Pictilisib (GDC-0941) 化学構造
分子量: 513.64

高品質保証

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Quality Control & MSDS

製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Pictilisib (GDC-0941)のメカニズム

製品の説明

生物活性

製品説明 Pictilisib (GDC-0941)は、PI3Kα、PI3Kβ、PI3KδとPI3Kγの強力な阻害剤で、IC50 がそれぞれ 3 nM、 33 nM、 3 nM、75 nMです。
ターゲット PI3Kα PI3Kβ PI3Kδ PI3Kγ
IC50 3 nM 33 nM 3 nM 75 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Sf9 MojUT4lv[XOnIFHzd4F6 NFTJeGgyKGh? NVjHUmpLTE2VTx?= NYLv[I96UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDk[Yx1[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN M3;aS|E5PzV2NkW0
Sf9 M1:1XGtqdmG|ZTDBd5NigQ>? M2PKXFEhcA>? MWXEUXNQ NVjiTpZCUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? MXOxPFc2PDZ3NB?=
Sf9 M3L0W2tqdmG|ZTDBd5NigQ>? M1\0UVEhcA>? NX7HO5E3TE2VTx?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN MWCxPFc2PDZ3NB?=
Sf9 NEjEb2dMcW6jc3WgRZN{[Xl? NH76O5YyKGh? M3KzSWROW09? NFLNeVJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFM{KM7:TR?= MkGwNVg4PTR4NUS=
Sf9 MVjLbY5ie2ViQYPzZZk> MVqxJIg> MVfEUXNQ MUfJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGGucHjhJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjh Moi2NVg4PTR4NUS=
MDA-MB-361 NV7CXIkxTnWwY4Tpc44hSXO|YYm= MlzHNkBp NGfYVXVFVVOR NWD4RnJNUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO MXmxPFc2PDZ3NB?=
PC3 NGnmVmhHfW6ldHnvckBCe3OjeR?= NED5epIzKGh? Mn;OSG1UVw>? MYDJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCSQ{OgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODN5IN88US=> MlrINVg4PTR4NUS=
U87MG NVP5emxRTnWwY4Tpc44hSXO|YYm= MnS3NkBp MmTVSG1UVw>? MmfzTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? MYCxPFc2PDZ3NB?=
MDA-MB-361 MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzXR206PiCq NX7KOoxHTE2VTx?= NVjUZ3R5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC55MjFOwG0> M{DXTlE5PzV2NkW0
A2780 MoLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S4Vlk3KGh? MWXEUXNQ NH62SYtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= M1roUFE5PzV2NkW0
PC3 NH:zelhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nvdlk3KGh? M3W0NWROW09? MoP4TWM2OD1yLkK4JO69VQ>? NU\4OlFGOTh5NUS2OVQ>
U87MG MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;k[|k3KGh? MoCwSG1UVw>? M2rLdWlEPTB;MD65OUDPxE1? MVexPFc2PDZ3NB?=
Sf9 NXfCflBbU2mwYYPlJGF{e2G7 Mn\ON|AhdWmw NV\UbGR3TE2VTx?= MlTjTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= NGCze3ozOjV2OEO0Ni=>
RAW 264.7 Mn;nT4lv[XOnIFHzd4F6 NIXFPFY6OCCvaX6= M3jCWmROW09? NHLw[2lKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> M1j2dFIzPTR6M{Sy
Sf9 NFXK[lhMcW6jc3WgRZN{[Xl? NXnOVIx2OSCq NGLRXG1KdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> MX[yN|U1ODZ2NR?=
Sf9 M{e4WWtqdmG|ZTDBd5NigQ>? NFXjO44yKGh? M1jRdmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= NUnUe3JFOjN3NEC2OFU>
Sf9 M2XiPGtqdmG|ZTDBd5NigQ>? NULtS5E1OSCq NFGzcIpKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM\2GvbXGg[ZhxemW|c3Xk MWWyN|U1ODZ2NR?=
Sf9 M4\rTWtqdmG|ZTDBd5NigQ>? NFLQSGIyKGh? MXLJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm M4\JSFI{PTRyNkS1
SKOV3 Mn\LT4lv[XOnIFHzd4F6 NYq5[mhHOSEQvF2= NWTkfGV7OSCq NEfNOHRFVVOR NHHVNItKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w NXPOPFZVOjN|NkCzOFg>
MCF7 MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT0NUDPxE1? NXTzOIh3QTZiaB?= MUXEUXNQ M4XWOmdKPTB;MD6wO|AzKM7:TR?= NGThb3IzOzN4MEO0PC=>
SKOV3 NFu5UoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HxRVEh|ryP M1G4N|k3KGh? NV3RR|dnTE2VTx?= NYjLTXhuT0l3ME2wMlE1PzZizszN M2iwR|I{OzZyM{S4
PC3 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG3NkBp M3j5bGROW09? MknQTWM2OD1yLkK4JO69VQ>? NXP1WohCOjF7OEG3NVQ>
MCF7.1 M3;Wfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr5[2s4OiCq M2\VPWROW09? MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? MlzVNlE6QDF5MUS=
MCF7-neo/Her2 NX;QfZczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K3S|czKGh? M2TuUGROW09? Mnf6TWM2OD1yLkK5JO69VQ>? MnXYNlM3PjJ7MEO=
MCF7-neo/Her2 M2rsZ2tqdmG|ZTDBd5NigQ>? NHXmVG1KdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiQVvUJJBpd3OyaH;yfYxifGmxbjDheEBUPDd|IIfpeIghUUN3MDDv[kAxNjByNzFOwG0> M3jtVVI{PjZ{OUCz
PC3 NY\BUVZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi3NkBp NHPjOVlFVVOR MULFR|UxRTBwM{Sg{txO NFixU5ozOTl6NU[zPS=>
MCF7.1 M{PNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jTTVczKGh? M133cWROW09? Mk\BRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? MnTvNlE6QDV4M{m=
PC3 NE\2WmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z0R|czKGh? MkO1SG1UVw>? NGGyOHBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> M4e3ZlIxODVyNk[5
MCF7.1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETocFM4OiCq MmLjSG1UVw>? MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCLQ{WwJI9nKDBwM{Sg{txO M3XwOlIxODVyNk[5
MCF7.1 M2XDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq3NkBp MXzFR|UxRTBwN{Kg{txO NI\vSVUzODN2Nk[1Oi=>
NCI-H1975 M4LDfGN6fG:2b4jpZ{BCe3OjeR?= MW[3NkBp MUPJR|UxRTBwMkeg{txO MV[yN|A2QTV2NR?=
H460 MYDDfZRwfG:6aXOgRZN{[Xl? NVrQO|VyPzJiaB?= NEm1bmlKSzVyPUCuPFch|ryP MmjPNlMxPTl3NEW=
HT-29 MXTDfZRwfG:6aXOgRZN{[Xl? MmfVO|IhcA>? NY\IWpVKUUN3ME2wMlY3KM7:TR?= M3Txe|I{ODV7NUS1
HepG2 MlzDR5l1d3SxeHnjJGF{e2G7 M4jRSFczKGh? MVLJR|UxRTFizszN MUKyN|A2QTV2NR?=
SGC7901 MoHBR5l1d3SxeHnjJGF{e2G7 MWe3NkBp MWLJR|UxRTFwODFOwG0> MXKyN|A2QTV2NR?=
NCI-H226 MXzDfZRwfG:6aXOgRZN{[Xl? MmHBO|IhcA>? NHriXopKSzVyPUKuPUDPxE1? M3OzRlI{ODV7NUS1
A549 MWrDfZRwfG:6aXOgRZN{[Xl? M1znTlczKGh? NYj5NJpiUUN3ME22Mlkh|ryP MnfWNlMxPTl3NEW=
U87MG NELkW5lEgXSxdH;4bYMhSXO|YYm= M{fWWFczKGh? MVTJR|UxRTdwN{eg{txO MWeyN|A2QTV2NR?=
HBC4 NWO5OIpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Hmboxw\0eLNUC9MVYvODNiTR?= M{fIW|IzOzN4MkS2
BSY1 MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7nUYNHdG:pR1m1NF0uPi57MDDN NUnWfmhJOjJ|M{[yOFY>
HBC5 NVnlVXNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P1[oxw\0eLNUC9MVYvPjBiTR?= M4nkelIzOzN4MkS2
MCF7 NYHj[FkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnrXJk5dG:pR1m1NF0uPy5|MzDN NFW5SYEzOjN|NkK0Oi=>
MDA-MB-231 M1O5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TpR4xw\0eLNUC9MVUvPDZiTR?= NIfufYUzOjN|NkK0Oi=>
U251 NFrVNFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HERoxw\0eLNUC9MVUvPTBiTR?= MUKyNlM{PjJ2Nh?=
SF268 NEC1c3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nC[Yxw\0eLNUC9MVUvOzliTR?= NID3fnQzOjN|NkK0Oi=>
SF295 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fwVYxw\0eLNUC9MVYvOzdiTR?= NV;y[5RxOjJ|M{[yOFY>
SF539 NH7EcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHLUlgydG:pR1m1NF0uPi53MDDN Mlf1NlI{OzZ{NE[=
SNB75 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjZO|Jtd2eJSUWwQU04NjFyIF2= Mlu1NlI{OzZ{NE[=
SNB78 NFHjcpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULsc4dIUTVyPT22MlUzKE1? Mm\QNlI{OzZ{NE[=
HCC2998 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDsc4dIUTVyPT22MlI6KE1? M{H3[lIzOzN4MkS2
KM12 NE\ZVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXHcndNdG:pR1m1NF0uPS55NjDN NG\se4wzOjN|NkK0Oi=>
HT-29 NHHsWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnRVoNPdG:pR1m1NF0uPi5|MDDN M3HoZlIzOzN4MkS2
HCT15 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HzNoxw\0eLNUC9MVYvOTJiTR?= MkHrNlI{OzZ{NE[=
HCT116 Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvZcI9oT0l3ME2tOU45PyCP Moq4NlI{OzZ{NE[=
NCI-H23 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XaW4xw\0eLNUC9MVUvPzNiTR?= NV3GVWR[OjJ|M{[yOFY>
NCI-H226 NFfES5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG0cI9oT0l3ME2tOk4zOSCP NITqWZYzOjN|NkK0Oi=>
NCI-H522 NFvVPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzYcI9oT0l3ME2tOk42QCCP M4\OUlIzOzN4MkS2
NCI-H483 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fDXoxw\0eLNUC9MVYvPTZiTR?= NGTTVnkzOjN|NkK0Oi=>
A549 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\UfZBRdG:pR1m1NF0uPi5zNTDN MX6yNlM{PjJ2Nh?=
DMS273 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPyS2pbdG:pR1m1NF0uPi52MzDN NYOxWXN[OjJ|M{[yOFY>
DMS114 NHHjXlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\Fd4xw\0eLNUC9MVUvQTJiTR?= MknRNlI{OzZ{NE[=
LOXIMVI NIHrPGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\sc4dIUTVyPT22MlI6KE1? MkDsNlI{OzZ{NE[=
OVCAR3 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzsc4dIUTVyPT22MlcyKE1? NWnNOI1KOjJ|M{[yOFY>
OVCAR4 M3HHNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLsc4dIUTVyPT21Mlc3KE1? NXKzSXgxOjJ|M{[yOFY>
OVCAR5 MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\SPYxw\0eLNUC9MVYvOjZiTR?= NUf4Xo1lOjJ|M{[yOFY>
OVCAR8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PBOIxw\0eLNUC9MVUvPzNiTR?= NWLveW9GOjJ|M{[yOFY>
SKOV3 NEnsSYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPsc4dIUTVyPT22MlUzKE1? MW[yNlM{PjJ2Nh?=
RXF631L NXi3enk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrsc4dIUTVyPT22Mlg5KE1? NWXneIJIOjJ|M{[yOFY>
ACHN MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES1NZFtd2eJSUWwQU03NjB5IF2= MYGyNlM{PjJ2Nh?=
St-4 MoraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHvdox5dG:pR1m1NF0uPS53NjDN MnP6NlI{OzZ{NE[=
MKN1 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTsc4dIUTVyPT23MlA5KE1? MW[yNlM{PjJ2Nh?=
MKN7 NHrDdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVr3SopFdG:pR1m1NF0uPi53MDDN M{\QVVIzOzN4MkS2
MKN28 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvsc4dIUTVyPT21MlUzKE1? MnXONlI{OzZ{NE[=
MKN45 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\pdZJWdG:pR1m1NF0uPi53NTDN M{Xt[|IzOzN4MkS2
MKN74 M1LCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2xdnNYdG:pR1m1NF0uPi5yMjDN Mm\PNlI{OzZ{NE[=
DU145 MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTVcI9oT0l3ME2tOU45PSCP NGfMUJYzOjN|NkK0Oi=>
PC3 NIjEfVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHyyXpltd2eJSUWwQU03NjZ4IF2= M1exT|IzOzN4MkS2
ES5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkS2TWM2OD13MD6yNUBvVQ>? M2m3ZnNCVkeHUh?=
HH M4rnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFzMT6wPEBvVQ>? NHr2dWxUSU6JRWK=
MHH-PREB-1 MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jGZmlEPTB;MUG0MlMhdk1? M4rod3NCVkeHUh?=
NCI-H1770 NYrwSXZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK3S5pKSzVyPUGyN{45PiCwTR?= NH7NNJBUSU6JRWK=
HuO9 NIHiXGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEflNXZKSzVyPUKwOk4xOiCwTR?= M1jUNHNCVkeHUh?=
HAL-01 MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJyNj63N{BvVQ>? MXjTRW5ITVJ?
NOS-1 NV\peVF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXFTWM2OD1{MUGuPFIhdk1? MkfUV2FPT0WU
HGC-27 MmfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJzMj61O{BvVQ>? Ml3TV2FPT0WU
NB69 NEDuT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfjVodKSzVyPUK0OU4zPyCwTR?= NXjzdHdyW0GQR1XS
RS4-11 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;QRmlEPTB;Mk[xMlc3KG6P M4XmO3NCVkeHUh?=
DOK M{iyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXsS3A2UUN3ME2zNFEvPyCwTR?= Mli0V2FPT0WU
LB2241-RCC NEm1cnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTNyMz64OEBvVQ>? NHTXeHlUSU6JRWK=
NCI-H1623 M{Xad2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPEdI1KSzVyPUOwOE4xQCCwTR?= M13VRXNCVkeHUh?=
YH-13 MmPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTNyND6zNkBvVQ>? NF75R41USU6JRWK=
BPH-1 M2rrdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTNzNDDuUS=> NUT1VWlbW0GQR1XS
AN3-CA NVT6dm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjLN|RKSzVyPUO0NE4{PyCwTR?= MnrNV2FPT0WU
ES7 NHrX[JVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LiN2lEPTB;M{SxMlk6KG6P M2LnNXNCVkeHUh?=
MDA-MB-175-VII NXTnZpM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDTZYJKSzVyPUO1Nk46OiCwTR?= NIDLRVFUSU6JRWK=
GAMG MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u4UGlEPTB;M{ewMlg2KG6P Mnn0V2FPT0WU
CHL-1 NWLvcGZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj6TWM2OD1|N{iuOlUhdk1? M4nGVHNCVkeHUh?=
NB7 NVHVeI9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HUe2lEPTB;M{i5Mlg{KG6P NWHxW3N[W0GQR1XS
MFE-280 NVrrbZFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjPZlVKSzVyPUSxPE4zKG6P MmHuV2FPT0WU
HL-60 NHewWIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTR{NT63OUBvVQ>? Mkm0V2FPT0WU
GCIY NVrDWY55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HsXmlEPTB;NEOzMlghdk1? NXq5UVN1W0GQR1XS
MDA-MB-361 MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXxTWM2OD12M{muNVMhdk1? NYXMTpNvW0GQR1XS
LXF-289 NEfze3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvYfGpKSzVyPUS0PE4zPyCwTR?= MnrDV2FPT0WU
NBsusSR MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTJVI9KSzVyPUS4PE45PSCwTR?= M2HheHNCVkeHUh?=
KU-19-19 M1nvVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf3b2x7UUN3ME21NVYvODdibl2= M3fNWXNCVkeHUh?=
A204 MnfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[zTWM2OD13MkKuN|Mhdk1? NWLaTnRKW0GQR1XS
LB1047-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTV{Mj65N{BvVQ>? MlXLV2FPT0WU
COLO-684 NIT4fFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r3NmlEPTB;NUKzMlEyKG6P MYHTRW5ITVJ?
PA-1 NHSzTWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ftcWlEPTB;NUOyMlQyKG6P M{DsSXNCVkeHUh?=
MG-63 M4H1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC4SFVwUUN3ME21OFEvOTFibl2= MVnTRW5ITVJ?
BHT-101 M{m3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jCemlEPTB;NUS0Mlk1KG6P M1u1cnNCVkeHUh?=
NKM-1 NWHiNnVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPQTWM2OD13OUOuNFkhdk1? MWfTRW5ITVJ?
T47D MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\lbGlEPTB;NUm3MlU3KG6P NEjwem9USU6JRWK=
MOLT-4 NILZb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;EbGlEPTB;NkKzMlYzKG6P M4jJNXNCVkeHUh?=
IGROV-1 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrXbYhKSzVyPU[zOE4{OSCwTR?= M{i4UHNCVkeHUh?=
ES4 NEnqW3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q3b2lEPTB;NkO5MlU1KG6P M2\PcXNCVkeHUh?=
HuO-3N1 NHvQOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPtSYNKSzVyPU[0Nk4{QCCwTR?= M33rfXNCVkeHUh?=
NEC8 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3KwcmlEPTB;NkWzMlU4KG6P MlzjV2FPT0WU
HO-1-N-1 MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XTSGlEPTB;NkW5MlE4KG6P NFL2NohUSU6JRWK=
EPCL-272H NHvVZm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLUV3dwUUN3ME22PFcvOjFibl2= M1;T[HNCVkeHUh?=
D-263MG MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDiTWM2OD15MUiuNUBvVQ>? MkDjV2FPT0WU
MV-4-11 M3\yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\4O215UUN3ME23NlQvOzFibl2= Ml\vV2FPT0WU
SK-NEP-1 MnfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPDTWM2OD15MkWuPVQhdk1? M1nET3NCVkeHUh?=
SW872 M4[4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInwVINKSzVyPUeyO{45QSCwTR?= NHjVTYJUSU6JRWK=
P30-OHK M1ztXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7vU|dKSzVyPUezNE44OSCwTR?= NEftcHRUSU6JRWK=
OMC-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\GTmlEPTB;N{WxMlA6KG6P MnrhV2FPT0WU
LoVo MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLEW3NDUUN3ME23O|cvQSCwTR?= Mn3uV2FPT0WU
LNCaP-Clone-FGC NWjYcZFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTd7Nj6zOEBvVQ>? NHzOOnZUSU6JRWK=
L-363 M1nNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH1bVBNUUN3ME23PVgvPDJibl2= MX;TRW5ITVJ?
ES8 M1zodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\5S21HUUN3ME24NVAvPTJibl2= Mo\vV2FPT0WU
697 NELVZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfYO|lKSzVyPUizNU42PSCwTR?= MV3TRW5ITVJ?
HSC-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLOTWM2OD16M{muOVQhdk1? NFOzdZZUSU6JRWK=
H4 NX7vNJNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTh3MD64OUBvVQ>? NUj2VZF7W0GQR1XS
QIMR-WIL Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfudpZKSzVyPUi2OU4zKG6P NHHyXGpUSU6JRWK=
OAW-42 NXuxSm5DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTh5Mj6xPUBvVQ>? M1zweHNCVkeHUh?=
MCF7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\EcIJKSzVyPUi5PE42QSCwTR?= MX7TRW5ITVJ?
SCC-25 M2ruemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTlzND6xPUBvVQ>? MVfTRW5ITVJ?
NCI-H1563 NVjCUmhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTlzNT65PUBvVQ>? NE\WPVZUSU6JRWK=
OVCAR-5 NHrydnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjBTWM2OD17NECuNVchdk1? Mln6V2FPT0WU
HDLM-2 NGHzfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTl2OT6yJI5O NFfMNWJUSU6JRWK=
NB5 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvxTnJtUUN3ME25OVYvPiCwTR?= NUnES|dXW0GQR1XS
NCI-H292 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTl5ND6zNkBvVQ>? M{mxfXNCVkeHUh?=
A101D NXzve45NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTl7MD6xPUBvVQ>? NY[xZoRYW0GQR1XS
NCI-H1648 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjxUWhKSzVyPUm5PE42OSCwTR?= NIX3OFlUSU6JRWK=
EKVX MnfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwMEGyPUDPxE1? Ml7UV2FPT0WU
SW1710 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1z5dGlEPTB;MT6wOFI{OyEQvF2= NF\WO|FUSU6JRWK=
WM-115 NF;WS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\JOGlEPTB;MT6wOlY2PiEQvF2= MoDSV2FPT0WU
CAL-54 NVTVWFRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjKTWM2OD1zLkC3NFgyKM7:TR?= M1;z[3NCVkeHUh?=
TGBC24TKB NYf1c3YxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS5[|N1UUN3ME2xMlA5ODR3IN88US=> Mn76V2FPT0WU
NCI-H520 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK4PGdKSzVyPUGuNFg6PjdizszN NU\vXJBtW0GQR1XS
D-423MG NH7NVFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFwMEm5OlIh|ryP MmTkV2FPT0WU
BFTC-905 M1Tscmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7TWJBKSzVyPUGuNVM1PDlizszN MYnTRW5ITVJ?
HT NEHtZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvhWolKSzVyPUGuNVM1PzhizszN NYrjTm1YW0GQR1XS
CTB-1 MoXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf5TWM2OD1zLkG0Nlk{KM7:TR?= M1P0O3NCVkeHUh?=
Hs-578-T NFy5XYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrHZVVKSzVyPUGuNVk2PjVizszN MW\TRW5ITVJ?
HuH-7 MoTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPBXHhKSzVyPUGuNlA6PDlizszN Ml;4V2FPT0WU
LB996-RCC NUW5OJVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXXTWM2OD1zLkKyNVc4KM7:TR?= NIC4XJFUSU6JRWK=
KYSE-270 M3z4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwMkm3N|Qh|ryP MonQV2FPT0WU
A4-Fuk MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fwOGlEPTB;MT6yPVk6OyEQvF2= NUPpSII6W0GQR1XS
A498 M4jNOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rwfWlEPTB;MT6zNFQ4PCEQvF2= M{\TN3NCVkeHUh?=
SK-MEL-1 NUjIWmQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHtdpJMUUN3ME2xMlMxPjd7IN88US=> M3T5VHNCVkeHUh?=
AU565 NVvnV|RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEWxdYVKSzVyPUGuN|E5PjNizszN NWXvOHp1W0GQR1XS
Saos-2 Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\PSWlEPTB;MT6zN|IxPSEQvF2= NGjDR4VUSU6JRWK=
A549 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17TNWlEPTB;MT6zPVk4KM7:TR?= NGDaTHRUSU6JRWK=
BFTC-909 NInP[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTsdnRqUUN3ME2xMlQ{OzB3IN88US=> NYriUIxIW0GQR1XS
MDA-MB-415 NEfBWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjBV|dFUUN3ME2xMlQ5Pjl{IN88US=> MmrRV2FPT0WU
639-V MoT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HoUGlEPTB;MT61NFI1PSEQvF2= Mn22V2FPT0WU
A704 NHzTT2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHPepVHUUN3ME2xMlUxPzh3IN88US=> NV;tb4ZGW0GQR1XS
PANC-03-27 M3TsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHpTWM2OD1zLkWxOFA5KM7:TR?= MX;TRW5ITVJ?
SK-MEL-28 MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLsTWM2OD1zLkW2NFg2KM7:TR?= MXjTRW5ITVJ?
Ramos-2G6-4C10 M4fXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFwNkC3OFYh|ryP NVPlOpg1W0GQR1XS
HuP-T4 MmLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILiNFVKSzVyPUGuOlA4PzhizszN MYrTRW5ITVJ?
VA-ES-BJ M4TQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDFTWM2OD1zLk[xNlch|ryP MlLKV2FPT0WU
EFM-19 NWHjeHBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF75XW1KSzVyPUGuOlE5OSEQvF2= M1nNUnNCVkeHUh?=
G-401 NYnuXJlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXMTWM2OD1zLk[yNVY1KM7:TR?= M4[0S3NCVkeHUh?=
D-566MG M{fpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwNkK1N{DPxE1? NGnRWG9USU6JRWK=
JVM-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFwNkS4O|Uh|ryP M3PMdXNCVkeHUh?=
TK10 NFnaPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm5TpNKSzVyPUGuOlcxQDNizszN MYDTRW5ITVJ?
BT-20 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHrVZVKSzVyPUGuOlg6ODJizszN M37DcHNCVkeHUh?=
EGI-1 M4Gw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;qXWlEPTB;MT64OFcxOSEQvF2= Mk\6V2FPT0WU
EW-16 M2\EeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDvbo5KSzVyPUGuPFUyQDJizszN NELyfXdUSU6JRWK=
NCI-H2228 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXMUFdKSzVyPUGuPFUzODNizszN NFXPT25USU6JRWK=
BB49-HNC NFjXNWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vnNmlEPTB;MT64PFY6OiEQvF2= M4fjVnNCVkeHUh?=
G-402 NHu5dFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TjU2lEPTB;MT64PVc6PyEQvF2= NHHC[Y9USU6JRWK=
NCI-H526 NH7YZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S1bWlEPTB;MT65NVM6KM7:TR?= NFPLTW1USU6JRWK=
ME-180 NFm1VYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPMTWM2OD1zLkmzOFc4KM7:TR?= MljmV2FPT0WU
PFSK-1 MnPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwOUS0OVgh|ryP NYDHOXZsW0GQR1XS
TYK-nu M1L6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu4c2FKSzVyPUGuPVU5OjNizszN M2nQTnNCVkeHUh?=
HOS MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHXV4Z{UUN3ME2xMlk4QTR6IN88US=> NF3sVZJUSU6JRWK=
T98G MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLQTWM2OD1zLkm5NFA3KM7:TR?= M4\LXXNCVkeHUh?=
SK-MES-1 NFv5RVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJwMEGzN|Ih|ryP M3fEWXNCVkeHUh?=
SNB75 NEK0T5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPYTWM2OD1{LkCxOVQyKM7:TR?= MoXlV2FPT0WU
LAMA-84 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfVTWM2OD1{LkCyOlg6KM7:TR?= M{XCUXNCVkeHUh?=
CAL-39 NUjEW3EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnzeXNKSzVyPUKuNFMzQCEQvF2= NILRbHpUSU6JRWK=
LOXIMVI M3\FVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJwMESwPFQh|ryP MmfiV2FPT0WU
NH-12 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJwMEW0NlQh|ryP NYrQbVBuW0GQR1XS
NCI-H1048 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[wTWM2OD1{LkGwOVIh|ryP NV\INoRbW0GQR1XS
KS-1 M2LGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJwMUGwNFEh|ryP MU\TRW5ITVJ?
NCI-N87 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\i[WdKSzVyPUKuNVM{QDRizszN MW\TRW5ITVJ?
CHP-212 NILGXoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJwMUi0OFIh|ryP M{P4eHNCVkeHUh?=
HCC1419 Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;yTWM2OD1{LkKxNVE2KM7:TR?= MnPEV2FPT0WU
ES1 NGjoNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLX[VE{UUN3ME2yMlIyOzJ4IN88US=> MmjqV2FPT0WU
NCI-H2030 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\J[nlKSzVyPUKuNlQyOjNizszN NILQN4pUSU6JRWK=
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NCI-H460 NHLJcmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\rZ21OUUN3ME2xNE4zQDB4IN88US=> NX35fVk4W0GQR1XS
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HuCCT1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFzLkGyPFEh|ryP MWHTRW5ITVJ?
RCC10RGB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFzLkGzOUDPxE1? Mo\OV2FPT0WU
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HEC-1 M3KzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;2TWM2OD1zMT60N|I5KM7:TR?= NXO0[JRvW0GQR1XS
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SW982 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX5TWM2OD1zMz64Nlc3KM7:TR?= MmfNV2FPT0WU
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KOSC-2 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOzPZo5UUN3ME2xOk4yOTJ3IN88US=> M{DyNHNCVkeHUh?=
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SNU-C2B MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF5LkCyN|ch|ryP MXvTRW5ITVJ?
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NB13 M1XiW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;3WWlEPTB;MUmuPFg{QSEQvF2= Mo\yV2FPT0WU
UACC-893 NFm0WZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LOUWlEPTB;MUmuPVc2PyEQvF2= M{fhWHNCVkeHUh?=
HT-1197 M2fxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX6TWM2OD1{MD6yPVU5KM7:TR?= NGHSUGdUSU6JRWK=
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HD-MY-Z NH;KfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjUVIJ6UUN3ME2yNU4{Pjl4IN88US=> M4TndnNCVkeHUh?=
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ACHN NX3UZ3dwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2SyPWlEPTB;MkSuOFY2PiEQvF2= M4WweHNCVkeHUh?=
M059J NGC2NIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P4NWlEPTB;MkSuOVY{PCEQvF2= NEXnSpJUSU6JRWK=
AM-38 M4D4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XxcWlEPTB;MkWuOFgyKM7:TR?= M{G5fXNCVkeHUh?=
KG-1 NGnxW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ3LkW0PVQh|ryP M3jrSHNCVkeHUh?=
COLO-824 NUnFSXlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP3TWM2OD1{NT61OVk6KM7:TR?= MYfTRW5ITVJ?
NCI-H1155 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fvXmlEPTB;MkWuOVg1PyEQvF2= MmnMV2FPT0WU
NCI-H441 NV62XHhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTJ3Lke0OlUh|ryP Mn\UV2FPT0WU
J-RT3-T3-5 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJ4LkOwNlch|ryP NYroUlh3W0GQR1XS
JEG-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPhTWM2OD1{Nj62PFA2KM7:TR?= M{TpWnNCVkeHUh?=
RKO NEe5T4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTuNWVKSzVyPUK2Mlc3OzJizszN MnLHV2FPT0WU
CAL-85-1 NX;jU41KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjiNnVQUUN3ME2yO{4zOTF6IN88US=> NX3iZ25wW0GQR1XS
CAL-120 Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GwdWlEPTB;MkeuOlkyPCEQvF2= MWrTRW5ITVJ?
NCI-H2452 MnrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LxOmlEPTB;MkeuO|cyPiEQvF2= Mn;1V2FPT0WU
NCI-H1395 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJ5Lke4N|Mh|ryP MkD4V2FPT0WU
KYSE-450 NX\wNGVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTJ5Lkm4OlIh|ryP MVnTRW5ITVJ?
S-117 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PVPGlEPTB;MkmuN|g2PyEQvF2= M3TTenNCVkeHUh?=
SW13 NYLNe4czT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLjTWM2OD1{OT64OVE6KM7:TR?= NGS4SWZUSU6JRWK=
ES3 M1jFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jlNWlEPTB;M{CuN|c{OyEQvF2= M3i1bnNCVkeHUh?=
HCT-116 MlK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P0XWlEPTB;M{CuOVU2PCEQvF2= M3jUfnNCVkeHUh?=
NCI-H1693 M{\pb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;UOWlEPTB;M{CuOVk1OiEQvF2= MkLYV2FPT0WU
VM-CUB-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTNyLk[0NVMh|ryP MW\TRW5ITVJ?
NCI-H2170 M4W0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rVNGlEPTB;M{GuOVc5PCEQvF2= NHn4[pFUSU6JRWK=
ALL-PO NXzHdHNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlWyTWM2OD1|MT64OFI5KM7:TR?= NUfPdpdpW0GQR1XS
NCI-H661 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPkTWM2OD1|Mj6wOlI{KM7:TR?= NInoRWRUSU6JRWK=
NCI-H2347 M4[wcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIniRoJKSzVyPUOyMlQ5OzdizszN NYfEflFzW0GQR1XS
FTC-133 MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fSTmlEPTB;M{KuO|A3KM7:TR?= NX\EV|hUW0GQR1XS
COLO-829 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHUTWM2OD1|Mz6zOFY4KM7:TR?= NGPmXItUSU6JRWK=
GOTO NFLzNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTN|LkWyOVgh|ryP MYfTRW5ITVJ?
YAPC M33ucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XJUGlEPTB;M{OuPFE2QSEQvF2= M1Hud3NCVkeHUh?=
LCLC-103H M1zENmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTN2LkG2NlQh|ryP MkjFV2FPT0WU
SiHa NIfMT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TVbGlEPTB;M{SuN|gyPyEQvF2= M3HpcHNCVkeHUh?=
LK-2 M13we2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGyTlZbUUN3ME2zOE42PzB6IN88US=> NEPk[5dUSU6JRWK=
KP-N-YS NV\4RVdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN2LkeyNFIh|ryP NWnlRpJWW0GQR1XS
NCI-SNU-1 NVmxUZNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rEVmlEPTB;M{WuNVc6KM7:TR?= NIHvcWpUSU6JRWK=
KNS-81-FD NXLsXplZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTN3Lk[2N{DPxE1? NYO1fWtPW0GQR1XS
SCC-9 M2HEcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnHZllKSzVyPUO2MlcyPDZizszN NH;uSo9USU6JRWK=
SH-4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFWxW2ZKSzVyPUO2Mlc{KM7:TR?= NGS1NIZUSU6JRWK=
HCC-1954 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7idIo1UUN3ME2zO{4zPzJ7IN88US=> M2DDUnNCVkeHUh?=
BALL-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O0SGlEPTB;M{euOVMyPiEQvF2= MUDTRW5ITVJ?
BE-13 MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4GzSmlEPTB;M{euO|AyQCEQvF2= MkTYV2FPT0WU
COLO-678 MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN5Lkm0N|ch|ryP NGLldYdUSU6JRWK=
SK-MEL-3 NXj0SY5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LEN2lEPTB;M{iuNlM6PyEQvF2= MXHTRW5ITVJ?
OAW-28 NH;s[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN6Lk[zPUDPxE1? Mnf6V2FPT0WU
CAMA-1 NW\Tb3BnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHLcGJKSzVyPUO4Mlk3QTFizszN MXjTRW5ITVJ?
C2BBe1 NYnnbnBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXaUY9LUUN3ME2zPU45OThizszN MYfTRW5ITVJ?
A3-KAW NH[0[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmzUXBKSzVyPUSwMlM3PjFizszN MV3TRW5ITVJ?
SK-MEL-24 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPDWJhKSzVyPUSwMlU6OzFizszN NVf2PGk4W0GQR1XS
KYSE-140 M{W3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLwTWM2OD12MD63NVY2KM7:TR?= NWXaT49FW0GQR1XS
MOLT-16 MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\5VFFKSzVyPUSxMlE2OzZizszN MoHUV2FPT0WU
CFPAC-1 NXf0NYFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjkTWM2OD12Mj61NlEyKM7:TR?= NHzlXm9USU6JRWK=
NB14 NXHPWW0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTR{LkewNlch|ryP MnfNV2FPT0WU
COLO-792 M1vqZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPMZWVKSzVyPUSyMlg6PjFizszN M3jQbXNCVkeHUh?=
RH-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTR|LkS4N|Yh|ryP NVHQR4VpW0GQR1XS
NCI-H522 NGPhbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjt[JpKSzVyPUS0MlM2PjhizszN M1zxUnNCVkeHUh?=
Ca-Ski M3LEUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4cGlEPTB;NESuPFEyPCEQvF2= M3vvTnNCVkeHUh?=
KGN NX\5d5dLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjwT4dVUUN3ME20PE4{ODZ|IN88US=> MkL2V2FPT0WU
UACC-62 NYW1[Iw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTR6LkSwO|Ih|ryP M1;JNHNCVkeHUh?=
NCI-H358 NFLjcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\TcYw4UUN3ME20PU4{ODF6IN88US=> M4KwVXNCVkeHUh?=
LS-411N M3WxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG5R4h{UUN3ME20PU4{OTF6IN88US=> MkfvV2FPT0WU
IST-MES1 M2DpWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi3NXJKSzVyPUS5MlU3OjVizszN NYC1b4tzW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase I study of GDC-0941 in patients with locally advanced or metastatic solid tumors, Non-Hodgkin's lymphoma, or multiple myeloma (MM) (expansion stage only) for which standard therapy either does not exist or has proven ineffective or intolerable is
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [2]

細胞株 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
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 48 and 72 hours
実験の流れ 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.

動物実験: [2]

動物モデル NCR nude mice implanted with MDA-MB-361.1 cells, and SCID, C.B-17/IcrHsd-Prkdcscid mice implanted subcutaneously with BT474-M1 cells
製剤 Dissolved in 10% DMSO, 5% Tween 20, 85% water
投薬量 ~150 mg/kg/day
投与方法 Oral gavage

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 Pictilisib (GDC-0941) SDF
分子量 513.64
化学式

C23H27N7O3S2

CAS No. 957054-30-7
保管 2年-20℃
6月-80℃in solvent
別名 RG7321
溶解度 (25°C) * In vitro DMSO 44 mg/mL (85.66 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 2% 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-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidine

カスタマーフィードバック (7)


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Rating
Source Cancer Res, 2011, 71, 2750-2760. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot, Immunofluorescence staining, flow cytometry
Cell Lines 1205Lu cells
Concentrations 3 µmol/L
Incubation Time 48 h
Results Combined PI3K and BRAF inhibition increased the level of BIM expression in both Western blot and immunofluorescence studies (Fig. A). Consistent with a role for increased AKT signaling suppressing BIM expression in PTEN- cells, dual BRAF and PI3K inhibition increased nuclear FOXO3a localization in the PTEN- cell lines (Fig. B) and enhanced the level of BIM mRNA (Fig. B). the combination of PLX4720 with the PI3K inhibitor GDC-0941 significantly enhanced the levels of apoptosis observed in PTEN melanoma cell lines compared to either the BRAF or PI3K inhibitor alone (Fig. C). Similar results were also observed in a 3D spheroid assay, where combined PLX4720 (3 µmol/L) and LY294002 (10 µmol/L) treatment prevented the recovery of cell growth observed when melanoma spheroids were treated with either drug alone (Fig. D).

Click to enlarge
Rating
Source J Inves Der, 2010, 131, 495-503. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines Mel-Juso cells, 518A2 cells
Concentrations 0.05–1 µmol/L
Incubation Time 24 h
Results In addition, GDC-0941 treatment blocked the phosphorylation of AKT protein (S473 and T308) at even lower concentrations than PI-103, and S6 protein phosphorylation was blocked at similar concentrations.

Click to enlarge
Rating
Source J Cell Sci, 2012, 125(Pt 5), 1259-73. Pictilisib (GDC-0941) purchased from Selleck
Method Western Blot
Cell Lines NMuMG cells
Concentrations 1 μM
Incubation Time 1 h
Results GDC-0941, a specific inhibitor of the class IA PI3K, similarly blocked the TGF-b-induced Akt(S473) phosphorylation, confirming the role of PI3K in the induction of mTORC2 kinase activity by TGF-β (Fig. C).

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Rating
Source Dr. Zhang of Tianjin Medical University. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-10 nM
Incubation Time 3 h
Results

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Rating
Source Saraswati Sukumar of Johns Hopkins University School of Medicine. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results

Click to enlarge
Rating
Source Biochim Biophys Acta, 2012, 1823, 2210-6. Pictilisib (GDC-0941) purchased from Selleck
Method confocal laser-scanning microscopy
Cell Lines HEK293 cells
Concentrations 1 μM
Incubation Time 30 min
Results Both LY294002 and GDC-0941 markedly attenuated the high-glucose-dependent plasma membrane translocation of DGKδ1, indicating that the event is positively regulated by phosphatidylinositol 3-kinase.

Click to enlarge
Rating
Source Pictilisib (GDC-0941) purchased from Selleck
Method Western blot analysis
Cell Lines MCF-7 cells
Concentrations 0 nM/50 nM/100 nM/400 nM
Incubation Time 24 h
Results GDC-0941 caused a surprising increase in phosphorylation of ERK proteins as well as AKT2 S474. GDC-0941 showed differences in its ability to suppr ess PI3K-dependent signaling across the genotypes. AKT1 mutant cells demonstrated greater residual AKT1 S473 phosphorylation and greater phosphorylation of downstream proteins FOXO 1/3, PRAS40, GSK3β , and p70S6K at equivalent doses of GDC-0941, compared to PIK3CA mutant cells.

文献中の引用 (57)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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