated tumors display decreased levels of phosphorylated Akt and S6, consistent with blockade of p110α and mTOR. PI-103 treatment is cytostatic to glioma xenografts. [2]

Protocol

Kinase Assay:[3]
- Collapse

Enzyme Assays:

Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.
Cell Research:[2]
- Collapse
  • Cell lines: U87MG cells
  • Concentrations: 0.5 μM
  • Incubation Time: 24 hours
  • Method: U87MG cells are treated with PI-103 for 24 hours. Cell death is quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit. Percentage of cell death (mean of three 12-well plates per experimental point) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
  • Formulation: 50% DMSO
  • Dosages: 5 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 24 mg/mL (68.89 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/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

Molecular Weight 348.36
Formula

C19H16N4O3

CAS No. 371935-74-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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

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 )

  • C1
    V1
    C2
    V2

* 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

  • 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

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

Tags: buy PI-103 | PI-103 supplier | purchase PI-103 | PI-103 cost | PI-103 manufacturer | order PI-103 | PI-103 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID