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 58 Publications

8 Customer Reviews

  • Dual PI3K/BRAF inhibition upregulates BIM and enhances apoptosis in PTEN cells. A, left, Western blot of 1205Lu cells treated with PLX4720 (3 μmol/L, 48 hours), the PI3K inhibitor GDC-0941 (3 μmol/L, 48 hours), or both drugs in combination (PtG); right, immunofluorescence staining of BIM (green) and DAPI (blue) in PTEN cells following PLX4720 treatment (3 μmol/L, 48 hours), the PI3K inhibitor LY294002 (10 μmol/L, 48 hours), or both drugs in combination (PLXtLY). B, left, immunofluorescence staining of PTEN 1205Lu following combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48hours) increases nuclear localization of FOXO3a (green). DAPI is shown in blue. Magnification 40. Right, combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48 hours) increases PTEN WM793 BIM mRNA levels to those observed with single BRAF inhibition (3 μmol/L PLX4720, 48 hours) in the PTENt WM35. C, PTEN cells were treated with PLX4720 (3 μmol/L, 48 hours), GDC-0941 (3 μmol/L, 48hours), or a combination of the 2 drugs (3Pt3G) before Annexin-V staining was analyzed by flow cytometry (*, P < 0.05 between the drug combination and each inhibitor alone). D, combined BRAF/PI3K inhibitor treatment blocks the escape of 1205Lu cells (PTEN) from therapy. Spheroids of 1205Lu cells were treated with either PLX4720 alone (3 and 10 μmol/L: data shows 3 mmol/L), LY294002 (10 μmol/L) alone or a combination of the 2 drugs for 72 hours. In other studies, spheroids were treated with drugs for 72 hours and then allowed to recover for 120 hours. Micrograph shows viability staining (green= live cells, red= dead cells). Magnification 10×.

    Cancer Res 2011 71, 2750-2760. Pictilisib (GDC-0941) purchased from Selleck.

    Combination of rapamycin and PI-103 leads to the suppression of AKT phosphorylation (phospho-specific western blot). Mel-Juso and 518A2 cells were treated with GDC-0941 from 0.05–1 μmol/L alone and in combination with rapamycin (50 nmol/L) for 24 hours. Control treatment was with DMSO.

     

     

    J Inves Der 2010 131, 495-503. Pictilisib (GDC-0941) purchased from Selleck.

  • Growth inhibition induced by the FGFR inhibitor BGJ398 and the PI3K inhibitors alone or in combination. AN3CA (A-C), JHUEM2 (D-F) and MFE296 (G-I) cells were treated with the indicated doses of BGJ398, GDC-0941 a n d BYL719 alone or in combination for 96 hours and an Sulforhodamine B (SRB) assay was subsequently performed. Data are presented as a percentage of the control, in which cells were treated with 0.1% (v/v) DMSO. Points represent the mean of three independent experiments (each performed in triplicate). Error bars represent the standard error of the mean (SEM) and lines were fitted using non-linear regression analysis. Interaction of BGJ398 and GDC-0941(redcircles) or BYL719(blacksquares) in AN3CA(C), JHUEM2(F) and MFE296(I). Median effect analysis was used to evaluate the interaction between the inhibitor combinations. Horizontal dotted lines indicate the boundaries for each interaction classification.

    Mol Cancer Ther, 2017.. Pictilisib (GDC-0941) purchased from Selleck.

    TGF-β induces mTORC2 activation. ( A ) NMuMG cells were treated with TGF-β for the indicated times before lysis and immunoblotting. (B ) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to anti-Rictor immunoprecipitation, and the immunoprecipitates were subjected to in vitro kinase assays using kinase-inactive Akt1 as a substrate, before immunoblotting of the kinase reactions, immunoprecipitates and cell lysates. The left panels are from the same gel, without differential exposure. ( C ) NMuMG cells were treated or not with TGF-β or insulin for the indicated times, in the presence or absence of SB431542 or GDC-0941. The kinase activity of mTORC2 was then assessed as in B. The top panels are from the same gel, without differential exposure. (D) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to immunoprecipitation using Rictor antibody, and/or immunoblotted.

    J Cell Sci 2012 125(Pt 5), 1259-73. Pictilisib (GDC-0941) purchased from Selleck.

  • Effects of LY294002 and GDC-0941 on the high-glucose-induced plasma membrane translocation of DGK δ1. (A, C) HEK293 cells were transfected with pAcGFP-DGKδ1 or pAcGFP-C1 vector. After being glucose-starved for 2.5 h and the subsequent pretreatment with (A) 10 μM LY294002 (Sigma-Aldrich) or (C) 1 μM GDC-0941 (Selleck Chemicals) for 30 min, the cells were incubated with or without high glucose (25 mM) for 5 min. The cells were fixed with 3.7% formaldehyde and observed using confocal laser-scanning microscopy. Scale bar = 10 μm. (B, D) After treatment with (B) LY294002 or (D) GDC-0941, the percentages of cells exhibiting the translocation of AcGFP-tagged DGK δ 1 to the plasma membrane were scored. More than 20 cells ex-pressing AcGFP-tagged DGK δ1 were counted in each experiment. The results are the means ± S.D. of three independent experiments. The statistical significance was deter-mined using Student's t -test (** P < 0.01, *** P < 0.005)

    Biochim Biophys Acta 2012 1823, 2210-6. Pictilisib (GDC-0941) purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of GDC-0941  for 3h,followed by 15-minute  stimulation of 100ng/ml EGF.

     

     

     

    Dr. Zhang of Tianjin Medical University. Pictilisib (GDC-0941) purchased from Selleck.

  • We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

     

     

    Saraswati Sukumar of Johns Hopkins University School of Medicine. Pictilisib (GDC-0941) purchased from Selleck.

     

    PI3K pathway signaling in GDC-0941 and MK-2206 treated MCF-7 derivatives with PIK3CA or  AKT1 mutations. Cells were grown in medium containing 5% FBS and treated with vehicle or increasing concentrations of GDC-0941 (0 nM, 50 nM, 100 nM, and 400 nM) or MK-2206 (0 nM, 100 nM, 250 nM, 1000 nM). After 24 hours of drug treatment, lysates were prepared and equal amounts of protein were load ed onto SDS-PAGE gels and blotted with the indicated antibodies.

    Pictilisib (GDC-0941) purchased from Selleck.

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 MoHQT4lv[XOnIFHzd4F6 NXXUXJJrOSCq M1LKV2ROW09? MYjJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGSnbIThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? M{\4UVE5PzV2NkW0
Sf9 MYXLbY5ie2ViQYPzZZk> MV2xJIg> NWTMRm5{TE2VTx?= MoLlTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGgyODR5LWKgcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> MmjtNVg4PTR4NUS=
Sf9 NF:ydHBMcW6jc3WgRZN{[Xl? MVOxJIg> MYfEUXNQ MVXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN NGjG[24yQDd3NE[1OC=>
Sf9 MXnLbY5ie2ViQYPzZZk> MnzGNUBp MXHEUXNQ M1LSfmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wN|Mh|ryP NVf3RlhEOTh5NUS2OVQ>
Sf9 Mn\BT4lv[XOnIFHzd4F6 NEjFSW4yKGh? MWHEUXNQ MUHJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGGucHjhJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjh MXWxPFc2PDZ3NB?=
MDA-MB-361 M4\oN2Z2dmO2aX;uJGF{e2G7 MkTtNkBp MoD0SG1UVw>? NIi1cphKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{ODFOwG0> NGHrcXkyQDd3NE[1OC=>
PC3 M1HFOGZ2dmO2aX;uJGF{e2G7 NEj3dlYzKGh? NVLGVolwTE2VTx?= NYDT[2U{UW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gVGM{KGOnbHzzJJdqfGhiSVO1NEBw\iByLkCzO{DPxE1? MWKxPFc2PDZ3NB?=
U87MG NWHXU2JuTnWwY4Tpc44hSXO|YYm= M3XLOVIhcA>? M1nRVWROW09? Mn6wTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? MlGwNVg4PTR4NUS=
MDA-MB-361 NF7lXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn1TpQ6PiCq MkXRSG1UVw>? NI\SdJdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> Ml\yNVg4PTR4NUS=
A2780 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LZUlk3KGh? Mlr3SG1UVw>? NWn4ZopmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= M3myfVE5PzV2NkW0
PC3 NE\pSXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e0[lk3KGh? NXHrUmFXTE2VTx?= NEnLVllKSzVyPUCuNlgh|ryP MVWxPFc2PDZ3NB?=
U87MG NV[yOWg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHTbpVmQTZiaB?= Mly3SG1UVw>? M3P2O2lEPTB;MD65OUDPxE1? NGL1[3kyQDd3NE[1OC=>
Sf9 NXnJdVlPU2mwYYPlJGF{e2G7 NGfnNGw{OCCvaX6= NFTRe2ZFVVOR NITLSVJKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgZY1wfW62IH;mJGFVWCClb37zeY1m\CC5aYToJGlEPTBib3[gNE4xPDJizszN M3HvclIzPTR6M{Sy
RAW 264.7 M3jje2tqdmG|ZTDBd5NigQ>? M4TDPVkxKG2rbh?= M3XtfWROW09? MUfJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlI6QCEQvF2= NUPiWWRKOjJ3NEizOFI>
Sf9 NEHjXXFMcW6jc3WgRZN{[Xl? NFrHbYIyKGh? NIXrV|BKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> MomxNlM2PDB4NEW=
Sf9 MUHLbY5ie2ViQYPzZZk> M1y4WVEhcA>? M{HWTmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= NGT0TJQzOzV2ME[0OS=>
Sf9 Mn\aT4lv[XOnIFHzd4F6 NXf5OFFoOSCq M4D6V2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= MlL2NlM2PDB4NEW=
Sf9 M3;hWWtqdmG|ZTDBd5NigQ>? NIi1RogyKGh? M3f6bGlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXS= NFTFZlMzOzV2ME[0OS=>
SKOV3 M2DJOmtqdmG|ZTDBd5NigQ>? M4LweFEh|ryP NHvOZm8yKGh? MUfEUXNQ MofHTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? MVOyN|M3ODN2OB?=
MCF7 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvWXWoyKM7:TR?= MmS5PVYhcA>? M4DLPGROW09? MV;HTVUxRTBwMEewNkDPxE1? NYKzWZh1OjN|NkCzOFg>
SKOV3 NV\aXZJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxJO69VQ>? NWLOVVdJQTZiaB?= M2nUNmROW09? NEWwVI9IUTVyPUCuNVQ4PiEQvF2= MkTRNlM{PjB|NEi=
PC3 M4fiRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr3OVk4OiCq NFj5NXNFVVOR M3rNbWlEPTB;MD6yPEDPxE1? M{Lpb|IyQThzN{G0
MCF7.1 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzUV2c4OiCq M3jLUWROW09? NV\YelhxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCKRWKyJIdmdmVid3n0bEBKSzVyIH;mJFAvOjhizszN M1LUR|IyQThzN{G0
MCF7-neo/Her2 NXLtT|Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYftc|FzPzJiaB?= NWPqb|M4TE2VTx?= NEj4ZlVKSzVyPUCuNlkh|ryP NHraSlkzOzZ4MkmwNy=>
MCF7-neo/Her2 NFPFeJJMcW6jc3WgRZN{[Xl? M1nYfGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> M1jYVVI{PjZ{OUCz
PC3 NEXDfJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mke3O|IhcA>? NH3UWlZFVVOR NIj2SpRGSzVyPUCuN|Qh|ryP MkDENlE6QDV4M{m=
MCF7.1 NEjxNmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nkVFczKGh? MnnJSG1UVw>? MkD5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? M{\YTFIyQTh3NkO5
PC3 NHHXU2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH35Smk4OiCq M4Ow[mROW09? M2CxcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> M3jxWlIxODVyNk[5
MCF7.1 NGXY[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3OYo2PzJiaB?= MlrNSG1UVw>? NHu3XYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDJR|UxKG:oIECuN|Qh|ryP NFn5WlYzODB3ME[2PS=>
MCF7.1 NUnHclc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v5[VczKGh? NGTvbXdGSzVyPUCuO|Ih|ryP Mn\aNlA{PDZ4NU[=
NCI-H1975 NFPnTmZEgXSxdH;4bYMhSXO|YYm= NGnyZ5A4OiCq M3;WO2lEPTB;MD6yO{DPxE1? MnTJNlMxPTl3NEW=
H460 Mmq4R5l1d3SxeHnjJGF{e2G7 MXu3NkBp NHrJU5ZKSzVyPUCuPFch|ryP MmTNNlMxPTl3NEW=
HT-29 M2\rR2N6fG:2b4jpZ{BCe3OjeR?= M{\UOVczKGh? NY\NbWFPUUN3ME2wMlY3KM7:TR?= NV3SO2E1OjNyNUm1OFU>
HepG2 M3zQVmN6fG:2b4jpZ{BCe3OjeR?= MWS3NkBp NX:0R2hwUUN3ME2xJO69VQ>? M4nRUVI{ODV7NUS1
SGC7901 NWXLZXBYS3m2b4TvfIlkKEG|c3H5 NF:z[WU4OiCq Mm\RTWM2OD1zLkig{txO MV6yN|A2QTV2NR?=
NCI-H226 MoTzR5l1d3SxeHnjJGF{e2G7 NU\xdZZzPzJiaB?= NV7TXmk4UUN3ME2yMlkh|ryP NFG0[XQzOzB3OUW0OS=>
A549 MVrDfZRwfG:6aXOgRZN{[Xl? NULnXmtkPzJiaB?= M2rNcmlEPTB;Nj65JO69VQ>? Ml\JNlMxPTl3NEW=
U87MG NV;MPVM2S3m2b4TvfIlkKEG|c3H5 MVe3NkBp Mmn4TWM2OD15Lke3JO69VQ>? NVzOZXdqOjNyNUm1OFU>
HBC4 M4Hh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFqxV4Ztd2eJSUWwQU03NjB|IF2= MkLvNlI{OzZ{NE[=
BSY1 NVe2ZXo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7O[2Ztd2eJSUWwQU03NjlyIF2= MmPuNlI{OzZ{NE[=
HBC5 NWXYVIF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\2fIxw\0eLNUC9MVYvPjBiTR?= MmXFNlI{OzZ{NE[=
MCF7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e2WIxw\0eLNUC9MVcvOzNiTR?= MoTPNlI{OzZ{NE[=
MDA-MB-231 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoC3cI9oT0l3ME2tOU41PiCP M3TXb|IzOzN4MkS2
U251 MoLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTQcI9oT0l3ME2tOU42OCCP NIO4epozOjN|NkK0Oi=>
SF268 MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fUV4xw\0eLNUC9MVUvOzliTR?= NVq0Zo0xOjJ|M{[yOFY>
SF295 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\Tcoxw\0eLNUC9MVYvOzdiTR?= NHLKXVYzOjN|NkK0Oi=>
SF539 Mk\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXlcI9oT0l3ME2tOk42OCCP NX2zVFFTOjJ|M{[yOFY>
SNB75 MoS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTBVm9td2eJSUWwQU04NjFyIF2= NImySHQzOjN|NkK0Oi=>
SNB78 NWrkXYFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DGO4xw\0eLNUC9MVYvPTJiTR?= M{H4S|IzOzN4MkS2
HCC2998 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDucI9oT0l3ME2tOk4zQSCP MYmyNlM{PjJ2Nh?=
KM12 M2LsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXsc4dIUTVyPT21Mlc3KE1? MkXENlI{OzZ{NE[=
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NCI-H226 Mm\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzGcpNtd2eJSUWwQU03NjJzIF2= MnKxNlI{OzZ{NE[=
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LOXIMVI Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\kcI9oT0l3ME2tOk4zQSCP MoLuNlI{OzZ{NE[=
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MKN45 NGD5epJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfKS5dtd2eJSUWwQU03NjV3IF2= MUeyNlM{PjJ2Nh?=
MKN74 NXr1SWkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L1eYxw\0eLNUC9MVYvODJiTR?= MmnwNlI{OzZ{NE[=
DU145 NH\VZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPpPGNtd2eJSUWwQU02Njh3IF2= NF7UR2EzOjN|NkK0Oi=>
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HH NIjFW3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7venE{UUN3ME2xNVEvODhibl2= NIG2TolUSU6JRWK=
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NCI-H1770 NIq1XlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF{Mz64OkBvVQ>? MmfYV2FPT0WU
HuO9 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjQNllKSzVyPUKwOk4xOiCwTR?= MUnTRW5ITVJ?
HAL-01 NV3wUJNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfwTpk1UUN3ME2yNFYvPzNibl2= MnjnV2FPT0WU
NOS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJzMT64NkBvVQ>? Mk\jV2FPT0WU
HGC-27 M3;Rfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrF[5VGUUN3ME2yNVIvPTdibl2= NYDWfnJGW0GQR1XS
NB69 NEP2c3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXsTWM2OD1{NEWuNlchdk1? NFnWeVhUSU6JRWK=
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DOK NVr1R|VQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTNyMT63JI5O M4fFcHNCVkeHUh?=
LB2241-RCC NXq3dFhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP3SGlKUUN3ME2zNFMvQDRibl2= NGTCeYdUSU6JRWK=
NCI-H1623 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTNyND6wPEBvVQ>? MVvTRW5ITVJ?
YH-13 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNyND6zNkBvVQ>? NFzBT3VUSU6JRWK=
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AN3-CA NXi0cIQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fZTmlEPTB;M{SwMlM4KG6P NYHSR5hVW0GQR1XS
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MDA-MB-175-VII MmO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEi3eYtKSzVyPUO1Nk46OiCwTR?= NX61WHR3W0GQR1XS
GAMG MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTN5MD64OUBvVQ>? NVL0VohOW0GQR1XS
CHL-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnryTWM2OD1|N{iuOlUhdk1? MYjTRW5ITVJ?
NB7 NGLj[HVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:0TWM2OD1|OEmuPFMhdk1? MYHTRW5ITVJ?
MFE-280 NGHPRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDBTWM2OD12MUiuNkBvVQ>? MlzTV2FPT0WU
HL-60 NXjhZnNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn34TWM2OD12MkWuO|Uhdk1? M1KzZXNCVkeHUh?=
GCIY MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTR|Mz64JI5O NICyNIZUSU6JRWK=
MDA-MB-361 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPUTWM2OD12M{muNVMhdk1? NXPsNI5KW0GQR1XS
LXF-289 NUXicWsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHxPVRKSzVyPUS0PE4zPyCwTR?= NF7teoVUSU6JRWK=
NBsusSR NXfkToRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn4bYZPUUN3ME20PFgvQDVibl2= NEfjPFNUSU6JRWK=
KU-19-19 NE[wRlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnkTWM2OD13MU[uNFchdk1? M1:1bXNCVkeHUh?=
A204 M3LYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP5eIdKUUN3ME21NlIvOzNibl2= M{PUOXNCVkeHUh?=
LB1047-RCC NGLRZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTV{Mj65N{BvVQ>? MYPTRW5ITVJ?
COLO-684 NVv3enhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTV{Mz6xNUBvVQ>? MUHTRW5ITVJ?
PA-1 MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrzTWM2OD13M{KuOFEhdk1? M1jLbXNCVkeHUh?=
MG-63 MonDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPOe4ptUUN3ME21OFEvOTFibl2= M1r3fXNCVkeHUh?=
BHT-101 NUDpelVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HSWGlEPTB;NUS0Mlk1KG6P NI\Xd5BUSU6JRWK=
NKM-1 M{n6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fBU2lEPTB;NUmzMlA6KG6P M1HGWnNCVkeHUh?=
T47D NITrOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTV7Nz61OkBvVQ>? M1\uSXNCVkeHUh?=
MOLT-4 MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfnTWM2OD14MkOuOlIhdk1? MWDTRW5ITVJ?
IGROV-1 NF\Rco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jlcGlEPTB;NkO0MlMyKG6P Ml7BV2FPT0WU
ES4 M3jxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTZ|OT61OEBvVQ>? MYTTRW5ITVJ?
HuO-3N1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULGTJFbUUN3ME22OFIvOzhibl2= MljFV2FPT0WU
NEC8 NIfk[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm1VWNjUUN3ME22OVMvPTdibl2= MnP1V2FPT0WU
HO-1-N-1 NH3V[oVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHOTWM2OD14NUmuNVchdk1? NETKbGtUSU6JRWK=
EPCL-272H M1PIcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LScGlEPTB;Nki3MlIyKG6P M363TnNCVkeHUh?=
D-263MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWwTWM2OD15MUiuNUBvVQ>? NWPrTmZIW0GQR1XS
MV-4-11 M37ST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNVGlEPTB;N{K0MlMyKG6P NYDXNIhyW0GQR1XS
SK-NEP-1 NGL2XGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPFOYxKSzVyPUeyOU46PCCwTR?= MlPpV2FPT0WU
SW872 NFKzT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O4V2lEPTB;N{K3Mlg6KG6P NUfSNXJ6W0GQR1XS
P30-OHK NV7EUVRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTd|MD63NUBvVQ>? M4LWd3NCVkeHUh?=
OMC-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXX2Uot2UUN3ME23OVEvODlibl2= M1m2THNCVkeHUh?=
LoVo Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGyTWM2OD15N{euPUBvVQ>? M1;0V3NCVkeHUh?=
LNCaP-Clone-FGC M2jpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTd7Nj6zOEBvVQ>? NUnyV3NbW0GQR1XS
L-363 M3LCPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T4[GlEPTB;N{m4MlQzKG6P NVvXWVhvW0GQR1XS
ES8 MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKwTWM2OD16MUCuOVIhdk1? NIC2UG1USU6JRWK=
697 MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknETWM2OD16M{GuOVUhdk1? NWXDfW83W0GQR1XS
HSC-3 M2LsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTh|OT61OEBvVQ>? NXnoRnRjW0GQR1XS
H4 NHL5[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;CTWM2OD16NUCuPFUhdk1? MXrTRW5ITVJ?
QIMR-WIL MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrXZ5hKSzVyPUi2OU4zKG6P NUK2cIZNW0GQR1XS
OAW-42 NUHuO3ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfRTWM2OD16N{KuNVkhdk1? NWrMOpFpW0GQR1XS
MCF7 Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj0[oxSUUN3ME24PVgvPTlibl2= Mor3V2FPT0WU
SCC-25 M{XGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXuVYdKSzVyPUmxOE4yQSCwTR?= NV3l[YZFW0GQR1XS
NCI-H1563 MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTlzNT65PUBvVQ>? MX7TRW5ITVJ?
OVCAR-5 MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvqU4FIUUN3ME25OFAvOTdibl2= NXfFRm8xW0GQR1XS
HDLM-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTl2OT6yJI5O MWDTRW5ITVJ?
NB5 M3HUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTl3Nj62JI5O NXm1XnVQW0GQR1XS
NCI-H292 M3;Qemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG5Z3FnUUN3ME25O|QvOzJibl2= NF72VZBUSU6JRWK=
A101D MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTl7MD6xPUBvVQ>? NYPOOWtSW0GQR1XS
NCI-H1648 NWTYVZo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXpNW05UUN3ME25PVgvPTFibl2= MkPJV2FPT0WU
EKVX MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELJN5FKSzVyPUGuNFEzQSEQvF2= NWPufplVW0GQR1XS
SW1710 M{K4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIftUIVKSzVyPUGuNFQzOzNizszN M3rTXHNCVkeHUh?=
WM-115 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW5TWM2OD1zLkC2OlU3KM7:TR?= MV;TRW5ITVJ?
CAL-54 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LtOmlEPTB;MT6wO|A5OSEQvF2= MorMV2FPT0WU
TGBC24TKB Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzQTWM2OD1zLkC4NFQ2KM7:TR?= NIW3c5FUSU6JRWK=
NCI-H520 M3zofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X5TGlEPTB;MT6wPFk3PyEQvF2= NIn4SI1USU6JRWK=
D-423MG MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG2e|ZjUUN3ME2xMlA6QTZ{IN88US=> MnrTV2FPT0WU
BFTC-905 M1PBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1zLkGzOFQ6KM7:TR?= NUfNXYZYW0GQR1XS
HT NWXRT49KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwMUO0O|gh|ryP NYPvPXFMW0GQR1XS
CTB-1 NIjLNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDzTWM2OD1zLkG0Nlk{KM7:TR?= MXHTRW5ITVJ?
Hs-578-T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnSTWM2OD1zLkG5OVY2KM7:TR?= MkfjV2FPT0WU
HuH-7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3iydmlEPTB;MT6yNFk1QSEQvF2= MYfTRW5ITVJ?
LB996-RCC NELM[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\NV2lEPTB;MT6yNlE4PyEQvF2= NUH1[5BYW0GQR1XS
KYSE-270 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTFNlZRUUN3ME2xMlI6PzN2IN88US=> M1TYUnNCVkeHUh?=
A4-Fuk M1P2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXpdoU1UUN3ME2xMlI6QTl|IN88US=> MmP4V2FPT0WU
A498 M4TUR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF25bopKSzVyPUGuN|A1PzRizszN MnXEV2FPT0WU
SK-MEL-1 M1GyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLlZlBKSzVyPUGuN|A3PzlizszN MYrTRW5ITVJ?
AU565 NVm5RYZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwM{G4OlMh|ryP M{K2XXNCVkeHUh?=
Saos-2 NGjOSllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFwM{OyNFUh|ryP NXH5b3p[W0GQR1XS
A549 NXmxUmVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3npPGlEPTB;MT6zPVk4KM7:TR?= NHXzOIVUSU6JRWK=
BFTC-909 NWjHPY5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHUTWM2OD1zLkSzN|A2KM7:TR?= M{fxUHNCVkeHUh?=
MDA-MB-415 NYC0bVVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwNEi2PVIh|ryP NYr2V5NLW0GQR1XS
639-V NXf3NYV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HrS2lEPTB;MT61NFI1PSEQvF2= MmjmV2FPT0WU
A704 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXXTWM2OD1zLkWwO|g2KM7:TR?= MmTlV2FPT0WU
PANC-03-27 NFKxWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfVeGtIUUN3ME2xMlUyPDB6IN88US=> MYXTRW5ITVJ?
SK-MEL-28 MoDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwNU[wPFUh|ryP NF\telFUSU6JRWK=
Ramos-2G6-4C10 NGXUPZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFwNkC3OFYh|ryP NELKTFdUSU6JRWK=
HuP-T4 NHHqc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC5R29KSzVyPUGuOlA4PzhizszN MWHTRW5ITVJ?
VA-ES-BJ MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXnb4dKSzVyPUGuOlEzPyEQvF2= NIjOUJNUSU6JRWK=
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NCI-H441 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJ3Lke0OlUh|ryP MYrTRW5ITVJ?
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RKO MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvxPXpCUUN3ME2yOk44PjN{IN88US=> MnGzV2FPT0WU
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CAL-120 NEXvUnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTZPXRKSzVyPUK3MlY6OTRizszN MWTTRW5ITVJ?
NCI-H2452 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ5Lke3NVYh|ryP MU\TRW5ITVJ?
NCI-H1395 NUXNT4M6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJ5Lke4N|Mh|ryP M{T5VHNCVkeHUh?=
KYSE-450 NIfiflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ5Lkm4OlIh|ryP MXTTRW5ITVJ?
S-117 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\WO2RrUUN3ME2yPU4{QDV5IN88US=> M4PDZ3NCVkeHUh?=
SW13 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXVSY9KSzVyPUK5Mlg2OTlizszN NXPYOWVyW0GQR1XS
ES3 NULlXYhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTNyLkO3N|Mh|ryP M1XaXXNCVkeHUh?=
HCT-116 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDaTWM2OD1|MD61OVU1KM7:TR?= NXXMVIQyW0GQR1XS
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VM-CUB-1 NIXxfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\1bZlCUUN3ME2zNE43PDF|IN88US=> NEn1OXZUSU6JRWK=
NCI-H2170 Ml35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHZRoZKSzVyPUOxMlU4QDRizszN M4j5dXNCVkeHUh?=
ALL-PO Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTaT|lNUUN3ME2zNU45PDJ6IN88US=> MUnTRW5ITVJ?
NCI-H661 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvGTWM2OD1|Mj6wOlI{KM7:TR?= M2fNSnNCVkeHUh?=
NCI-H2347 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP6TWM2OD1|Mj60PFM4KM7:TR?= NI\sVVhUSU6JRWK=
FTC-133 M3fCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jVN2lEPTB;M{KuO|A3KM7:TR?= NULWTnNNW0GQR1XS
COLO-829 NVjWUYk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTN|LkO0Olch|ryP MXLTRW5ITVJ?
GOTO MojLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTvXJNUUUN3ME2zN{42OjV6IN88US=> MnGyV2FPT0WU
YAPC NVLhNFV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTN|LkixOVkh|ryP MWrTRW5ITVJ?
LCLC-103H NHjQdnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzNTWM2OD1|ND6xOlI1KM7:TR?= Mlr3V2FPT0WU
SiHa M1zVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTN2LkO4NVch|ryP MXnTRW5ITVJ?
LK-2 M2jrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTN2LkW3NFgh|ryP NIi2NoJUSU6JRWK=
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NCI-SNU-1 NVPKb5dLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\KOI5KSzVyPUO1MlE4QSEQvF2= NFvseYtUSU6JRWK=
KNS-81-FD MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\YOGlEPTB;M{WuOlY{KM7:TR?= NUnLVm5EW0GQR1XS
SCC-9 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvwTWM2OD1|Nj63NVQ3KM7:TR?= MYTTRW5ITVJ?
SH-4 NYT6SWdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHC[m1PUUN3ME2zOk44OyEQvF2= NE\1ZlRUSU6JRWK=
HCC-1954 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ixbmlEPTB;M{euNlczQSEQvF2= MmTSV2FPT0WU
BALL-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13nUWlEPTB;M{euOVMyPiEQvF2= NFL3fJRUSU6JRWK=
BE-13 NIjWUoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTN5LkewNVgh|ryP M2LMRnNCVkeHUh?=
COLO-678 NIDnSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN5Lkm0N|ch|ryP M1X3cnNCVkeHUh?=
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OAW-28 M124N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTN6Lk[zPUDPxE1? NIjjSpZUSU6JRWK=
CAMA-1 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHHc5hJUUN3ME2zPE46PjlzIN88US=> NX;3bpYyW0GQR1XS
C2BBe1 M1zwVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN7LkixPEDPxE1? NIXoRZFUSU6JRWK=
A3-KAW MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{SxUWlEPTB;NECuN|Y3OSEQvF2= MWrTRW5ITVJ?
SK-MEL-24 NIrTOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfofJFkUUN3ME20NE42QTNzIN88US=> NYT0cHI2W0GQR1XS
KYSE-140 M{jPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLzUYptUUN3ME20NE44OTZ3IN88US=> M3j2WXNCVkeHUh?=
MOLT-16 NWezN4Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILuVm1KSzVyPUSxMlE2OzZizszN NXTL[2tHW0GQR1XS
CFPAC-1 NWm4PY9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTYbXpKSzVyPUSyMlUzOTFizszN MV;TRW5ITVJ?
NB14 NFHqZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknaTWM2OD12Mj63NFI4KM7:TR?= M37NPXNCVkeHUh?=
COLO-792 NVPLdnVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTIOphKSzVyPUSyMlg6PjFizszN MX7TRW5ITVJ?
RH-1 NWTuOGx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj6PIFKSzVyPUSzMlQ5OzZizszN M4DTXnNCVkeHUh?=
NCI-H522 NUjUVlA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHIe|MxUUN3ME20OE4{PTZ6IN88US=> M121SXNCVkeHUh?=
Ca-Ski MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m2OWlEPTB;NESuPFEyPCEQvF2= MoHwV2FPT0WU
KGN NVmxToxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrTVoFKSzVyPUS4MlMxPjNizszN M2D4e3NCVkeHUh?=
UACC-62 M1TwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTCTWM2OD12OD60NFczKM7:TR?= MmrSV2FPT0WU
NCI-H358 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;kOI0xUUN3ME20PU4{ODF6IN88US=> MnTsV2FPT0WU
LS-411N NHLqeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn6THFKSzVyPUS5MlMyOThizszN M1rTOXNCVkeHUh?=
IST-MES1 NETqTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vHRmlEPTB;NEmuOVYzPSEQvF2= M2\Bd3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
Synonyms RG7321

Bio Calculators

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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00999128 Completed Healthy Volunteers Genentech, Inc. October 26, 2009 Phase 1
NCT02092831 Completed Healthy Volunteer Genentech, Inc. April 2014 Phase 1
NCT01740336 Active, not recruiting Breast Cancer Genentech, Inc. February 2013 Phase 2
NCT01493843 Completed Non-Squamous Non-Small Cell Lung Cancer Genentech, Inc. January 2012 Phase 2
NCT01474668 Completed Healthy Volunteer Genentech, Inc. October 2011 Phase 1
NCT01437566 Completed Breast Cancer Genentech, Inc. October 2011 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

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

  • * Indicates a Required Field

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID