Pictilisib (GDC-0941)

For research use only.

Catalog No.S1065 Synonyms: RG7321

359 publications

Pictilisib (GDC-0941) Chemical Structure

CAS No. 957054-30-7

Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

Selleck's Pictilisib (GDC-0941) has been cited by 359 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Targets
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
3 nM 3 nM 33 nM 75 nM 0.58 μM(Ki app)
In vitro

GDC-0941 is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold), and greater levels of selectivity against members of PI3K class II, III, and IV, including C2β, Vps34, DNA-PK, and mTOR. GDC-0941 potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. GDC-0941 inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 μM, 0.14 μM, 0.28 μM, and 0.72 μM, respectively. [1] GDC-0941 treatment potently inhibits the proliferation of both trastuzumab-sensitive and -insensitive HER2-amplified cells with IC50 of 149-944 nM. GDC-0941 inhibits proliferation of HER2-amplified cells that harbor PIK3CA mutations with IC50 of <500 nM, and effectively inhibits both proliferation and viability of HER2-amplified breast cancer cells that are resistant to trastuzumab due to PTEN loss. [2] GDC-0941 significantly inhibits the growth of HCT116, DLD1 and HT29 cells with GI50 of 1081 nM, 1070 nM and 157 nM, respectively. [3] GDC-0941 inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 NFi2bFVMcW6jc3WgRZN{[Xl? MlPVNUBp M{LERWROW09? MVLJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGSnbIThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NFnlOmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe1OFY2PCd-MUi3OVQ3PTR:L3G+
Sf9 MYrLbY5ie2ViQYPzZZk> MV2xJIg> M{\1NmROW09? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgTFExPDdvUjDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NVrBPHlTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
Sf9 NUPKXnpYU2mwYYPlJGF{e2G7 M2L4N|EhcA>? M13ZcmROW09? NYHNOmdlUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEV3NEWtT{BufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMECzJO69VQ>? NEiyZ4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe1OFY2PCd-MUi3OVQ3PTR:L3G+
Sf9 M4\uOmtqdmG|ZTDBd5NigQ>? NV;hRYdXOSCq MVPEUXNQ MW\Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMEOzJO69VQ>? NXK4[HZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
Sf9 MmjRT4lv[XOnIFHzd4F6 NIOybmEyKGh? NEHvXJFFVVOR MVXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGGucHjhJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjh M1;3NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{W0OlU1Lz5zOEe1OFY2PDxxYU6=
MDA-MB-361 NEHMeZBHfW6ldHnvckBCe3OjeR?= M2f1OFIhcA>? NU\hfHkyTE2VTx?= NHmxNYpKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{ODFOwG0> M2ewflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{W0OlU1Lz5zOEe1OFY2PDxxYU6=
PC3 M4rjUmZ2dmO2aX;uJGF{e2G7 M2D1WFIhcA>? MUfEUXNQ M3zi[2lvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGDDN{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yM{eg{txO MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
U87MG MknxSpVv[3Srb36gRZN{[Xl? NIfIXnozKGh? MoPySG1UVw>? MYPJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yNE[g{txO NIfqd3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe1OFY2PCd-MUi3OVQ3PTR:L3G+
MDA-MB-361 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXG5OkBp Mnj5SG1UVw>? M{\xfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvPzJizszN MoPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
A2780 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETYfIU6PiCq MXvEUXNQ MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IIfpeIghWEmNM1PBJIFv\CCSVFXOJI12fGG2aX;uJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? NVn6U|JjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
PC3 NXr6Xm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrXPVYhcA>? M{XoSGROW09? M3GyZmlEPTB;MD6yPEDPxE1? NWW3S4N1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
U87MG MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\MZXY6PiCq MVXEUXNQ MkjoTWM2OD1yLkm1JO69VQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
Sf9 NVvac4FiU2mwYYPlJGF{e2G7 M{HORVMxKG2rbh?= NFOyR3pFVVOR MlnsTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= NX\oNm1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFg{PDJpPkKyOVQ5OzR{PD;hQi=>
RAW 264.7 MULLbY5ie2ViQYPzZZk> M4DXfFkxKG2rbh?= M13oNGROW09? M4LUZmlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvOjl6IN88US=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2OEO0Nkc,OjJ3NEizOFI9N2F-
Sf9 NXzCNY0{U2mwYYPlJGF{e2G7 M2DOfFEhcA>? MVjJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZoV1[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW0Z7IHPlcIx{KHerdHigTWM2OCCxZjCwMlAyPyEQvF2= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0OUc,OjN3NEC2OFU9N2F-
Sf9 MojXT4lv[XOnIFHzd4F6 NU\W[4YxOSCq MmO3TY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= MkD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFUoRjJ|NUSwOlQ2RC:jPh?=
Sf9 MmH2T4lv[XOnIFHzd4F6 NVTPO45yOSCq NHfBXphKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM\2GvbXGg[ZhxemW|c3Xk NVe4NIVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDVpPkKzOVQxPjR3PD;hQi=>
Sf9 NXHaNZFRU2mwYYPlJGF{e2G7 MXKxJIg> MV;Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm NXvyOnp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDVpPkKzOVQxPjR3PD;hQi=>
SKOV3 M{WxNWtqdmG|ZTDBd5NigQ>? MoXWNUDPxE1? NYDxdoZFOSCq M3\J[GROW09? M2DX[mlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN4MEO0PEc,OjN|NkCzOFg9N2F-
MCF7 NXXWS4U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojUNUDPxE1? MUC5OkBp M2fkSWROW09? NGPZPFVIUTVyPUCuNFcxOiEQvF2= MmrvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NkCzOFgoRjJ|M{[wN|Q5RC:jPh?=
SKOV3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWexJO69VQ>? MlXYPVYhcA>? MVvEUXNQ M4K3OGdKPTB;MD6xOFc3KM7:TR?= NHvkPGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O2NFM1QCd-MkOzOlA{PDh:L3G+
PC3 M1rPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDKWGRYPzJiaB?= MWjEUXNQ MYHJR|UxRTBwMkig{txO M4DIN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUixO|E1Lz5{MUm4NVcyPDxxYU6=
MCF7.1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[3NkBp MoXLSG1UVw>? NHHMV3lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKEiHUkKg[4Vv\SC5aYToJGlEPTBib3[gNE4zQCEQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl6MUexOEc,OjF7OEG3NVQ9N2F-
MCF7-neo/Her2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYK3NkBp M4e2d2ROW09? M1TzU2lEPTB;MD6yPUDPxE1? NUnVTpVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OlI6ODNpPkKzOlYzQTB|PD;hQi=>
MCF7-neo/Her2 MWfLbY5ie2ViQYPzZZk> MlXaTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC5aYToJGlEPTBib3[gNE4xODdizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4MkmwN{c,OjN4NkK5NFM9N2F-
PC3 NGfnTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jMV|czKGh? MUnEUXNQ MnLrSWM2OD1yLkO0JO69VQ>? NGjZcJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm4OVY{QSd-MkG5PFU3Ozl:L3G+
MCF7.1 M2nYfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHKdGJoPzJiaB?= MlzQSG1UVw>? MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCHQ{WwJI9nKDBwM{mg{txO MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl6NU[zPUc,OjF7OEW2N|k9N2F-
PC3 M1TubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fZNlczKGh? M17WOWROW09? M2e2S2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> NWS1R3pvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwOVA3PjlpPkKwNFUxPjZ7PD;hQi=>
MCF7.1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV23NkBp NXL2NVU5TE2VTx?= MorkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? MkfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNUC2OlkoRjJyMEWwOlY6RC:jPh?=
MCF7.1 M1jHOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi3NkBp M13ESGVEPTB;MD63NkDPxE1? M2TuVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{S2OlU3Lz5{MEO0OlY2PjxxYU6=
NCI-H1975 NXjaemE4S3m2b4TvfIlkKEG|c3H5 Mn36O|IhcA>? NX\RfJR3UUN3ME2wMlI4KM7:TR?= NFXHU2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C1PVU1PSd-MkOwOVk2PDV:L3G+
H460 NUjYTWZKS3m2b4TvfIlkKEG|c3H5 NGXrbZc4OiCq NETlW29KSzVyPUCuPFch|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3OUW0OUc,OjNyNUm1OFU9N2F-
HT-29 NXjQS|VjS3m2b4TvfIlkKEG|c3H5 M1WxZ|czKGh? MXfJR|UxRTBwNk[g{txO MkXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNUm1OFUoRjJ|MEW5OVQ2RC:jPh?=
HepG2 NWi4dnVHS3m2b4TvfIlkKEG|c3H5 MYC3NkBp MVrJR|UxRTFizszN M1z4VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEW5OVQ2Lz5{M{C1PVU1PTxxYU6=
SGC7901 MkPHR5l1d3SxeHnjJGF{e2G7 NXGySW1LPzJiaB?= NXnvfFF2UUN3ME2xMlgh|ryP NWHqPW9tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOVk2PDVpPkKzNFU6PTR3PD;hQi=>
NCI-H226 M4\rbGN6fG:2b4jpZ{BCe3OjeR?= NXjZbW9ZPzJiaB?= M{KzTGlEPTB;Mj65JO69VQ>? NHrnOJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C1PVU1PSd-MkOwOVk2PDV:L3G+
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NCI-H358 M{iyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIizOFdKSzVyPUS5MlMxOThizszN NFzTXIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OjF6NUGvK|5USU6JRWK8M4E,
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-FoxO3a / FoxO3a / PUMA; 

PubMed: 29137323     


HCT116 cells were treated with 4μmol/L NVP-BKM120 or 4μmol/L Pictilisib for 24 hours. Indicated protein levels were analyzed by Western blotting.

p-S6RP / S6RP; 

PubMed: 30042442     


Western blot analysis of proteins as indicated in 4T1 cells treated with 1 µM GDC-0941 or vehicle for 24 h. Vinculin was used as a loading control. 

p-4EBP1 / 4EBP1; 

PubMed: 25857298     


Cells were treated with 0.5 μM GDC-0941 for the indicated time course and then collected for Western blot analysis of p-4EBP1. 

p-LRP6 / LRP6; 

PubMed: 25857298     


MDAMB-231, HCC1937 and MCF7 cells were treated with 0.5 µM GDC-0941 for 1 hr, and cell lysates were used for immunoblot analyses.

p-PAK / PAK1 / p-CRAF / RAF / p-MEK / MEK / p-ERK / ERK; 

PubMed: 24327733     


Cells were treated with 1 μM GDC-0941 for the indicated times, and lysates were probed with the indicated antibodies. Independent experiments were performed at least three times, and a representative result is shown.

29137323 30042442 25857298 24327733
Immunofluorescence
p65; 

PubMed: 30042442     


Representative images of immunofluorescent staining of p65 cellular localization in 4T1 cells treated with 1 µM GDC-0941 or vehicle for 24 h. 4T1 cells were cultured alone or co-cultured with RAW264.7 macrophages. Representative images of three independent experiments are shown. 

beta-catenin; 

PubMed: 25857298     


Cells were seeded on coverslips the day before the experiment and treated with 0.5 µM GDC-0941 for 18 hr. The immunofluorescence (IF) of beta-catenin is indicated as red fluorescence, and double staining with DAPI is blue. Magnification: 400 X for the left three panels. The right panel shows enlarged images from the white squares.

30042442 25857298
Growth inhibition assay
Cell viability; 

PubMed: 27117832     


The viability of the indicated cells treated with increasing concentrations of GDC-0941 (ranging from 70nM to 20 μM) for 72 hours, determined by CellTiter Glo Viability assay. The IC50 concentrations were calculated using GraphPad Prism program. The assay was performed in triplicate, and the error bars represent standard deviations.

27117832
In vivo GDC-0941 shows limited microsomal metabolism, resulting in 78% oral bioavailability [5]. Administration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. [1] Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. [2] GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases. [4]

Protocol

Kinase Assay:

[1]

- Collapse

Scintillation proximity assay:

Recombinant human PI3Kα, PI3Kβ, and PI3Kδ are coexpressed in a Sf9 baculovirus system with the p85α regulatory subunit and purified as GST-fusion proteins using affinity chromatography on glutathione-sepharose. Recombinant human PI3Kγ is expressed as monomeric GST-fusions and purified similarly. GDC-0941 is dissolved in DMSO and added to 20 mM Tris-HCl (pH 7.5) containing 200 μg yttrium silicate (Ysi) polylysine SPA beads, 4 mM MgCl2, 1 mM dithiothreitol (DTT), 1 μM ATP, 0.125 μCi [γ-33P]-ATP, and 4% (v/v) DMSO in a total volume of 50 μL. The recombinant GST-fusion of PI3Kα (5 ng), PI3Kβ (5 ng), PI3Kδ (5 ng), or PI3Kγ (5 ng) is added to the assay mixture to initiate the kinase reaction. After incubation for 1 hour at room temperature, the kinase reaction is terminated with 150 μL PBS. The mixture is then centrifuged for 2 minutes at 2000 rpm and read using a Wallac Microbeta counter. The reported IC50 values are calculated using a sigmoidal, dose-response curve fit in MDL Assay Explorer.
Cell Research:

[2]

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  • Cell lines: SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, and MKN-7 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 48 and 72 hours
  • Method:

    Cells are exposed to various concentrations of GDC-0941 for 48, and 72 hours. Proliferation/viability of cells is detected by using the CellTiter-Glo Luminescent Cell Viability Assay. The pAkt (Ser473), cleaved caspase-3, and cleaved PARP are analyzed by western blot. The Caspase-Glo 3/7 assay and the Cell Death Detection ELISAplus assay are used to detect caspase 3/7 activity, and apoptosis, respectively.


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: NCR nude mice implanted with MDA-MB-361.1 cells, and SCID, C.B-17/IcrHsd-Prkdcscid mice implanted subcutaneously with BT474-M1 cells
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 44 mg/mL (85.66 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/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 513.64
Formula

C23H27N7O3S2

CAS No. 957054-30-7
Storage powder
in solvent
Synonyms RG7321
Smiles CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6

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    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / 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

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02092831 Completed Drug: GDC-0941 Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT01740336 Completed Drug: GDC-0941|Drug: Placebo|Drug: Paclitaxel Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01474668 Completed Drug: GDC-0941 Healthy Volunteer Genentech Inc. October 2011 Phase 1
NCT01240226 Completed Drug: GDC-0941|Drug: ketoconazole Healthy Volunteer Genentech Inc. November 2010 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

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

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

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID