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 63 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 NF\4U|RMcW6jc3WgRZN{[Xl? MXyxJIg> M3LvNWROW09? NW\KV|lSUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDk[Yx1[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN MYOxPFc2PDZ3NB?=
Sf9 NG[yT3JMcW6jc3WgRZN{[Xl? M2\kdVEhcA>? MoTlSG1UVw>? NGC4VmRKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEhUDFyNEetVkBufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMECzJO69VQ>? NXXjbm5bOTh5NUS2OVQ>
Sf9 MVHLbY5ie2ViQYPzZZk> NIL2cpEyKGh? MoPkSG1UVw>? NHW5XVFKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEhTTV2NT3LJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO NFmxO3MyQDd3NE[1OC=>
Sf9 MVLLbY5ie2ViQYPzZZk> MYmxJIg> M4[0b2ROW09? NWnwd2FSUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= NFvHTI0yQDd3NE[1OC=>
Sf9 NYjXUG1UU2mwYYPlJGF{e2G7 Mmr4NUBp NVP1WGdXTE2VTx?= NGDDU2tKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHHsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhi MXGxPFc2PDZ3NB?=
MDA-MB-361 MkPPSpVv[3Srb36gRZN{[Xl? NY[1NJF3OiCq Mon5SG1UVw>? NWroS|VoUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO M{LOelE5PzV2NkW0
PC3 NFvUe4FHfW6ldHnvckBCe3OjeR?= NW\aXIRJOiCq MVPEUXNQ NYXVO212UW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gVGM{KGOnbHzzJJdqfGhiSVO1NEBw\iByLkCzO{DPxE1? Mm\iNVg4PTR4NUS=
U87MG NX:4WWF7TnWwY4Tpc44hSXO|YYm= MWmyJIg> Mlj6SG1UVw>? M4D2dWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? M4n1[|E5PzV2NkW0
MDA-MB-361 M2G3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XGdFk3KGh? M{TxNGROW09? NFXnVFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> Mo\DNVg4PTR4NUS=
A2780 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\BWIZFQTZiaB?= MoLhSG1UVw>? NIG5XmFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= NFTHOFUyQDd3NE[1OC=>
PC3 M3f1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLPVYhcA>? MWHEUXNQ NXv1NVJDUUN3ME2wMlI5KM7:TR?= NGnDRYIyQDd3NE[1OC=>
U87MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXUPVYhcA>? Mo\MSG1UVw>? M{S2cmlEPTB;MD65OUDPxE1? NX7BfY9OOTh5NUS2OVQ>
Sf9 MYfLbY5ie2ViQYPzZZk> M2HyOFMxKG2rbh?= MlvCSG1UVw>? MmHtTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= MWCyNlU1QDN2Mh?=
RAW 264.7 NGHINVBMcW6jc3WgRZN{[Xl? NHzCRmk6OCCvaX6= NF;CbZpFVVOR M13DUWlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvOjl6IN88US=> NVrkSJA5OjJ3NEizOFI>
Sf9 M{T1XmtqdmG|ZTDBd5NigQ>? NGLzeXYyKGh? MUfJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZoV1[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW0Z7IHPlcIx{KHerdHigTWM2OCCxZjCwMlAyPyEQvF2= NEKwVVMzOzV2ME[0OS=>
Sf9 MmfhT4lv[XOnIFHzd4F6 MkDDNUBp M4\5ZmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= NVrCNphlOjN3NEC2OFU>
Sf9 M1TEXGtqdmG|ZTDBd5NigQ>? MUKxJIg> M3rrVmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= M2nrTVI{PTRyNkS1
Sf9 NHnpW|VMcW6jc3WgRZN{[Xl? MYexJIg> MVTJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm M{nOfVI{PTRyNkS1
SKOV3 NXL5VpFRU2mwYYPlJGF{e2G7 NHzxbI0yKM7:TR?= MVWxJIg> M{m0NWROW09? NFj5[nRKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w MnTCNlM{PjB|NEi=
MCF7 NUnDOZFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzTbXUyKM7:TR?= M{LMPVk3KGh? Mn7HSG1UVw>? MXjHTVUxRTBwMEewNkDPxE1? MXSyN|M3ODN2OB?=
SKOV3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjCUJAyKM7:TR?= NInIRY46PiCq NHTIRnZFVVOR NVvPbWRjT0l3ME2wMlE1PzZizszN M{TONVI{OzZyM{S4
PC3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:3NkBp MV7EUXNQ NUHpOmxvUUN3ME2wMlI5KM7:TR?= MX6yNVk5OTdzNB?=
MCF7.1 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor3O|IhcA>? NGfQWVNFVVOR MnT1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BJTVJ{IHflcoUhf2m2aDDJR|UxKG:oIECuNlgh|ryP MXGyNVk5OTdzNB?=
MCF7-neo/Her2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[3NkBp NEGxXXFFVVOR NF3M[|hKSzVyPUCuNlkh|ryP M3PvU|I{PjZ{OUCz
MCF7-neo/Her2 NH;lbFZMcW6jc3WgRZN{[Xl? MUjJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDTOFc{KHerdHigTWM2OCCxZjCwMlAxPyEQvF2= M4i5OFI{PjZ{OUCz
PC3 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfTfVhUPzJiaB?= MorvSG1UVw>? MkH6SWM2OD1yLkO0JO69VQ>? NWrrb4tCOjF7OEW2N|k>
MCF7.1 NEH3fGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnEO|IhcA>? MWfEUXNQ M{njdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFXDOVAhd2ZiMD6zPUDPxE1? MV2yNVk5PTZ|OR?=
PC3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnzXYNkPzJiaB?= MXfEUXNQ MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCmZX\pZ4lmdnRiaX6gVHRGViC5aYToJGlEPTBib3[gNE4{QSEQvF2= MlXiNlAxPTB4Nkm=
MCF7.1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr1ZlFVPzJiaB?= NX3FNWh[TE2VTx?= NX\oXlRlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigTWM2OCCxZjCwMlM1KM7:TR?= M2fjT|IxODVyNk[5
MCF7.1 NX71cFZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\JO|IhcA>? MYPFR|UxRTBwN{Kg{txO M{fGZVIxOzR4NkW2
NCI-H1975 NYHhfWZvS3m2b4TvfIlkKEG|c3H5 MnrvO|IhcA>? NFS4cXNKSzVyPUCuNlch|ryP Mn3wNlMxPTl3NEW=
H460 M3X3NGN6fG:2b4jpZ{BCe3OjeR?= NEXGVYs4OiCq NV\JNZNKUUN3ME2wMlg4KM7:TR?= MVyyN|A2QTV2NR?=
HT-29 MULDfZRwfG:6aXOgRZN{[Xl? NVf3Z4x2PzJiaB?= M2TSXGlEPTB;MD62OkDPxE1? MYeyN|A2QTV2NR?=
HepG2 MkTQR5l1d3SxeHnjJGF{e2G7 MnfnO|IhcA>? MnGyTWM2OD1zIN88US=> MWWyN|A2QTV2NR?=
SGC7901 MlSyR5l1d3SxeHnjJGF{e2G7 MmfXO|IhcA>? NIr6T2dKSzVyPUGuPEDPxE1? Ml;wNlMxPTl3NEW=
NCI-H226 M1P0N2N6fG:2b4jpZ{BCe3OjeR?= M3v5elczKGh? MYjJR|UxRTJwOTFOwG0> NFLrUGMzOzB3OUW0OS=>
A549 NWXWe4w2S3m2b4TvfIlkKEG|c3H5 M1;MUFczKGh? NWTsR2U{UUN3ME22Mlkh|ryP NF:3fmozOzB3OUW0OS=>
U87MG MVfDfZRwfG:6aXOgRZN{[Xl? M3vpNlczKGh? M{f0V2lEPTB;Nz63O{DPxE1? NUC5UHlHOjNyNUm1OFU>
HBC4 NUPRTIRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvacI9oT0l3ME2tOk4xOyCP MmDNNlI{OzZ{NE[=
BSY1 MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILpfVNtd2eJSUWwQU03NjlyIF2= MUeyNlM{PjJ2Nh?=
HBC5 NFKwTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrGRWxtd2eJSUWwQU03NjZyIF2= M1\nXFIzOzN4MkS2
MCF7 NHzaSo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTrcI9oT0l3ME2tO{4{OyCP MVOyNlM{PjJ2Nh?=
MDA-MB-231 NWDkSHZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD1Uod6dG:pR1m1NF0uPS52NjDN M4HDXFIzOzN4MkS2
U251 NWDQUmFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlWycI9oT0l3ME2tOU42OCCP MmHRNlI{OzZ{NE[=
SF268 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{K2fYxw\0eLNUC9MVUvOzliTR?= MlziNlI{OzZ{NE[=
SF295 NWi3XI1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7sc4dIUTVyPT22MlM4KE1? MV2yNlM{PjJ2Nh?=
SF539 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGyTpBtd2eJSUWwQU03NjVyIF2= NWjPOnNSOjJ|M{[yOFY>
SNB75 M2HPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\FVIxw\0eLNUC9MVcvOTBiTR?= M2LHZlIzOzN4MkS2
SNB78 Mly0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfhd|Ztd2eJSUWwQU03NjV{IF2= MW[yNlM{PjJ2Nh?=
HCC2998 M1zOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXNcI9oT0l3ME2tOk4zQSCP MXmyNlM{PjJ2Nh?=
KM12 M2rh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW2Opptd2eJSUWwQU02Njd4IF2= NYTFe2gxOjJ|M{[yOFY>
HT-29 NF;zc2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLXW5NWdG:pR1m1NF0uPi5|MDDN NXu0eWxROjJ|M{[yOFY>
HCT15 NI[0UYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrpS2Rtd2eJSUWwQU03NjF{IF2= NH\zfYYzOjN|NkK0Oi=>
HCT116 NIfNOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7sc4dIUTVyPT21Mlg4KE1? M3ToTFIzOzN4MkS2
NCI-H23 NFjxOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3ocI9oT0l3ME2tOU44OyCP MnTyNlI{OzZ{NE[=
NCI-H226 M3i5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHUXGNTdG:pR1m1NF0uPi5{MTDN NVKxT2RqOjJ|M{[yOFY>
NCI-H522 M{nifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXsc4dIUTVyPT22MlU5KE1? NU[wPIZ1OjJ|M{[yOFY>
NCI-H483 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;sc4dIUTVyPT22MlU3KE1? MkfaNlI{OzZ{NE[=
A549 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M374T4xw\0eLNUC9MVYvOTViTR?= NGT3eHozOjN|NkK0Oi=>
DMS273 NHS2bpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPsc4dIUTVyPT22MlQ{KE1? MmOyNlI{OzZ{NE[=
DMS114 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr5cI9oT0l3ME2tOU46OiCP M1\nUFIzOzN4MkS2
LOXIMVI M1u1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[5OYxw\0eLNUC9MVYvOjliTR?= MX6yNlM{PjJ2Nh?=
OVCAR3 M32xfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\LNZVtd2eJSUWwQU03NjdzIF2= MX:yNlM{PjJ2Nh?=
OVCAR4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LndIxw\0eLNUC9MVUvPzZiTR?= NYHxTIk1OjJ|M{[yOFY>
OVCAR5 M3jtXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjYcI9oT0l3ME2tOk4zPiCP Mo\KNlI{OzZ{NE[=
OVCAR8 NVrvb4N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTURWVtd2eJSUWwQU02Njd|IF2= NGnWS|gzOjN|NkK0Oi=>
SKOV3 M2G0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonWcI9oT0l3ME2tOk42OiCP MmLCNlI{OzZ{NE[=
RXF631L MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\1XI9mdG:pR1m1NF0uPi56ODDN MX2yNlM{PjJ2Nh?=
ACHN NF3vN|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3sc4dIUTVyPT22MlA4KE1? M{fvflIzOzN4MkS2
St-4 NWKwe5N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[1SllXdG:pR1m1NF0uPS53NjDN MUOyNlM{PjJ2Nh?=
MKN1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnsc4dIUTVyPT23MlA5KE1? NXXkd|h[OjJ|M{[yOFY>
MKN7 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj2d|Vtd2eJSUWwQU03NjVyIF2= MYeyNlM{PjJ2Nh?=
MKN28 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXjTlBXdG:pR1m1NF0uPS53MjDN NIDv[3ozOjN|NkK0Oi=>
MKN45 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke3cI9oT0l3ME2tOk42PSCP MmDUNlI{OzZ{NE[=
MKN74 Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn4cVZtd2eJSUWwQU03NjB{IF2= Mlj4NlI{OzZ{NE[=
DU145 M{\NfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XLUoxw\0eLNUC9MVUvQDViTR?= NUKwbnRKOjJ|M{[yOFY>
PC3 NEDVdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXnNXltd2eJSUWwQU03NjZ4IF2= NFznUWwzOjN|NkK0Oi=>
ES5 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjLW|hYUUN3ME21NE4zOSCwTR?= NXHHc3g2W0GQR1XS
HH NU[4UZJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFzMT6wPEBvVQ>? MXjTRW5ITVJ?
MHH-PREB-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvhdWhuUUN3ME2xNVQvOyCwTR?= MWXTRW5ITVJ?
NCI-H1770 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnidIlGUUN3ME2xNlMvQDZibl2= M2\5NnNCVkeHUh?=
HuO9 NHnURpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITpenlKSzVyPUKwOk4xOiCwTR?= MmjwV2FPT0WU
HAL-01 NXTr[JFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXqXFRKSzVyPUKwOk44OyCwTR?= M3zmfXNCVkeHUh?=
NOS-1 NF\ISGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzSTWM2OD1{MUGuPFIhdk1? NWTSdFhkW0GQR1XS
HGC-27 M4CyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJzMj61O{BvVQ>? MYPTRW5ITVJ?
NB69 NFrF[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXxenlKSzVyPUK0OU4zPyCwTR?= NFexdopUSU6JRWK=
RS4-11 NEHO[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1H3UmlEPTB;Mk[xMlc3KG6P NFrCTFNUSU6JRWK=
DOK M3LW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPkZo1pUUN3ME2zNFEvPyCwTR?= NITXbolUSU6JRWK=
LB2241-RCC MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q5[mlEPTB;M{CzMlg1KG6P MWfTRW5ITVJ?
NCI-H1623 M3LFb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTsTWM2OD1|MESuNFghdk1? NU\4cWVRW0GQR1XS
YH-13 M1Hxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTRU4JuUUN3ME2zNFQvOzJibl2= Mn3PV2FPT0WU
BPH-1 NHTBUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DyTmlEPTB;M{G0JI5O M4TnXnNCVkeHUh?=
AN3-CA M2TDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fsTmlEPTB;M{SwMlM4KG6P M2\DZ3NCVkeHUh?=
ES7 NUHwSWpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfWOVdJUUN3ME2zOFEvQTlibl2= MnHlV2FPT0WU
MDA-MB-175-VII MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W1b2lEPTB;M{WyMlkzKG6P MWHTRW5ITVJ?
GAMG NFvnSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTN5MD64OUBvVQ>? MmrSV2FPT0WU
CHL-1 M3fSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTN5OD62OUBvVQ>? NGDxPY9USU6JRWK=
NB7 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzoTWM2OD1|OEmuPFMhdk1? MkH4V2FPT0WU
MFE-280 NYftWWt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TlRWlEPTB;NEG4MlIhdk1? M1PTVnNCVkeHUh?=
HL-60 M{LmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR{NT63OUBvVQ>? Ml\mV2FPT0WU
GCIY MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTR|Mz64JI5O MmGwV2FPT0WU
MDA-MB-361 M1\oO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonBTWM2OD12M{muNVMhdk1? M2\WU3NCVkeHUh?=
LXF-289 NVfzOnJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR2OD6yO{BvVQ>? MU\TRW5ITVJ?
NBsusSR Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR6OD64OUBvVQ>? NFjmZWpUSU6JRWK=
KU-19-19 M{GxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTVzNj6wO{BvVQ>? M2LCTHNCVkeHUh?=
A204 M2DVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTV{Mj6zN{BvVQ>? MXnTRW5ITVJ?
LB1047-RCC NH22T41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVyyNmduUUN3ME21NlIvQTNibl2= M17Sc3NCVkeHUh?=
COLO-684 NEPmR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjkWlBKSzVyPUWyN{4yOSCwTR?= MWLTRW5ITVJ?
PA-1 NVjtcoYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfLUZEzUUN3ME21N|IvPDFibl2= M4n0e3NCVkeHUh?=
MG-63 NHzWSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\jUGlEPTB;NUSxMlEyKG6P NF\H[mxUSU6JRWK=
BHT-101 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDZTWM2OD13NESuPVQhdk1? NF3WXmxUSU6JRWK=
NKM-1 M3WxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTV7Mz6wPUBvVQ>? NVPWbpJpW0GQR1XS
T47D MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PZNmlEPTB;NUm3MlU3KG6P MWHTRW5ITVJ?
MOLT-4 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfYVlVSUUN3ME22NlMvPjJibl2= NIXUXnRUSU6JRWK=
IGROV-1 M1\uRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr5TWM2OD14M{SuN|Ehdk1? M37OS3NCVkeHUh?=
ES4 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvjTWM2OD14M{muOVQhdk1? NHXTTXNUSU6JRWK=
HuO-3N1 NYT0fJlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T6OWlEPTB;NkSyMlM5KG6P M4D4c3NCVkeHUh?=
NEC8 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjEZ|lKSzVyPU[1N{42PyCwTR?= MWjTRW5ITVJ?
HO-1-N-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTZ3OT6xO{BvVQ>? M{jlTHNCVkeHUh?=
EPCL-272H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUGzO2dmUUN3ME22PFcvOjFibl2= NVLKe29NW0GQR1XS
D-263MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzoSm5GUUN3ME23NVgvOSCwTR?= MXjTRW5ITVJ?
MV-4-11 NEPoSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzxTWM2OD15MkSuN|Ehdk1? M17OWnNCVkeHUh?=
SK-NEP-1 MnXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e5SWlEPTB;N{K1Mlk1KG6P NHvzVmZUSU6JRWK=
SW872 M33pNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz6TWM2OD15MkeuPFkhdk1? MVLTRW5ITVJ?
P30-OHK MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTd|MD63NUBvVQ>? NGTSfolUSU6JRWK=
OMC-1 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz1PXZKSzVyPUe1NU4xQSCwTR?= M3TxdnNCVkeHUh?=
LoVo MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV75WmhCUUN3ME23O|cvQSCwTR?= NEDEUYJUSU6JRWK=
LNCaP-Clone-FGC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnNTWM2OD15OU[uN|Qhdk1? MoP6V2FPT0WU
L-363 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFO5NpJKSzVyPUe5PE41OiCwTR?= NFPhSHFUSU6JRWK=
ES8 NIjnNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2H5W2lEPTB;OEGwMlUzKG6P NHLKcnhUSU6JRWK=
697 M3v1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjyfVFKSzVyPUizNU42PSCwTR?= MkXSV2FPT0WU
HSC-3 MnH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTh|OT61OEBvVQ>? NEjmbVFUSU6JRWK=
H4 NXPUfHhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnviTWM2OD16NUCuPFUhdk1? NVXxXXVWW0GQR1XS
QIMR-WIL MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zRPWlEPTB;OE[1MlIhdk1? M17GOXNCVkeHUh?=
OAW-42 NWH2NI1bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr0WlN[UUN3ME24O|IvOTlibl2= MYfTRW5ITVJ?
MCF7 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zESWlEPTB;OEm4MlU6KG6P MYDTRW5ITVJ?
SCC-25 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXxTWM2OD17MUSuNVkhdk1? NXW4fZZyW0GQR1XS
NCI-H1563 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDjXZpqUUN3ME25NVUvQTlibl2= M{TJVnNCVkeHUh?=
OVCAR-5 NIPuc4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTl2MD6xO{BvVQ>? NWPLV5o{W0GQR1XS
HDLM-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTl2OT6yJI5O M4n4UHNCVkeHUh?=
NB5 M3fYTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTHTWM2OD17NU[uOkBvVQ>? MYfTRW5ITVJ?
NCI-H292 MnHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\OdWlEPTB;OUe0MlMzKG6P Mkm4V2FPT0WU
A101D NWDpfJF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnUclBKSzVyPUm5NE4yQSCwTR?= NHrU[pZUSU6JRWK=
NCI-H1648 NInVcYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrucVJYUUN3ME25PVgvPTFibl2= M4fIdHNCVkeHUh?=
EKVX M{exSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvhbpNKSzVyPUGuNFEzQSEQvF2= MXrTRW5ITVJ?
SW1710 NWHvTXR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v4e2lEPTB;MT6wOFI{OyEQvF2= NIj4WldUSU6JRWK=
WM-115 NUDzfmxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml6yTWM2OD1zLkC2OlU3KM7:TR?= NEnPTWJUSU6JRWK=
CAL-54 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHHTWM2OD1zLkC3NFgyKM7:TR?= MWHTRW5ITVJ?
TGBC24TKB MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDsSpB7UUN3ME2xMlA5ODR3IN88US=> NFPqU2lUSU6JRWK=
NCI-H520 M{XUbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFwMEi5Olch|ryP MX\TRW5ITVJ?
D-423MG MmjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwMEm5OlIh|ryP M1rTfHNCVkeHUh?=
BFTC-905 NFTzbY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPYd2JKSzVyPUGuNVM1PDlizszN MlLBV2FPT0WU
HT NH:zdWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwMUO0O|gh|ryP MW\TRW5ITVJ?
CTB-1 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[0OIxLUUN3ME2xMlE1Ojl|IN88US=> M1;lZnNCVkeHUh?=
Hs-578-T NYLIWJYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvuN2pvUUN3ME2xMlE6PTZ3IN88US=> MmnoV2FPT0WU
HuH-7 NFjDPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjXTWM2OD1zLkKwPVQ6KM7:TR?= MlOwV2FPT0WU
LB996-RCC NXLrPIRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zBWmlEPTB;MT6yNlE4PyEQvF2= M2XieXNCVkeHUh?=
KYSE-270 MkntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PlcWlEPTB;MT6yPVc{PCEQvF2= M1XXTXNCVkeHUh?=
A4-Fuk NFG3dnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\vPZFKSzVyPUGuNlk6QTNizszN NIXwVoNUSU6JRWK=
A498 MnPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LPbWlEPTB;MT6zNFQ4PCEQvF2= M1uwT3NCVkeHUh?=
SK-MEL-1 M4rTNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfv[HJKSzVyPUGuN|A3PzlizszN MUnTRW5ITVJ?
AU565 M2Die2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITZdXBKSzVyPUGuN|E5PjNizszN MYjTRW5ITVJ?
Saos-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr1Zm5KSzVyPUGuN|MzODVizszN NGLKdYhUSU6JRWK=
A549 NXzQVpRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi3SmpKUUN3ME2xMlM6QTdizszN MXvTRW5ITVJ?
BFTC-909 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwNEOzNFUh|ryP NH;Xe3pUSU6JRWK=
MDA-MB-415 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrveFR5UUN3ME2xMlQ5Pjl{IN88US=> MYPTRW5ITVJ?
639-V NWLYWHhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTFwNUCyOFUh|ryP MVPTRW5ITVJ?
A704 MnrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\RTWM2OD1zLkWwO|g2KM7:TR?= NF7M[GFUSU6JRWK=
PANC-03-27 M2[3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;lbmNKSzVyPUGuOVE1ODhizszN M33MO3NCVkeHUh?=
SK-MEL-28 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\STWM2OD1zLkW2NFg2KM7:TR?= NEPVSnpUSU6JRWK=
Ramos-2G6-4C10 M1vEZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW1TWM2OD1zLk[wO|Q3KM7:TR?= NUTsNVMzW0GQR1XS
HuP-T4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL6cZY4UUN3ME2xMlYxPzd6IN88US=> Mlr6V2FPT0WU
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S-117 NXraSlNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjTbIJ[UUN3ME2yPU4{QDV5IN88US=> MXXTRW5ITVJ?
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HCT-116 NI\kUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV20OoQ5UUN3ME2zNE42PTV2IN88US=> M{OzT3NCVkeHUh?=
NCI-H1693 NF\m[2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;E[3JKSzVyPUOwMlU6PDJizszN NH;KTFFUSU6JRWK=
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NCI-H661 MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjt[phKSzVyPUOyMlA3OjNizszN M4DsXnNCVkeHUh?=
NCI-H2347 NEDORWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO2TWM2OD1|Mj60PFM4KM7:TR?= MVHTRW5ITVJ?
FTC-133 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HaeGlEPTB;M{KuO|A3KM7:TR?= NHe4b3lUSU6JRWK=
COLO-829 NHXP[IlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXDTWM2OD1|Mz6zOFY4KM7:TR?= Ml2yV2FPT0WU
GOTO M4HOW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjpRZhKSzVyPUOzMlUzPThizszN MV\TRW5ITVJ?
YAPC MnLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe4Z3VKSzVyPUOzMlgyPTlizszN NXvCO5NpW0GQR1XS
LCLC-103H MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrCWVVtUUN3ME2zOE4yPjJ2IN88US=> NUTCUXcxW0GQR1XS
SiHa NF\xR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DCTWlEPTB;M{SuN|gyPyEQvF2= MnXkV2FPT0WU
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NCI-SNU-1 Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTN3LkG3PUDPxE1? MXLTRW5ITVJ?
KNS-81-FD NEXuWGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPRTWM2OD1|NT62OlMh|ryP NYXwRoVSW0GQR1XS
SCC-9 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnkTWM2OD1|Nj63NVQ3KM7:TR?= MVnTRW5ITVJ?
SH-4 M1j6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHzO|NKSzVyPUO2Mlc{KM7:TR?= MX;TRW5ITVJ?
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COLO-678 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zEe2lEPTB;M{euPVQ{PyEQvF2= MVfTRW5ITVJ?
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OAW-28 NHviWnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:xXWlEPTB;M{iuOlM6KM7:TR?= M{CxSnNCVkeHUh?=
CAMA-1 M{jITGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq2XFVKSzVyPUO4Mlk3QTFizszN NXjoVHJMW0GQR1XS
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A3-KAW M37mNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDtdGVKSzVyPUSwMlM3PjFizszN MofJV2FPT0WU
SK-MEL-24 NVqzXZNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPxTWM2OD12MD61PVMyKM7:TR?= M3zMWHNCVkeHUh?=
KYSE-140 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[2WmlEPTB;NECuO|E3PSEQvF2= MmPQV2FPT0WU
MOLT-16 NFPZWYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTvRmxXUUN3ME20NU4yPTN4IN88US=> MYHTRW5ITVJ?
CFPAC-1 MmX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTR{LkWyNVEh|ryP MYrTRW5ITVJ?
NB14 NWH3PZFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj3cZBiUUN3ME20Nk44ODJ5IN88US=> NH7aV4FUSU6JRWK=
COLO-792 NHrob3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTR{Lki5OlEh|ryP MVrTRW5ITVJ?
RH-1 MnHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13SUGlEPTB;NEOuOFg{PiEQvF2= NXXvUlRbW0GQR1XS
NCI-H522 NH3QSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\rTWM2OD12ND6zOVY5KM7:TR?= M1TwOnNCVkeHUh?=
Ca-Ski M{i0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTR2LkixNVQh|ryP NHTTTnlUSU6JRWK=
KGN MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLJbW9pUUN3ME20PE4{ODZ|IN88US=> Mn3DV2FPT0WU
UACC-62 Mme4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGybG9KSzVyPUS4MlQxPzJizszN NUfGXIViW0GQR1XS
NCI-H358 NYrWSYhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR7LkOwNVgh|ryP M{XUPHNCVkeHUh?=
LS-411N NFLm[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnr5TWM2OD12OT6zNVE5KM7:TR?= NGiw[2hUSU6JRWK=
IST-MES1 MnnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nUVWlEPTB;NEmuOVYzPSEQvF2= NXPhc5lWW0GQR1XS

... 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(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

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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
NCT02092831 Completed Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT02092831 Completed Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 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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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID