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 59 Publications

9 Customer Reviews

  • Clonogenic assays of TNBC cell lines grown continuously in increasing concentrations of palbociclib, divided by gene expression subtypes: LAR, luminal androgen receptor; MSL, mesenchymal stem-like; MES, mesenchymal and basal-like. All cell lines are RB1 wild-type except RB1 mutant BT549.

    Clin Cancer Res, 2017, 23(18):5561-5572. Pictilisib (GDC-0941) purchased from Selleck.

    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, 16(4):637-648. 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.

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    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 MWLLbY5ie2ViQYPzZZk> MnjmNUBp MULEUXNQ M2m1cWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= NYi4OohNOTh5NUS2OVQ>
Sf9 MXLLbY5ie2ViQYPzZZk> MVyxJIg> NV\TfI56TE2VTx?= NVry[IJPUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? MVexPFc2PDZ3NB?=
Sf9 MXnLbY5ie2ViQYPzZZk> NFj3PVEyKGh? NEDZXm5FVVOR Ml\WTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> MmPMNVg4PTR4NUS=
Sf9 MWLLbY5ie2ViQYPzZZk> NXLYTo0yOSCq MlfvSG1UVw>? M4jSNmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wN|Mh|ryP MYexPFc2PDZ3NB?=
Sf9 NIHBOGFMcW6jc3WgRZN{[Xl? MlXpNUBp MXTEUXNQ M4rWdGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> NYj0ZXJCOTh5NUS2OVQ>
MDA-MB-361 M1q5TmZ2dmO2aX;uJGF{e2G7 NHzkeGczKGh? NWH0XGF{TE2VTx?= MkjVTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPRFGtUWIuOzZzIHPlcIx{KHerdHigVGlMO0ODIFW1OFUuUyCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4xOjhizszN NYr1ZZJMOTh5NUS2OVQ>
PC3 NX:zUVNNTnWwY4Tpc44hSXO|YYm= NYXqepJPOiCq MXjEUXNQ MYHJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCSQ{OgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODN5IN88US=> MYKxPFc2PDZ3NB?=
U87MG MkLKSpVv[3Srb36gRZN{[Xl? MkfPNkBp NXvHNXlOTE2VTx?= MWfJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yNE[g{txO MoLNNVg4PTR4NUS=
MDA-MB-361 M1fYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S4clk3KGh? MojpSG1UVw>? NFnwXpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> M1roWFE5PzV2NkW0
A2780 M1W0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK5OkBp M2\YSWROW09? NFnOXVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= Mm[2NVg4PTR4NUS=
PC3 MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L1S|k3KGh? NHHY[5hFVVOR NV\QRmhCUUN3ME2wMlI5KM7:TR?= NFP3c2EyQDd3NE[1OC=>
U87MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Lx[Vk3KGh? M1HXNmROW09? NFH0dY1KSzVyPUCuPVUh|ryP MnWxNVg4PTR4NUS=
Sf9 NVLvVZZTU2mwYYPlJGF{e2G7 NXfRbnlDOzBibXnu NECxbHRFVVOR NGDOe|VKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgZY1wfW62IH;mJGFVWCClb37zeY1m\CC5aYToJGlEPTBib3[gNE4xPDJizszN MX6yNlU1QDN2Mh?=
RAW 264.7 NGjLXpdMcW6jc3WgRZN{[Xl? MYi5NEBucW5? M2nBZ2ROW09? MmXqTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4zQThizszN MUmyNlU1QDN2Mh?=
Sf9 MWrLbY5ie2ViQYPzZZk> NHjE[|QyKGh? MV7Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZoV1[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW0Z7IHPlcIx{KHerdHigTWM2OCCxZjCwMlAyPyEQvF2= MoTINlM2PDB4NEW=
Sf9 NVvjdnFEU2mwYYPlJGF{e2G7 MYmxJIg> M3\CXmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= Mn\zNlM2PDB4NEW=
Sf9 M{PpNWtqdmG|ZTDBd5NigQ>? M3XXRVEhcA>? NF:zRm1KdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM\2GvbXGg[ZhxemW|c3Xk M1PWWVI{PTRyNkS1
Sf9 NX6xTFE3U2mwYYPlJGF{e2G7 MUCxJIg> NIXVcWZKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[WyyaHGg[ZhxemW|c3Xk NUm3SWhJOjN3NEC2OFU>
SKOV3 M2D3dGtqdmG|ZTDBd5NigQ>? MmewNUDPxE1? M{\FSFEhcA>? NF;iNlVFVVOR M1PFSWlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25? NIf0SowzOzN4MEO0PC=>
MCF7 NF\HTVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jTTVEh|ryP NGTG[YU6PiCq MkC2SG1UVw>? Mor5S2k2OD1yLkC3NFIh|ryP NYq4OpJXOjN|NkCzOFg>
SKOV3 NHK3XZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVixJO69VQ>? M2Dp[Fk3KGh? NFz6doFFVVOR MVLHTVUxRTBwMUS3OkDPxE1? NH7IUmgzOzN4MEO0PC=>
PC3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG2O|IhcA>? MVvEUXNQ MnvrTWM2OD1yLkK4JO69VQ>? NFfJN4EzOTl6MUexOC=>
MCF7.1 MkL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPyelk4OiCq NVHDbY9jTE2VTx?= Mnf6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BJTVJ{IHflcoUhf2m2aDDJR|UxKG:oIECuNlgh|ryP NIC5WnQzOTl6MUexOC=>
MCF7-neo/Her2 M2Xp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TiTlczKGh? NV3mWZN7TE2VTx?= NVj0bWR2UUN3ME2wMlI6KM7:TR?= NU\2UoRUOjN4NkK5NFM>
MCF7-neo/Her2 MWrLbY5ie2ViQYPzZZk> Mmf0TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC5aYToJGlEPTBib3[gNE4xODdizszN Mn7TNlM3PjJ7MEO=
PC3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITEWWg4OiCq MlXqSG1UVw>? NX7wU3dvTUN3ME2wMlM1KM7:TR?= M4m0TFIyQTh3NkO5
MCF7.1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXnVZJrPzJiaB?= MUHEUXNQ NIPHdXhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDFR|UxKG:oIECuN|kh|ryP Ml\pNlE6QDV4M{m=
PC3 NXT4cYIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfGN3U4OiCq NUnOSJdrTE2VTx?= M37QTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> NFz6bJozODB3ME[2PS=>
MCF7.1 Ml7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnsO|IhcA>? MV3EUXNQ NGf0ZmZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDJR|UxKG:oIECuN|Qh|ryP M37YVlIxODVyNk[5
MCF7.1 M2PSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkThO|IhcA>? NHPjVm1GSzVyPUCuO|Ih|ryP MnXENlA{PDZ4NU[=
NCI-H1975 NFjpSmFEgXSxdH;4bYMhSXO|YYm= NFLFToI4OiCq MnLITWM2OD1yLkK3JO69VQ>? MXeyN|A2QTV2NR?=
H460 NXftTmNQS3m2b4TvfIlkKEG|c3H5 MV23NkBp M2fyRWlEPTB;MD64O{DPxE1? M1\KeFI{ODV7NUS1
HT-29 Mnn5R5l1d3SxeHnjJGF{e2G7 MYq3NkBp NFz0dGpKSzVyPUCuOlYh|ryP MYOyN|A2QTV2NR?=
HepG2 NGX1fmREgXSxdH;4bYMhSXO|YYm= NGfsOI04OiCq NGnjXVZKSzVyPUGg{txO NHryWZAzOzB3OUW0OS=>
SGC7901 NHX4[XlEgXSxdH;4bYMhSXO|YYm= MWC3NkBp NVnFfGJtUUN3ME2xMlgh|ryP MkHONlMxPTl3NEW=
NCI-H226 NH\EXIVEgXSxdH;4bYMhSXO|YYm= NX32b|BkPzJiaB?= MlLWTWM2OD1{Lkmg{txO MkTuNlMxPTl3NEW=
A549 NVWzem51S3m2b4TvfIlkKEG|c3H5 Mn;3O|IhcA>? MmroTWM2OD14Lkmg{txO MVOyN|A2QTV2NR?=
U87MG MnnLR5l1d3SxeHnjJGF{e2G7 MWW3NkBp Mm[wTWM2OD15Lke3JO69VQ>? M{LRXVI{ODV7NUS1
HBC4 NIjMdGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jYXYxw\0eLNUC9MVYvODNiTR?= M1TofVIzOzN4MkS2
BSY1 NFvqXVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLXVGNtd2eJSUWwQU03NjlyIF2= MXqyNlM{PjJ2Nh?=
HBC5 NVL3b256T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrpdHptd2eJSUWwQU03NjZyIF2= MXOyNlM{PjJ2Nh?=
MCF7 NWXaNGY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHaV|Ntd2eJSUWwQU04NjN|IF2= NGfHeWgzOjN|NkK0Oi=>
MDA-MB-231 NYXJT5IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3yPXppdG:pR1m1NF0uPS52NjDN NVnpUYtYOjJ|M{[yOFY>
U251 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPycI9oT0l3ME2tOU42OCCP MnLYNlI{OzZ{NE[=
SF268 NFXMfXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\Kdnltd2eJSUWwQU02NjN7IF2= NH\oTpgzOjN|NkK0Oi=>
SF295 MkTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPTU483dG:pR1m1NF0uPi5|NzDN M{D6cVIzOzN4MkS2
SF539 NYGwW4t1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T1Voxw\0eLNUC9MVYvPTBiTR?= M1ruTlIzOzN4MkS2
SNB75 NHv1PXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pp[Ixw\0eLNUC9MVcvOTBiTR?= NFzsOoEzOjN|NkK0Oi=>
SNB78 NWfKVIVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTXcI9oT0l3ME2tOk42OiCP NYPicpVnOjJ|M{[yOFY>
HCC2998 NFzXS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7zbZFKdG:pR1m1NF0uPi5{OTDN MmXmNlI{OzZ{NE[=
KM12 M2HkOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO2WXl{dG:pR1m1NF0uPS55NjDN MnLzNlI{OzZ{NE[=
HT-29 NISx[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rzWoxw\0eLNUC9MVYvOzBiTR?= NG\oXlAzOjN|NkK0Oi=>
HCT15 MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PFVYxw\0eLNUC9MVYvOTJiTR?= M{DMPVIzOzN4MkS2
HCT116 Ml\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjYPJlFdG:pR1m1NF0uPS56NzDN Ml3rNlI{OzZ{NE[=
NCI-H23 NVTkbmsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq1cI9oT0l3ME2tOU44OyCP MYCyNlM{PjJ2Nh?=
NCI-H226 NXPjVHdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULje|hndG:pR1m1NF0uPi5{MTDN MmHCNlI{OzZ{NE[=
NCI-H522 M4\hV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjrVJI{dG:pR1m1NF0uPi53ODDN NVvXdYFtOjJ|M{[yOFY>
NCI-H483 NEX1OphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr3cI9oT0l3ME2tOk42PiCP NHXFZVYzOjN|NkK0Oi=>
A549 NFHv[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jXWoxw\0eLNUC9MVYvOTViTR?= M1z0PFIzOzN4MkS2
DMS273 NWTJXGhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHsc4dIUTVyPT22MlQ{KE1? MYSyNlM{PjJ2Nh?=
DMS114 M1raNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHSTIxtd2eJSUWwQU02Njl{IF2= M2LSclIzOzN4MkS2
LOXIMVI Mk[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHsc4dIUTVyPT22MlI6KE1? MlTsNlI{OzZ{NE[=
OVCAR3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIO2[5Rtd2eJSUWwQU03NjdzIF2= MkDTNlI{OzZ{NE[=
OVCAR4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3Hb28xdG:pR1m1NF0uPS55NjDN NEfXdogzOjN|NkK0Oi=>
OVCAR5 M3LaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:4N2Ztd2eJSUWwQU03NjJ4IF2= NFjRb3QzOjN|NkK0Oi=>
OVCAR8 M{PDfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\sc4dIUTVyPT21Mlc{KE1? NU\hN5ZQOjJ|M{[yOFY>
SKOV3 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInrcIttd2eJSUWwQU03NjV{IF2= NXPYSZJlOjJ|M{[yOFY>
RXF631L NHXzTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\GdYxw\0eLNUC9MVYvQDhiTR?= NVvnd3FVOjJ|M{[yOFY>
ACHN NYK4PWtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq5cI9oT0l3ME2tOk4xPyCP MnLSNlI{OzZ{NE[=
St-4 NF;kXnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\mUphNdG:pR1m1NF0uPS53NjDN NX\EVJdIOjJ|M{[yOFY>
MKN1 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HyUYxw\0eLNUC9MVcvODhiTR?= M2nYdlIzOzN4MkS2
MKN7 MkjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSxcI9oT0l3ME2tOk42OCCP MUeyNlM{PjJ2Nh?=
MKN28 NHj6d2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDsc4dIUTVyPT21MlUzKE1? M3XJRVIzOzN4MkS2
MKN45 NGi1SJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi5d5dtd2eJSUWwQU03NjV3IF2= MUeyNlM{PjJ2Nh?=
MKN74 NWnw[4xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3sc4dIUTVyPT22MlAzKE1? NGDofXczOjN|NkK0Oi=>
DU145 NFG1cW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzsc4dIUTVyPT21Mlg2KE1? NFiw[pozOjN|NkK0Oi=>
PC3 M{ntT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP6Vpptd2eJSUWwQU03NjZ4IF2= MV6yNlM{PjJ2Nh?=
ES5 NIXWfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvwSoRTUUN3ME21NE4zOSCwTR?= M37TNHNCVkeHUh?=
HH MlrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLJclFrUUN3ME2xNVEvODhibl2= NUG0[VRtW0GQR1XS
MHH-PREB-1 NF\PPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\xbZpKSzVyPUGxOE4{KG6P NWrjZ5NJW0GQR1XS
NCI-H1770 M2T1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LUd2lEPTB;MUKzMlg3KG6P NFn3bpZUSU6JRWK=
HuO9 M1;NN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnqcIZKSzVyPUKwOk4xOiCwTR?= MmXjV2FPT0WU
HAL-01 NGe4VJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nm[mlEPTB;MkC2Mlc{KG6P M1HrNXNCVkeHUh?=
NOS-1 NGH3dJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2W0bmlEPTB;MkGxMlgzKG6P M{XJ[HNCVkeHUh?=
HGC-27 MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJzMj61O{BvVQ>? MoLUV2FPT0WU
NB69 MmLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrvUJNKSzVyPUK0OU4zPyCwTR?= M2faR3NCVkeHUh?=
RS4-11 M2Wzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXHTWM2OD1{NkGuO|Yhdk1? MWHTRW5ITVJ?
DOK NEDv[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTNyMT63JI5O NF;LPGtUSU6JRWK=
LB2241-RCC M{jkbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTNyMz64OEBvVQ>? MX3TRW5ITVJ?
NCI-H1623 M1HPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nKe2lEPTB;M{C0MlA5KG6P NEjwXoRUSU6JRWK=
YH-13 NXP6NGtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTmRZNvUUN3ME2zNFQvOzJibl2= MVjTRW5ITVJ?
BPH-1 NWGwU|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTNzNDDuUS=> NEixb5hUSU6JRWK=
AN3-CA Ml\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD0bINKSzVyPUO0NE4{PyCwTR?= MWDTRW5ITVJ?
ES7 NYDSV2RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX2NId6UUN3ME2zOFEvQTlibl2= Mmn1V2FPT0WU
MDA-MB-175-VII M1PoSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnCT5dKSzVyPUO1Nk46OiCwTR?= NVvTPGRuW0GQR1XS
GAMG MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPNWppiUUN3ME2zO|AvQDVibl2= NYrKc|RxW0GQR1XS
CHL-1 M{XHWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH6b4JlUUN3ME2zO|gvPjVibl2= NHTOTnVUSU6JRWK=
NB7 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPzSVJKSzVyPUO4PU45OyCwTR?= MnvQV2FPT0WU
MFE-280 NX71OFZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvJdJlHUUN3ME20NVgvOiCwTR?= MWPTRW5ITVJ?
HL-60 NGT6O4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nvVGlEPTB;NEK1Mlc2KG6P MkHDV2FPT0WU
GCIY NFS5bmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;DTWM2OD12M{OuPEBvVQ>? NH\RTW1USU6JRWK=
MDA-MB-361 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LpZmlEPTB;NEO5MlE{KG6P MYXTRW5ITVJ?
LXF-289 NXvSeFA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTR2OD6yO{BvVQ>? NH\OdFVUSU6JRWK=
NBsusSR NIHwNZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TxRWlEPTB;NEi4Mlg2KG6P M2C2Z3NCVkeHUh?=
KU-19-19 NETPSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTVzNj6wO{BvVQ>? NF7xc5lUSU6JRWK=
A204 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2n3RWlEPTB;NUKyMlM{KG6P NInpOnhUSU6JRWK=
LB1047-RCC NXzGTVdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETZR21KSzVyPUWyNk46OyCwTR?= M4LRTXNCVkeHUh?=
COLO-684 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT5SWRrUUN3ME21NlMvOTFibl2= M1fMXnNCVkeHUh?=
PA-1 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfwVpYzUUN3ME21N|IvPDFibl2= NUW4SlB[W0GQR1XS
MG-63 M4\2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTV2MT6xNUBvVQ>? Ml7hV2FPT0WU
BHT-101 NWTPdWtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nhPWlEPTB;NUS0Mlk1KG6P NVW1[YdtW0GQR1XS
NKM-1 MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\ofGlEPTB;NUmzMlA6KG6P Mn71V2FPT0WU
T47D Mle1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HG[2lEPTB;NUm3MlU3KG6P NFjNbXFUSU6JRWK=
MOLT-4 NUDpc|F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTZ{Mz62NkBvVQ>? M1HrZXNCVkeHUh?=
IGROV-1 M{DCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTZ|ND6zNUBvVQ>? MnTsV2FPT0WU
ES4 NVfTOZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFziW49KSzVyPU[zPU42PCCwTR?= NVH2TY5QW0GQR1XS
HuO-3N1 NEXibnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fNN2lEPTB;NkSyMlM5KG6P NXmwc5B3W0GQR1XS
NEC8 NGS2bG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjvZ4NmUUN3ME22OVMvPTdibl2= M1vqeXNCVkeHUh?=
HO-1-N-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXSTWM2OD14NUmuNVchdk1? NWjIdXhwW0GQR1XS
EPCL-272H MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTZ6Nz6yNUBvVQ>? Mn:1V2FPT0WU
D-263MG M{XtVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\mNFJKSzVyPUexPE4yKG6P NVLpXo91W0GQR1XS
MV-4-11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fl[2lEPTB;N{K0MlMyKG6P NGj5SGJUSU6JRWK=
SK-NEP-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTd{NT65OEBvVQ>? Mn75V2FPT0WU
SW872 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[0O2tKSzVyPUeyO{45QSCwTR?= NWn3ZXlQW0GQR1XS
P30-OHK NFz6dGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TMUGlEPTB;N{OwMlcyKG6P Ml;MV2FPT0WU
OMC-1 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4izPWlEPTB;N{WxMlA6KG6P NF;uUHdUSU6JRWK=
LoVo M3ToW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;QcGlEPTB;N{e3Mlkhdk1? MXjTRW5ITVJ?
LNCaP-Clone-FGC M4CxOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfuTWM2OD15OU[uN|Qhdk1? MoXhV2FPT0WU
L-363 Ml7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHIZpdKSzVyPUe5PE41OiCwTR?= MVzTRW5ITVJ?
ES8 NFjuSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRThzMD61NkBvVQ>? Mn7UV2FPT0WU
697 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkKyTWM2OD16M{GuOVUhdk1? Mni2V2FPT0WU
HSC-3 M3G2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTh|OT61OEBvVQ>? NXPNd4pJW0GQR1XS
H4 NFW2Zo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLGTWM2OD16NUCuPFUhdk1? M1TUbXNCVkeHUh?=
QIMR-WIL MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXnTWM2OD16NkWuNkBvVQ>? NYPENnhqW0GQR1XS
OAW-42 M2WzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jzbGlEPTB;OEeyMlE6KG6P MXLTRW5ITVJ?
MCF7 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq4WZl[UUN3ME24PVgvPTlibl2= M4rL[nNCVkeHUh?=
SCC-25 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqzTWM2OD17MUSuNVkhdk1? NEP6SIlUSU6JRWK=
NCI-H1563 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnBVWN{UUN3ME25NVUvQTlibl2= NX35UGJFW0GQR1XS
OVCAR-5 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;Y[Fl[UUN3ME25OFAvOTdibl2= MoHyV2FPT0WU
HDLM-2 NX72OZp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r5NmlEPTB;OUS5MlIhdk1? MnzpV2FPT0WU
NB5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\0ZpFKSzVyPUm1Ok43KG6P NEHFb4FUSU6JRWK=
NCI-H292 NX7CNlBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTl5ND6zNkBvVQ>? NEnmUWZUSU6JRWK=
A101D NUfPcZR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUCyOG52UUN3ME25PVAvOTlibl2= M4LNeXNCVkeHUh?=
NCI-H1648 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHFRldSUUN3ME25PVgvPTFibl2= NHG5UFFUSU6JRWK=
EKVX Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD0TWM2OD1zLkCxNlkh|ryP NXHpdnVmW0GQR1XS
SW1710 MlS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC2U2xKSzVyPUGuNFQzOzNizszN MYLTRW5ITVJ?
WM-115 NV\y[JhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfHSoxLUUN3ME2xMlA3PjV4IN88US=> M4fjRXNCVkeHUh?=
CAL-54 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j4PWlEPTB;MT6wO|A5OSEQvF2= MXLTRW5ITVJ?
TGBC24TKB Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfwU4RKSzVyPUGuNFgxPDVizszN NXnGXWNQW0GQR1XS
NCI-H520 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jJ[WlEPTB;MT6wPFk3PyEQvF2= NXXnR282W0GQR1XS
D-423MG Ml74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPYTWM2OD1zLkC5PVYzKM7:TR?= NXe2U2Y5W0GQR1XS
BFTC-905 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMUO0OFkh|ryP MnP2V2FPT0WU
HT NWn3Oph6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLJNnRKSzVyPUGuNVM1PzhizszN NWj5ZWNFW0GQR1XS
CTB-1 M1LNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljQTWM2OD1zLkG0Nlk{KM7:TR?= MVXTRW5ITVJ?
Hs-578-T NFLlUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTFwMUm1OlUh|ryP M4fWZXNCVkeHUh?=
HuH-7 Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTMb2pKSzVyPUGuNlA6PDlizszN MmPIV2FPT0WU
LB996-RCC NXHsUI9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2myPGlEPTB;MT6yNlE4PyEQvF2= NHSxO2VUSU6JRWK=
KYSE-270 MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwMkm3N|Qh|ryP MkfwV2FPT0WU
A4-Fuk MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnDRlFCUUN3ME2xMlI6QTl|IN88US=> NX;NW3U6W0GQR1XS
A498 M4X3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELvUWlKSzVyPUGuN|A1PzRizszN NGXhUHdUSU6JRWK=
SK-MEL-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL5TWM2OD1zLkOwOlc6KM7:TR?= NV:0WXBiW0GQR1XS
AU565 M1fQfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTFwM{G4OlMh|ryP MkO2V2FPT0WU
Saos-2 NIXaTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v0dGlEPTB;MT6zN|IxPSEQvF2= MmKzV2FPT0WU
A549 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\hTmFWUUN3ME2xMlM6QTdizszN M{\udXNCVkeHUh?=
BFTC-909 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\EUoN1UUN3ME2xMlQ{OzB3IN88US=> NED2Ro1USU6JRWK=
MDA-MB-415 NVTpb41XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLQTWM2OD1zLkS4OlkzKM7:TR?= NFe5PZZUSU6JRWK=
639-V NUXNN4h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j6WWlEPTB;MT61NFI1PSEQvF2= NETpU5NUSU6JRWK=
A704 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rae2lEPTB;MT61NFc5PSEQvF2= M2HySHNCVkeHUh?=
PANC-03-27 MlPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlewTWM2OD1zLkWxOFA5KM7:TR?= MoqyV2FPT0WU
SK-MEL-28 NX61N5RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwNU[wPFUh|ryP NH[xeZZUSU6JRWK=
Ramos-2G6-4C10 NISzb2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXQc4pFUUN3ME2xMlYxPzR4IN88US=> MnLGV2FPT0WU
HuP-T4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:0[|VKSzVyPUGuOlA4PzhizszN NHy0N4xUSU6JRWK=
VA-ES-BJ MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\wWWRXUUN3ME2xMlYyOjdizszN MXPTRW5ITVJ?
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KGN Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTR6LkOwOlMh|ryP MU\TRW5ITVJ?
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... 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 to the product individually and in order:
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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID