Pictilisib (GDC-0941)

Catalog No.S1065 Synonyms: RG7321

Pictilisib (GDC-0941) Chemical Structure

Molecular Weight(MW): 513.64

Pictilisib (GDC-0941) 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). Phase 2.

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Cited by 294 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description Pictilisib (GDC-0941) 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). 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 M4nqVmtqdmG|ZTDBd5NigQ>? MmHDNUBp NHPFeVhFVVOR M4PBemlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= NWPIfphjOTh5NUS2OVQ>
Sf9 M3\hXmtqdmG|ZTDBd5NigQ>? NHv1SVIyKGh? NVjPflQ2TE2VTx?= M1TvTWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBJOTB2Nz3SJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO MnzFNVg4PTR4NUS=
Sf9 MYjLbY5ie2ViQYPzZZk> NWPme3M1OSCq MoTySG1UVw>? MYjJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN M3ziN|E5PzV2NkW0
Sf9 MYPLbY5ie2ViQYPzZZk> M1fq[VEhcA>? NXP1W3J{TE2VTx?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMEOzJO69VQ>? MlPXNVg4PTR4NUS=
Sf9 NWPuTWo3U2mwYYPlJGF{e2G7 MYSxJIg> NH3jeGdFVVOR NWfpUIFvUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[Q>? NYruTGx6OTh5NUS2OVQ>
MDA-MB-361 M2fNXmZ2dmO2aX;uJGF{e2G7 MnXqNkBp MYTEUXNQ NUn6NWs2UW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO MX:xPFc2PDZ3NB?=
PC3 MVTGeY5kfGmxbjDBd5NigQ>? M1HHUFIhcA>? MVfEUXNQ NHG5V21KdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? MUKxPFc2PDZ3NB?=
U87MG MVjGeY5kfGmxbjDBd5NigQ>? NXLsW2V2OiCq NFf6UYtFVVOR NF7GWHpKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFnDOVAhd2ZiMD6wOFYh|ryP M4TidlE5PzV2NkW0
MDA-MB-361 M1X4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm5OkBp NV:xNGtUTE2VTx?= NUHEdm9XSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC55MjFOwG0> MYSxPFc2PDZ3NB?=
A2780 M2n1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\Velk3KGh? MkTNSG1UVw>? NXLRTJg1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= MX:xPFc2PDZ3NB?=
PC3 M364V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHWNIlRQTZiaB?= MnXLSG1UVw>? M3j4SmlEPTB;MD6yPEDPxE1? NYLrUY5kOTh5NUS2OVQ>
U87MG NIPacZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG5OkBp NU[zc2pmTE2VTx?= NW\6bFhOUUN3ME2wMlk2KM7:TR?= MY[xPFc2PDZ3NB?=
Sf9 MmPyT4lv[XOnIFHzd4F6 MYmzNEBucW5? NVLseXBwTE2VTx?= MlvKTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= MnnLNlI2PDh|NEK=
RAW 264.7 MnT6T4lv[XOnIFHzd4F6 NWTzSXk2QTBibXnu M4\jc2ROW09? NFO5NpJKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> MmHaNlI2PDh|NEK=
Sf9 NHX5cINMcW6jc3WgRZN{[Xl? MV:xJIg> M2HOd2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tj\XSjIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVRkmgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODF5IN88US=> MXGyN|U1ODZ2NR?=
Sf9 M2nkZmtqdmG|ZTDBd5NigQ>? MXqxJIg> Mnn5TY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= MUeyN|U1ODZ2NR?=
Sf9 MoLaT4lv[XOnIFHzd4F6 MkHUNUBp MUnJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[4FudWFiZYjwdoV{e2Wm M1\2[lI{PTRyNkS1
Sf9 M4H3T2tqdmG|ZTDBd5NigQ>? NWnlZ|hmOSCq MoDwTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZB?= NYnySXpnOjN3NEC2OFU>
SKOV3 MVzLbY5ie2ViQYPzZZk> NFy1dXkyKM7:TR?= NELWcpcyKGh? NHSzUG5FVVOR NEHCVXhKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w NWi1XYVIOjN|NkCzOFg>
MCF7 NGjVNXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHlNUDPxE1? NUDNVpZsQTZiaB?= M3rhW2ROW09? NEjnOVdIUTVyPUCuNFcxOiEQvF2= NX;V[np5OjN|NkCzOFg>
SKOV3 M2DpSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7aUIkyKM7:TR?= M1fEXlk3KGh? MnvOSG1UVw>? MoizS2k2OD1yLkG0O|Yh|ryP M2\PWVI{OzZyM{S4
PC3 NV7iPJUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjFRmRHPzJiaB?= M3L3bWROW09? M3i3S2lEPTB;MD6yPEDPxE1? NHf6VmwzOTl6MUexOC=>
MCF7.1 NX3nfFBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH0[2FRPzJiaB?= MXTEUXNQ M2DtfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochUEWUMjDn[Y5mKHerdHigTWM2OCCxZjCwMlI5KM7:TR?= NF3McpEzOTl6MUexOC=>
MCF7-neo/Her2 M{TOd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S3cFczKGh? MnTESG1UVw>? NF\1S5NKSzVyPUCuNlkh|ryP NFPRZnMzOzZ4MkmwNy=>
MCF7-neo/Her2 NVniSINUU2mwYYPlJGF{e2G7 M1LjPWlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> M3SzOVI{PjZ{OUCz
PC3 NXHLU41IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES1ZZQ4OiCq MoiySG1UVw>? NHfBdGNGSzVyPUCuN|Qh|ryP M4C4XVIyQTh3NkO5
MCF7.1 M2rVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XJWlczKGh? NX3pPGNjTE2VTx?= MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCHQ{WwJI9nKDBwM{mg{txO M1L3[|IyQTh3NkO5
PC3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13wVVczKGh? NFPIWINFVVOR M{LBZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> NEfKPYkzODB3ME[2PS=>
MCF7.1 NEjYTZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nrUFczKGh? M1PBRWROW09? Mn65RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? M4TrfFIxODVyNk[5
MCF7.1 NYH2OXF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVK3NkBp MoPaSWM2OD1yLkeyJO69VQ>? NVzsZW1uOjB|NE[2OVY>
NCI-H1975 MnW0R5l1d3SxeHnjJGF{e2G7 NFfpdYo4OiCq MVrJR|UxRTBwMkeg{txO MofxNlMxPTl3NEW=
H460 M{PHPGN6fG:2b4jpZ{BCe3OjeR?= M{ja[lczKGh? NHnUSmxKSzVyPUCuPFch|ryP NXTyblQ3OjNyNUm1OFU>
HT-29 NIXGfmFEgXSxdH;4bYMhSXO|YYm= NFzRTWg4OiCq NVzRXXhIUUN3ME2wMlY3KM7:TR?= NFLKUVIzOzB3OUW0OS=>
HepG2 MljnR5l1d3SxeHnjJGF{e2G7 M{C3OVczKGh? M{\1UmlEPTB;MTFOwG0> MWiyN|A2QTV2NR?=
SGC7901 MXPDfZRwfG:6aXOgRZN{[Xl? MYO3NkBp NG[4UHpKSzVyPUGuPEDPxE1? MVqyN|A2QTV2NR?=
NCI-H226 MmXSR5l1d3SxeHnjJGF{e2G7 NXXyfol[PzJiaB?= M2D3UGlEPTB;Mj65JO69VQ>? NE\HbIQzOzB3OUW0OS=>
A549 MVPDfZRwfG:6aXOgRZN{[Xl? NIHkUXU4OiCq M2WwUWlEPTB;Nj65JO69VQ>? NUfUcIZbOjNyNUm1OFU>
U87MG NYrDbJU4S3m2b4TvfIlkKEG|c3H5 NWDWVnRGPzJiaB?= NVu2fld3UUN3ME23Mlc4KM7:TR?= NHfQbYczOzB3OUW0OS=>
HBC4 NIfQbHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHsc4dIUTVyPT22MlA{KE1? M4HnblIzOzN4MkS2
BSY1 NID4bnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnGclRXdG:pR1m1NF0uPi57MDDN NHL2NmIzOjN|NkK0Oi=>
HBC5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfyeWltd2eJSUWwQU03NjZyIF2= M{C5dFIzOzN4MkS2
MCF7 M{DKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L3d4xw\0eLNUC9MVcvOzNiTR?= M1PndlIzOzN4MkS2
MDA-MB-231 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nOfYxw\0eLNUC9MVUvPDZiTR?= MX:yNlM{PjJ2Nh?=
U251 NIHlUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrMcI9oT0l3ME2tOU42OCCP M1exNFIzOzN4MkS2
SF268 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\BcI9oT0l3ME2tOU4{QSCP MnjtNlI{OzZ{NE[=
SF295 NF\4bINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHHNYVRdG:pR1m1NF0uPi5|NzDN MnzMNlI{OzZ{NE[=
SF539 M{jX[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\sc4dIUTVyPT22MlUxKE1? M{jRdVIzOzN4MkS2
SNB75 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml31cI9oT0l3ME2tO{4yOCCP M1H4N|IzOzN4MkS2
SNB78 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnOycI9oT0l3ME2tOk42OiCP MWOyNlM{PjJ2Nh?=
HCC2998 NFHvO2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHsc4dIUTVyPT22MlI6KE1? M1Hje|IzOzN4MkS2
KM12 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[zU|JbdG:pR1m1NF0uPS55NjDN NYrZTm9NOjJ|M{[yOFY>
HT-29 M4fFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;sc4dIUTVyPT22MlMxKE1? MYOyNlM{PjJ2Nh?=
HCT15 NIrTUo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEGyWYhtd2eJSUWwQU03NjF{IF2= NGixWYQzOjN|NkK0Oi=>
HCT116 NYjRUFc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHIcm5ndG:pR1m1NF0uPS56NzDN Mnu0NlI{OzZ{NE[=
NCI-H23 MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmydYVtd2eJSUWwQU02Njd|IF2= MmLDNlI{OzZ{NE[=
NCI-H226 NWnq[lJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;sc4dIUTVyPT22MlIyKE1? NH\xSIMzOjN|NkK0Oi=>
NCI-H522 NWXNU4xYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTsc4dIUTVyPT22MlU5KE1? MXyyNlM{PjJ2Nh?=
NCI-H483 NE\UVoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXRcI9oT0l3ME2tOk42PiCP NYrYcohTOjJ|M{[yOFY>
A549 M3zveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MomycI9oT0l3ME2tOk4yPSCP NUHofXN3OjJ|M{[yOFY>
DMS273 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DKS4xw\0eLNUC9MVYvPDNiTR?= MWKyNlM{PjJ2Nh?=
DMS114 NID5cZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPacI9oT0l3ME2tOU46OiCP MmfiNlI{OzZ{NE[=
LOXIMVI MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0ZYxw\0eLNUC9MVYvOjliTR?= NYDmVYFROjJ|M{[yOFY>
OVCAR3 M1nSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jMfYxw\0eLNUC9MVYvPzFiTR?= NGr2O|IzOjN|NkK0Oi=>
OVCAR4 NEXobHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4izfoxw\0eLNUC9MVUvPzZiTR?= MYiyNlM{PjJ2Nh?=
OVCAR5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL5cI9oT0l3ME2tOk4zPiCP MkDGNlI{OzZ{NE[=
OVCAR8 NUHONJA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnsc4dIUTVyPT21Mlc{KE1? NGLGUXkzOjN|NkK0Oi=>
SKOV3 NFu0blRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\sc4dIUTVyPT22MlUzKE1? MWeyNlM{PjJ2Nh?=
RXF631L MljvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\obYsxdG:pR1m1NF0uPi56ODDN NUTNe4I2OjJ|M{[yOFY>
ACHN M1LaR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjpS|dtd2eJSUWwQU03NjB5IF2= MX:yNlM{PjJ2Nh?=
St-4 NFXtW4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT3fYdPdG:pR1m1NF0uPS53NjDN NF:5cZgzOjN|NkK0Oi=>
MKN1 NW\ZXIl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz4cI9oT0l3ME2tO{4xQCCP MYmyNlM{PjJ2Nh?=
MKN7 M3P3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jqOIxw\0eLNUC9MVYvPTBiTR?= NGS1TYYzOjN|NkK0Oi=>
MKN28 NEHEbXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL3WWJtd2eJSUWwQU02NjV{IF2= NGL5PZEzOjN|NkK0Oi=>
MKN45 NYH3W5VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfLW2Jtd2eJSUWwQU03NjV3IF2= MkXINlI{OzZ{NE[=
MKN74 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHftNnhtd2eJSUWwQU03NjB{IF2= MVOyNlM{PjJ2Nh?=
DU145 MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4q4UYxw\0eLNUC9MVUvQDViTR?= NH3hU44zOjN|NkK0Oi=>
PC3 NXjCR5B3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nXTYxw\0eLNUC9MVYvPjZiTR?= Mln6NlI{OzZ{NE[=
ES5 M2TGTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLMNmtlUUN3ME21NE4zOSCwTR?= M{fHWXNCVkeHUh?=
HH NVHWTpAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK0WZJvUUN3ME2xNVEvODhibl2= M2H3UHNCVkeHUh?=
MHH-PREB-1 NXHPRm1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDUTWM2OD1zMUSuN{BvVQ>? NXXkXWZZW0GQR1XS
NCI-H1770 NIG2TmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF{Mz64OkBvVQ>? NXe4SWJ4W0GQR1XS
HuO9 NEfaUW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrsdIl[UUN3ME2yNFYvODJibl2= NWPQbopbW0GQR1XS
HAL-01 Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIj3[mVKSzVyPUKwOk44OyCwTR?= Ml\1V2FPT0WU
NOS-1 NYCxbYp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37EcmlEPTB;MkGxMlgzKG6P NGHBVopUSU6JRWK=
HGC-27 NHHY[2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1KwfmlEPTB;MkGyMlU4KG6P NGfUeGpUSU6JRWK=
NB69 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfwTWM2OD1{NEWuNlchdk1? NGHEZXhUSU6JRWK=
RS4-11 M1;4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP1TWM2OD1{NkGuO|Yhdk1? M1;xXXNCVkeHUh?=
DOK M3TiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIizUFJKSzVyPUOwNU44KG6P NILVXZZUSU6JRWK=
LB2241-RCC MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlftTWM2OD1|MEOuPFQhdk1? NEnTbVBUSU6JRWK=
NCI-H1623 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrCbJl[UUN3ME2zNFQvODhibl2= NH;INFVUSU6JRWK=
YH-13 NFjvNodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf0RoxFUUN3ME2zNFQvOzJibl2= M13YSHNCVkeHUh?=
BPH-1 Mk\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1e4emlEPTB;M{G0JI5O MWHTRW5ITVJ?
AN3-CA MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTN2MD6zO{BvVQ>? NITKeYRUSU6JRWK=
ES7 NF:2NnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnmdolKSzVyPUO0NU46QSCwTR?= MXXTRW5ITVJ?
MDA-MB-175-VII NXvRWnMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\XVWh4UUN3ME2zOVIvQTJibl2= M{O4bXNCVkeHUh?=
GAMG M4LFWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2OwVmlEPTB;M{ewMlg2KG6P MULTRW5ITVJ?
CHL-1 NUDYe3BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\q[lVKSzVyPUO3PE43PSCwTR?= MXXTRW5ITVJ?
NB7 M{L3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7DXWZIUUN3ME2zPFkvQDNibl2= NXLBSWZ4W0GQR1XS
MFE-280 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjBXGNKSzVyPUSxPE4zKG6P M1P2UnNCVkeHUh?=
HL-60 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH6zUHJKSzVyPUSyOU44PSCwTR?= MVnTRW5ITVJ?
GCIY NVv5eHdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTR|Mz64JI5O M{OzcnNCVkeHUh?=
MDA-MB-361 MnTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTSTWM2OD12M{muNVMhdk1? MYfTRW5ITVJ?
LXF-289 MnfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv6TWM2OD12NEiuNlchdk1? M1LxPHNCVkeHUh?=
NBsusSR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLMRW9OUUN3ME20PFgvQDVibl2= NUPaNmpzW0GQR1XS
KU-19-19 M3W0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDQOWFpUUN3ME21NVYvODdibl2= MV;TRW5ITVJ?
A204 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37yR2lEPTB;NUKyMlM{KG6P MY\TRW5ITVJ?
LB1047-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTV{Mj65N{BvVQ>? MVHTRW5ITVJ?
COLO-684 MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHxTWM2OD13MkOuNVEhdk1? MX\TRW5ITVJ?
PA-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjwTWM2OD13M{KuOFEhdk1? Mne4V2FPT0WU
MG-63 MoThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr5WYZRUUN3ME21OFEvOTFibl2= Mli0V2FPT0WU
BHT-101 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTV2ND65OEBvVQ>? M3;UNHNCVkeHUh?=
NKM-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PVWGlEPTB;NUmzMlA6KG6P NV7EVmpIW0GQR1XS
T47D NHfYXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTV7Nz61OkBvVQ>? NX\PSYRpW0GQR1XS
MOLT-4 NIHzR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTZ{Mz62NkBvVQ>? MkXFV2FPT0WU
IGROV-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXUTWF[UUN3ME22N|QvOzFibl2= MlqyV2FPT0WU
ES4 M2nrd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTFWHJ6UUN3ME22N|kvPTRibl2= MXrTRW5ITVJ?
HuO-3N1 NWTKZYptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTLTWM2OD14NEKuN|ghdk1? NGPIbHNUSU6JRWK=
NEC8 NUKyeWxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\ZfGlEPTB;NkWzMlU4KG6P NF3mRndUSU6JRWK=
HO-1-N-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr5TWM2OD14NUmuNVchdk1? NEDEPGtUSU6JRWK=
EPCL-272H NXXqSIdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXewT2pLUUN3ME22PFcvOjFibl2= M{PHV3NCVkeHUh?=
D-263MG M132fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofPTWM2OD15MUiuNUBvVQ>? NGrn[opUSU6JRWK=
MV-4-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTd{ND6zNUBvVQ>? MmrpV2FPT0WU
SK-NEP-1 NXHQW3c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTd{NT65OEBvVQ>? NGS0[4lUSU6JRWK=
SW872 NYf4NlVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnX[XlKSzVyPUeyO{45QSCwTR?= MYXTRW5ITVJ?
P30-OHK NH60d41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTd|MD63NUBvVQ>? NVLkbmRqW0GQR1XS
OMC-1 NVzXRYlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDJTWM2OD15NUGuNFkhdk1? M3H5R3NCVkeHUh?=
LoVo M3TTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;iNpNKSzVyPUe3O{46KG6P MUjTRW5ITVJ?
LNCaP-Clone-FGC M4jjN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnrXZVKSzVyPUe5Ok4{PCCwTR?= MmXKV2FPT0WU
L-363 M4PRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;hdXpKSzVyPUe5PE41OiCwTR?= MnLJV2FPT0WU
ES8 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHnPI9HUUN3ME24NVAvPTJibl2= NXL4RYtyW0GQR1XS
697 NWXvUFlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm0fIhFUUN3ME24N|EvPTVibl2= M1r4OnNCVkeHUh?=
HSC-3 M4nPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXVe2JKSzVyPUizPU42PCCwTR?= NFzJcmxUSU6JRWK=
H4 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXLdpNKSzVyPUi1NE45PSCwTR?= M{L4NHNCVkeHUh?=
QIMR-WIL M{nY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPEbJA4UUN3ME24OlUvOiCwTR?= M4XCOXNCVkeHUh?=
OAW-42 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fNSmlEPTB;OEeyMlE6KG6P MYrTRW5ITVJ?
MCF7 NWC3elNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrDW4NKSzVyPUi5PE42QSCwTR?= NVnpOG5OW0GQR1XS
SCC-25 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DYVmlEPTB;OUG0MlE6KG6P M1ewbnNCVkeHUh?=
NCI-H1563 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvyZ5lWUUN3ME25NVUvQTlibl2= MorQV2FPT0WU
OVCAR-5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLEUnlKSzVyPUm0NE4yPyCwTR?= NYW5dpNxW0GQR1XS
HDLM-2 Mn\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r6UmlEPTB;OUS5MlIhdk1? M{nPVnNCVkeHUh?=
NB5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvPeVZKSzVyPUm1Ok43KG6P NH\0fZlUSU6JRWK=
NCI-H292 NF;5bY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPKcpRtUUN3ME25O|QvOzJibl2= M1LBUXNCVkeHUh?=
A101D M2W3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[4XFRKSzVyPUm5NE4yQSCwTR?= NEPGOnlUSU6JRWK=
NCI-H1648 M3nQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zQUmlEPTB;OUm4MlUyKG6P M1\ZSnNCVkeHUh?=
EKVX NWLk[oxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXwOJZKSzVyPUGuNFEzQSEQvF2= NHLxcmNUSU6JRWK=
SW1710 NWe5UJBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPYbFduUUN3ME2xMlA1OjN|IN88US=> NE\2V4lUSU6JRWK=
WM-115 M13XOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HZUmlEPTB;MT6wOlY2PiEQvF2= MmPBV2FPT0WU
CAL-54 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwMEewPFEh|ryP MV7TRW5ITVJ?
TGBC24TKB MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm3TWM2OD1zLkC4NFQ2KM7:TR?= MnXkV2FPT0WU
NCI-H520 MlnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm4TWM2OD1zLkC4PVY4KM7:TR?= Mn6yV2FPT0WU
D-423MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVza[4hSUUN3ME2xMlA6QTZ{IN88US=> NELjPHhUSU6JRWK=
BFTC-905 NGD5boxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwMUO0OFkh|ryP NYPWRlZQW0GQR1XS
HT NUnKdI9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTITWM2OD1zLkGzOFc5KM7:TR?= NEDuOXVUSU6JRWK=
CTB-1 NYSzbIN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\hTWM2OD1zLkG0Nlk{KM7:TR?= NXfkdWZjW0GQR1XS
Hs-578-T MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrqTWM2OD1zLkG5OVY2KM7:TR?= M4Kzb3NCVkeHUh?=
HuH-7 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPqeIxSUUN3ME2xMlIxQTR7IN88US=> MWDTRW5ITVJ?
LB996-RCC NH\zW3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjoTWM2OD1zLkKyNVc4KM7:TR?= NWrCN|YzW0GQR1XS
KYSE-270 M{K0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfyTWM2OD1zLkK5O|M1KM7:TR?= M3z1PHNCVkeHUh?=
A4-Fuk MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFwMkm5PVMh|ryP NVX4R4p1W0GQR1XS
A498 NEP3R4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfHSYlKSzVyPUGuN|A1PzRizszN NInBVm5USU6JRWK=
SK-MEL-1 NVr5ZopET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;kTWlEPTB;MT6zNFY4QSEQvF2= M3\BR3NCVkeHUh?=
AU565 NUjMXldIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwM{G4OlMh|ryP NUW4RlRGW0GQR1XS
Saos-2 NXrUbYlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTFwM{OyNFUh|ryP NUfUU2pjW0GQR1XS
A549 NX\LbJZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfFV5hCUUN3ME2xMlM6QTdizszN NF7YXVlUSU6JRWK=
BFTC-909 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLncVNxUUN3ME2xMlQ{OzB3IN88US=> NUnoeYxFW0GQR1XS
MDA-MB-415 M1PUVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nxPWlEPTB;MT60PFY6OiEQvF2= M4fqcHNCVkeHUh?=
639-V NEew[2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPkXZBKSzVyPUGuOVAzPDVizszN MWTTRW5ITVJ?
A704 NF\Ue|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn31TWM2OD1zLkWwO|g2KM7:TR?= NGHNS5hUSU6JRWK=
PANC-03-27 M{LRRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnnO3hKSzVyPUGuOVE1ODhizszN MXTTRW5ITVJ?
SK-MEL-28 NXvGeI11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3ReIdEUUN3ME2xMlU3ODh3IN88US=> MXPTRW5ITVJ?
Ramos-2G6-4C10 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPNXJFqUUN3ME2xMlYxPzR4IN88US=> NHXNPFFUSU6JRWK=
HuP-T4 MmDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rkZmlEPTB;MT62NFc4QCEQvF2= MWPTRW5ITVJ?
VA-ES-BJ NY\iOYFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXzU|NKSzVyPUGuOlEzPyEQvF2= MXXTRW5ITVJ?
EFM-19 NGHMXJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwNkG4NUDPxE1? NUSyRWhUW0GQR1XS
G-401 M{K4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfu[JZ6UUN3ME2xMlYzOTZ2IN88US=> MXrTRW5ITVJ?
D-566MG M1exOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LkT2lEPTB;MT62NlU{KM7:TR?= MUjTRW5ITVJ?
JVM-3 M3XMUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTFwNkS4O|Uh|ryP MlPvV2FPT0WU
TK10 M{XZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml32TWM2OD1zLk[3NFg{KM7:TR?= NFXObZZUSU6JRWK=
BT-20 MnX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfTRpNKSzVyPUGuOlg6ODJizszN NH;i[4tUSU6JRWK=
EGI-1 Mn\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\aW|hKSzVyPUGuPFQ4ODFizszN Ml\NV2FPT0WU
EW-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfNTWM2OD1zLki1NVgzKM7:TR?= NWjheIs3W0GQR1XS
NCI-H2228 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2KzOmlEPTB;MT64OVIxOyEQvF2= MWjTRW5ITVJ?
BB49-HNC NVLWVoRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX1VZpjUUN3ME2xMlg5Pjl{IN88US=> NHPhPWlUSU6JRWK=
G-402 M{PSWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLXOGZKSzVyPUGuPFk4QTdizszN MkLqV2FPT0WU
NCI-H526 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOyXmRDUUN3ME2xMlkyOzlizszN MUHTRW5ITVJ?
ME-180 NUDUeFU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\FTWM2OD1zLkmzOFc4KM7:TR?= NILOPGtUSU6JRWK=
PFSK-1 NXfXUXpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\EXWlEPTB;MT65OFQ2QCEQvF2= M123dnNCVkeHUh?=
TYK-nu NEK1eVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n2TmlEPTB;MT65OVgzOyEQvF2= NEXVfFVUSU6JRWK=
HOS Mle1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwOUe5OFgh|ryP NWPiNm0xW0GQR1XS
T98G MkLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTjTWM2OD1zLkm5NFA3KM7:TR?= M3LTVnNCVkeHUh?=
SK-MES-1 NF3PfoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTOTWM2OD1{LkCxN|MzKM7:TR?= NEHlWWVUSU6JRWK=
SNB75 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL5TWM2OD1{LkCxOVQyKM7:TR?= NGi4NppUSU6JRWK=
LAMA-84 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2O2PGlEPTB;Mj6wNlY5QSEQvF2= M2fLO3NCVkeHUh?=
CAL-39 NF\kcFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfRTWM2OD1{LkCzNlgh|ryP MYjTRW5ITVJ?
LOXIMVI M33zUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;iNWVKSzVyPUKuNFQxQDRizszN NFvHTXlUSU6JRWK=
NH-12 MnjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJwMEW0NlQh|ryP NWjYVZdSW0GQR1XS
NCI-H1048 M2mzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;5dVFoUUN3ME2yMlExPTJizszN NIDqVWlUSU6JRWK=
KS-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPTSY9KSzVyPUKuNVExODFizszN MUfTRW5ITVJ?
NCI-N87 NXznN2ZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33FOmlEPTB;Mj6xN|M5PCEQvF2= NV;uNXdWW0GQR1XS
CHP-212 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHySGZjUUN3ME2yMlE5PDR{IN88US=> NWrrS4dCW0GQR1XS
HCC1419 NFn3RVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS5VGpKSzVyPUKuNlEyOTVizszN NGiy[oxUSU6JRWK=
ES1 NVnidppOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfFPGRxUUN3ME2yMlIyOzJ4IN88US=> MXvTRW5ITVJ?
NCI-H2030 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTJwMkSxNlMh|ryP MnjOV2FPT0WU
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HOP-92 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJwN{S3NVch|ryP MULTRW5ITVJ?
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OVCAR-8 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\STWM2OD12LkKyOVQ{KM7:TR?= NVj1PWxnW0GQR1XS
DMS-114 Ml7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\CfG1YUUN3ME20MlI{QDlzIN88US=> NX7PO5R{W0GQR1XS
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NCI-H1355 M37EcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHiTWM2OD12LkW1NVQ3KM7:TR?= M{nL[nNCVkeHUh?=
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A375 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv5[4tGUUN3ME21MlA6OjV4IN88US=> MYnTRW5ITVJ?
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OC-314 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorkTWM2OD13LkO3OFQ1KM7:TR?= MXLTRW5ITVJ?
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CAN M2HsZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTyTWM2OD13LkmyPFIh|ryP M{HoVHNCVkeHUh?=
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KYSE-150 NWXXRohJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTrW4NUUUN3ME22MlEzPDd4IN88US=> M3TiZ3NCVkeHUh?=
RPMI-8866 NEnab3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjBSWRKSzVyPU[uNVkyPjNizszN NF25SXRUSU6JRWK=
SW780 NUHNbXVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3JTWM2OD14LkKwOFIh|ryP Mk\UV2FPT0WU
A388 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrYWG9OUUN3ME22MlI{OTF3IN88US=> NGi1T3JUSU6JRWK=
NCI-H1437 NY\MT4JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHmwTWRKSzVyPU[uNlQxPzNizszN MVTTRW5ITVJ?
NCI-H1755 M165[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\0VGlEPTB;Nj6zOlYyOiEQvF2= NX7YendFW0GQR1XS
LS-123 MoTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3LTWM2OD14LkSwOVIyKM7:TR?= Mn31V2FPT0WU
CaR-1 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTZwNE[zO|Mh|ryP MoX2V2FPT0WU
RT-112 MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfkTWM2OD14Lk[wN|M5KM7:TR?= MnLzV2FPT0WU
CGT M{XJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXKTWM2OD14LkezOlgyKM7:TR?= M{fMS3NCVkeHUh?=
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TI-73 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnoTWM2OD15LkC2Nlg2KM7:TR?= MYHTRW5ITVJ?
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KYSE-510 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfEVYZJUUN3ME23MlA5PDN{IN88US=> NFTwN4FUSU6JRWK=
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LB-831-BLC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLlZZdWUUN3ME2xN{43OjR4IN88US=> NHrKfoJUSU6JRWK=
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SW982 NHnHcHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jwUWlEPTB;MUOuPFI4PiEQvF2= MWrTRW5ITVJ?
DB MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTkOGxSUUN3ME2xN{45Ozh2IN88US=> MYDTRW5ITVJ?
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CAL-72 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF2Lke3PFMh|ryP M3S3NHNCVkeHUh?=
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CAS-1 NXH3W21QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jtfWlEPTB;MUWuNFY3KM7:TR?= MUDTRW5ITVJ?
A2058 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor2TWM2OD1zNT61OlM5KM7:TR?= MkjTV2FPT0WU
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Detroit562 MoTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL1VVQ5UUN3ME2xOU46OTN7IN88US=> MkDBV2FPT0WU
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SF268 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TpW2lEPTB;MU[uOFUzKM7:TR?= NYTPOVRrW0GQR1XS
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NCI-H727 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HScGlEPTB;MUmuN|I6PSEQvF2= NUPmO3E2W0GQR1XS
KP-4 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXHTWM2OD1zOT64OVMyKM7:TR?= NVfYNYYxW0GQR1XS
NB13 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DDXWlEPTB;MUmuPFg{QSEQvF2= M37tT3NCVkeHUh?=
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NCI-H2029 NETB[JFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\LTWM2OD1{MD6zNlY3KM7:TR?= M2fTOXNCVkeHUh?=
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OVCAR-3 NFHt[JVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPINlQxUUN3ME2yNE42QDJ{IN88US=> MX\TRW5ITVJ?
HD-MY-Z NHvQWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi0VJlnUUN3ME2yNU4{Pjl4IN88US=> Ml\qV2FPT0WU
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SCH NXzHSnB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJ{LkS5OkDPxE1? NVXnWYRIW0GQR1XS
KARPAS-299 NGHIT3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ|LkO4PFch|ryP Mo\FV2FPT0WU
NCI-H1650 NGTk[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LXW2lEPTB;MkOuPVI1OSEQvF2= NIHVb5pUSU6JRWK=
ACHN NVH0b2luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ2LkS2OVYh|ryP MoW4V2FPT0WU
M059J M3nOcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zGWGlEPTB;MkSuOVY{PCEQvF2= NGWxXndUSU6JRWK=
AM-38 M{\kZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ3LkS4NUDPxE1? MVPTRW5ITVJ?
KG-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3faRWlEPTB;MkWuOVQ6PCEQvF2= MWnTRW5ITVJ?
COLO-824 NFzTWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLwTWM2OD1{NT61OVk6KM7:TR?= NYTWRW9oW0GQR1XS
NCI-H1155 NYTyOIY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzLW5BQUUN3ME2yOU42QDR5IN88US=> M{LtcHNCVkeHUh?=
NCI-H441 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PzZWlEPTB;MkWuO|Q3PSEQvF2= MVXTRW5ITVJ?
J-RT3-T3-5 MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\T[mlEPTB;Mk[uN|AzPyEQvF2= Moj0V2FPT0WU
JEG-3 MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nsO2lEPTB;Mk[uOlgxPSEQvF2= NWPi[IozW0GQR1XS
RKO NYfNeJZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW3TWM2OD1{Nj63OlMzKM7:TR?= Mm\2V2FPT0WU
CAL-85-1 NV;INGY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3JTG97UUN3ME2yO{4zOTF6IN88US=> Ml7rV2FPT0WU
CAL-120 MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHtTWM2OD1{Nz62PVE1KM7:TR?= MVvTRW5ITVJ?
NCI-H2452 MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ5Lke3NVYh|ryP M4HmUnNCVkeHUh?=
NCI-H1395 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DhfWlEPTB;MkeuO|g{OyEQvF2= MnzlV2FPT0WU
KYSE-450 NEHHe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTWTWM2OD1{Nz65PFYzKM7:TR?= M1HMfXNCVkeHUh?=
S-117 M2nyW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O5b2lEPTB;MkmuN|g2PyEQvF2= NIG0S|lUSU6JRWK=
SW13 M3PrRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHwSXZbUUN3ME2yPU45PTF7IN88US=> NULjN5ptW0GQR1XS
ES3 NEjDNVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nqXWlEPTB;M{CuN|c{OyEQvF2= NWLwO45FW0GQR1XS
HCT-116 NVnHWZJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTaTWM2OD1|MD61OVU1KM7:TR?= M{m1THNCVkeHUh?=
NCI-H1693 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X6PGlEPTB;M{CuOVk1OiEQvF2= NGnYPWZUSU6JRWK=
VM-CUB-1 M{\T[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDONIY2UUN3ME2zNE43PDF|IN88US=> NXzrelV2W0GQR1XS
NCI-H2170 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTyUG1KSzVyPUOxMlU4QDRizszN NYqwUmhSW0GQR1XS
ALL-PO MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL1TWM2OD1|MT64OFI5KM7:TR?= Ml\CV2FPT0WU
NCI-H661 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLZdoZpUUN3ME2zNk4xPjJ|IN88US=> Ml3iV2FPT0WU
NCI-H2347 M1K2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fvRWlEPTB;M{KuOFg{PyEQvF2= NIDVbZpUSU6JRWK=
FTC-133 NYi4eldLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7iVGpOUUN3ME2zNk44ODZizszN NELIbppUSU6JRWK=
COLO-829 NEXKdYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN|LkO0Olch|ryP NHi3fHRUSU6JRWK=
GOTO MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn0TWM2OD1|Mz61NlU5KM7:TR?= M1\QdXNCVkeHUh?=
YAPC MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nIRWlEPTB;M{OuPFE2QSEQvF2= NHfrUVJUSU6JRWK=
LCLC-103H M4eyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;V[oVKSzVyPUO0MlE3OjRizszN M4ewT3NCVkeHUh?=
SiHa M17hXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nFd2lEPTB;M{SuN|gyPyEQvF2= NUToWWJ2W0GQR1XS
LK-2 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTN2LkW3NFgh|ryP MXrTRW5ITVJ?
KP-N-YS NH3tWmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTN2LkeyNFIh|ryP NEXxWnVUSU6JRWK=
NCI-SNU-1 M4fPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN3LkG3PUDPxE1? NGK3Wo9USU6JRWK=
KNS-81-FD M{nmNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTN3Lk[2N{DPxE1? M2K4SXNCVkeHUh?=
SCC-9 M3HPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN4LkexOFYh|ryP NWnIUpM4W0GQR1XS
SH-4 NF2yemdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHNNnBmUUN3ME2zOk44OyEQvF2= NWnhZ3k2W0GQR1XS
HCC-1954 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDtPJBKSzVyPUO3MlI4OjlizszN NEnsW3dUSU6JRWK=
BALL-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTEPHhkUUN3ME2zO{42OzF4IN88US=> MWnTRW5ITVJ?
BE-13 NGj5XpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TBR2lEPTB;M{euO|AyQCEQvF2= NXX3bFdtW0GQR1XS
COLO-678 NGLKN3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN5Lkm0N|ch|ryP NGrjfoFUSU6JRWK=
SK-MEL-3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfjTWM2OD1|OD6yN|k4KM7:TR?= NETSS2xUSU6JRWK=
OAW-28 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTN6Lk[zPUDPxE1? NGH3S2NUSU6JRWK=
CAMA-1 NYG5PGpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH5TWM2OD1|OD65OlkyKM7:TR?= NGC2[npUSU6JRWK=
C2BBe1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULTSoUxUUN3ME2zPU45OThizszN MlLhV2FPT0WU
A3-KAW M1KxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjDcGFKSzVyPUSwMlM3PjFizszN MX3TRW5ITVJ?
SK-MEL-24 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml63TWM2OD12MD61PVMyKM7:TR?= NY[xXG5ZW0GQR1XS
KYSE-140 M4Pse2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zXbmlEPTB;NECuO|E3PSEQvF2= NVf3Z5BEW0GQR1XS
MOLT-16 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPte3BKSzVyPUSxMlE2OzZizszN NYHEXo5oW0GQR1XS
CFPAC-1 NH7RNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSxcIxEUUN3ME20Nk42OjFzIN88US=> MVnTRW5ITVJ?
NB14 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XteGlEPTB;NEKuO|AzPyEQvF2= M1m1e3NCVkeHUh?=
COLO-792 NXvaXVRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV20UWFqUUN3ME20Nk45QTZzIN88US=> MmS4V2FPT0WU
RH-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTR|LkS4N|Yh|ryP NEK3fY1USU6JRWK=
NCI-H522 M161eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\qTWM2OD12ND6zOVY5KM7:TR?= NHLw[JJUSU6JRWK=
Ca-Ski NEOxO5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR2LkixNVQh|ryP M{\jXXNCVkeHUh?=
KGN NHXSTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD6TWM2OD12OD6zNFY{KM7:TR?= M3\CSnNCVkeHUh?=
UACC-62 NVfRRppoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfNd5JKSzVyPUS4MlQxPzJizszN M3vGNHNCVkeHUh?=
NCI-H358 NYPWOFVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInLTG1KSzVyPUS5MlMxOThizszN NXLwZ5lSW0GQR1XS
LS-411N MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHHTWM2OD12OT6zNVE5KM7:TR?= MoDlV2FPT0WU
IST-MES1 M{CwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\yPY46UUN3ME20PU42PjJ3IN88US=> M{XoUXNCVkeHUh?=

... 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]

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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
  • Formulation: Dissolved in 10% DMSO, 5% Tween 20, 85% water
  • 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

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)

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*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 )

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* 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

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  • Computed Result

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Molecular Weight Calculator

Molecular Weight Calculator

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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID