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.

  •  

    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 NFe3e5BMcW6jc3WgRZN{[Xl? M2nMV|EhcA>? MVfEUXNQ MnywTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCmZXz0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wNFMh|ryP NH\4dmEyQDd3NE[1OC=>
Sf9 NW\OSYc3U2mwYYPlJGF{e2G7 M4C2bFEhcA>? NUPSZYhbTE2VTx?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgTFExPDdvUjDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> MXGxPFc2PDZ3NB?=
Sf9 M1j1XmtqdmG|ZTDBd5NigQ>? NGLPUnoyKGh? NX\JfXhHTE2VTx?= NV3ndIM3UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEV3NEWtT{BufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMECzJO69VQ>? NYq1OppIOTh5NUS2OVQ>
Sf9 MYrLbY5ie2ViQYPzZZk> NHHOXlMyKGh? NHXkZpJFVVOR NYHlU5JOUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= NIXHVHkyQDd3NE[1OC=>
Sf9 MWLLbY5ie2ViQYPzZZk> MV:xJIg> NX\NZ|BtTE2VTx?= M132TWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> NVzpe5k4OTh5NUS2OVQ>
MDA-MB-361 MVHGeY5kfGmxbjDBd5NigQ>? M4TxS|IhcA>? MXPEUXNQ NX;INGxTUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO MmTqNVg4PTR4NUS=
PC3 NXLvWmNvTnWwY4Tpc44hSXO|YYm= MmPPNkBp M4ntU2ROW09? NHLLRYpKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? M{ntS|E5PzV2NkW0
U87MG M33UPWZ2dmO2aX;uJGF{e2G7 MnixNkBp NHTxUYJFVVOR MknVTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? NVnB[JFROTh5NUS2OVQ>
MDA-MB-361 NV7XVll5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT3UlU{QTZiaB?= MUHEUXNQ NXnJTHJwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC55MjFOwG0> M3rOcVE5PzV2NkW0
A2780 M1rF[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETmOZk6PiCq NY\sd|g5TE2VTx?= MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IIfpeIghWEmNM1PBJIFv\CCSVFXOJI12fGG2aX;uJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? M4LTfFE5PzV2NkW0
PC3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHzbmNXQTZiaB?= MYLEUXNQ NWDBW4dMUUN3ME2wMlI5KM7:TR?= NU\rW2VWOTh5NUS2OVQ>
U87MG MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkSwPVYhcA>? NFW1O3JFVVOR M4G3PGlEPTB;MD65OUDPxE1? NITXUVUyQDd3NE[1OC=>
Sf9 NF:0[2lMcW6jc3WgRZN{[Xl? MnPKN|AhdWmw MlXxSG1UVw>? NFi3N4ZKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgZY1wfW62IH;mJGFVWCClb37zeY1m\CC5aYToJGlEPTBib3[gNE4xPDJizszN M2O1bVIzPTR6M{Sy
RAW 264.7 NXewRZJRU2mwYYPlJGF{e2G7 MoX5PVAhdWmw NXvzNFk1TE2VTx?= NHTFd|RKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> Mm\TNlI2PDh|NEK=
Sf9 Ml;KT4lv[XOnIFHzd4F6 M1P3UVEhcA>? NGmzeXBKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> NV3XPWxIOjN3NEC2OFU>
Sf9 MYjLbY5ie2ViQYPzZZk> MUixJIg> NYLnN406UW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> NGjKc5UzOzV2ME[0OS=>
Sf9 M13GZ2tqdmG|ZTDBd5NigQ>? NHTyc2gyKGh? Mk\YTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4didW2jIHX4dJJme3OnZB?= NUj2XXdOOjN3NEC2OFU>
Sf9 NX70S41OU2mwYYPlJGF{e2G7 MYmxJIg> MkTsTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZB?= Ml\uNlM2PDB4NEW=
SKOV3 NXzxXGNGU2mwYYPlJGF{e2G7 MXyxJO69VQ>? NV;Q[oRpOSCq MUjEUXNQ NGfSU5FKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w M3jrdVI{OzZyM{S4
MCF7 Mn;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXzNUDPxE1? M2jqelk3KGh? M2jSZWROW09? NIHtXW1IUTVyPUCuNFcxOiEQvF2= NF7mcm4zOzN4MEO0PC=>
SKOV3 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXEPHZuOSEQvF2= NHH1PHI6PiCq MkXiSG1UVw>? MXTHTVUxRTBwMUS3OkDPxE1? M1\PWlI{OzZyM{S4
PC3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Py[FczKGh? MnHRSG1UVw>? Mk[5TWM2OD1yLkK4JO69VQ>? M3mxeVIyQThzN{G0
MCF7.1 NEPZR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7uO|IhcA>? NFLYSZpFVVOR NUTBVXc2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCKRWKyJIdmdmVid3n0bEBKSzVyIH;mJFAvOjhizszN M1TSbFIyQThzN{G0
MCF7-neo/Her2 M4raPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHIe2ZmPzJiaB?= M3;oXWROW09? MV3JR|UxRTBwMkmg{txO NEDkZmszOzZ4MkmwNy=>
MCF7-neo/Her2 NHrtVppMcW6jc3WgRZN{[Xl? M3\rO2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> MVyyN|Y3OjlyMx?=
PC3 NI\1dIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\DOlczKGh? NWjHclBsTE2VTx?= M3PucGVEPTB;MD6zOEDPxE1? M{PhPVIyQTh3NkO5
MCF7.1 NUnJdJhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS3NkBp MUnEUXNQ MnnKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? NHTwZlczOTl6NU[zPS=>
PC3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\TO|IhcA>? M{joS2ROW09? Ml;HRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiZHXmbYNq\W62IHnuJHBVTU5id3n0bEBKSzVyIH;mJFAvOzlizszN NFXadXQzODB3ME[2PS=>
MCF7.1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G2O|czKGh? M{excWROW09? NF7WSWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDJR|UxKG:oIECuN|Qh|ryP M4[zXFIxODVyNk[5
MCF7.1 M1PJc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\wUZBQPzJiaB?= Mny0SWM2OD1yLkeyJO69VQ>? MViyNFM1PjZ3Nh?=
NCI-H1975 NXyxNZc2S3m2b4TvfIlkKEG|c3H5 M3H2OVczKGh? M2jtfGlEPTB;MD6yO{DPxE1? M{flRVI{ODV7NUS1
H460 M2e5V2N6fG:2b4jpZ{BCe3OjeR?= NHiyUGU4OiCq M3z4PWlEPTB;MD64O{DPxE1? M1\2O|I{ODV7NUS1
HT-29 NGDXToNEgXSxdH;4bYMhSXO|YYm= MkeyO|IhcA>? NGDo[VdKSzVyPUCuOlYh|ryP M3TBeVI{ODV7NUS1
HepG2 MWnDfZRwfG:6aXOgRZN{[Xl? MYO3NkBp NH:wZoRKSzVyPUGg{txO NYj3SGZmOjNyNUm1OFU>
SGC7901 NI\VOWZEgXSxdH;4bYMhSXO|YYm= M3n1dVczKGh? NXLHR2VDUUN3ME2xMlgh|ryP M33pfFI{ODV7NUS1
NCI-H226 NUPWeFI5S3m2b4TvfIlkKEG|c3H5 NHPX[|E4OiCq M3rtbWlEPTB;Mj65JO69VQ>? M3jxbFI{ODV7NUS1
A549 NF\BU3REgXSxdH;4bYMhSXO|YYm= NYLGb|E5PzJiaB?= NX\uPXRyUUN3ME22Mlkh|ryP MkLuNlMxPTl3NEW=
U87MG NVK1ZZRJS3m2b4TvfIlkKEG|c3H5 NX;GNll4PzJiaB?= Mn;3TWM2OD15Lke3JO69VQ>? MX2yN|A2QTV2NR?=
HBC4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\mVYttd2eJSUWwQU03NjB|IF2= NFXNZlYzOjN|NkK0Oi=>
BSY1 NEjzVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH6wcGFtd2eJSUWwQU03NjlyIF2= NHWxcVczOjN|NkK0Oi=>
HBC5 MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfuR|Ftd2eJSUWwQU03NjZyIF2= NWTIPXE5OjJ|M{[yOFY>
MCF7 NWK1N|d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPrNmhZdG:pR1m1NF0uPy5|MzDN M{DiSVIzOzN4MkS2
MDA-MB-231 NWK1PItzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jJU4xw\0eLNUC9MVUvPDZiTR?= NV\TOW42OjJ|M{[yOFY>
U251 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fjWoxw\0eLNUC9MVUvPTBiTR?= NHzNSGczOjN|NkK0Oi=>
SF268 NVPsdolUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PVVIxw\0eLNUC9MVUvOzliTR?= NGTKXVczOjN|NkK0Oi=>
SF295 M4rjd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Pyb4xw\0eLNUC9MVYvOzdiTR?= MnXSNlI{OzZ{NE[=
SF539 NEjwXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fJdoxw\0eLNUC9MVYvPTBiTR?= NVL1NFltOjJ|M{[yOFY>
SNB75 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfmUlZpdG:pR1m1NF0uPy5zMDDN MlL2NlI{OzZ{NE[=
SNB78 NVjKN3h3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrCcI9oT0l3ME2tOk42OiCP NVy4[ItuOjJ|M{[yOFY>
HCC2998 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDsc4dIUTVyPT22MlI6KE1? NFSzW24zOjN|NkK0Oi=>
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NCI-H226 NGjV[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDGe5htd2eJSUWwQU03NjJzIF2= Mon5NlI{OzZ{NE[=
NCI-H522 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\6VI5td2eJSUWwQU03NjV6IF2= MVqyNlM{PjJ2Nh?=
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A549 NYPrXXltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rxWIxw\0eLNUC9MVYvOTViTR?= NFXoNIgzOjN|NkK0Oi=>
DMS273 NWrIWo17T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTrcI9oT0l3ME2tOk41OyCP NX7Jb|B[OjJ|M{[yOFY>
DMS114 M1zpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHsc4dIUTVyPT21MlkzKE1? M2C4ZVIzOzN4MkS2
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OVCAR3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXvO3FCdG:pR1m1NF0uPi55MTDN M3LkOFIzOzN4MkS2
OVCAR4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvpUWZtd2eJSUWwQU02Njd4IF2= NVnSV4tkOjJ|M{[yOFY>
OVCAR5 M1HNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFqwRWFtd2eJSUWwQU03NjJ4IF2= MXeyNlM{PjJ2Nh?=
OVCAR8 MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3ucI9oT0l3ME2tOU44OyCP NWPBVIFUOjJ|M{[yOFY>
SKOV3 NVfCNGd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7yenpUdG:pR1m1NF0uPi53MjDN MVOyNlM{PjJ2Nh?=
RXF631L Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTxU3UxdG:pR1m1NF0uPi56ODDN MnLGNlI{OzZ{NE[=
ACHN MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[5botMdG:pR1m1NF0uPi5yNzDN NIPET4ozOjN|NkK0Oi=>
St-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoOzcI9oT0l3ME2tOU42PiCP MUeyNlM{PjJ2Nh?=
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DU145 NYrydZNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P4eYxw\0eLNUC9MVUvQDViTR?= NH7qeXYzOjN|NkK0Oi=>
PC3 MnnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXETFJtd2eJSUWwQU03NjZ4IF2= NHfyeI8zOjN|NkK0Oi=>
ES5 MlTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nqbmlEPTB;NUCuNlEhdk1? NYLwbGNXW0GQR1XS
HH M{TOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTYb|hHUUN3ME2xNVEvODhibl2= NInXPZNUSU6JRWK=
MHH-PREB-1 NEnINXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzWZXh[UUN3ME2xNVQvOyCwTR?= MmfsV2FPT0WU
NCI-H1770 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ixVWlEPTB;MUKzMlg3KG6P NXvISlcxW0GQR1XS
HuO9 NHvLbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJyNj6wNkBvVQ>? NYTqSYtTW0GQR1XS
HAL-01 M3fCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDTXIdFUUN3ME2yNFYvPzNibl2= M3XCXXNCVkeHUh?=
NOS-1 M{PneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTJzMT64NkBvVQ>? NVjHVIM2W0GQR1XS
HGC-27 NYnhOoluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vUSmlEPTB;MkGyMlU4KG6P M4TMTnNCVkeHUh?=
NB69 NXjjZoxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7te3lyUUN3ME2yOFUvOjdibl2= NX;0dZk3W0GQR1XS
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DOK MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfqTWM2OD1|MEGuO{BvVQ>? MU\TRW5ITVJ?
LB2241-RCC NYjFOoF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7uTWM2OD1|MEOuPFQhdk1? NUfDPY5sW0GQR1XS
NCI-H1623 NWftTYFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTNyND6wPEBvVQ>? MlTTV2FPT0WU
YH-13 MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[3O25KSzVyPUOwOE4{OiCwTR?= M4DrOnNCVkeHUh?=
BPH-1 NH3aUFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHzTWM2OD1|MUSgcm0> MlnLV2FPT0WU
AN3-CA NXnHemtsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfIfVZjUUN3ME2zOFAvOzdibl2= MmLQV2FPT0WU
ES7 M4jqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnINYc5UUN3ME2zOFEvQTlibl2= NGq1XJBUSU6JRWK=
MDA-MB-175-VII MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f6d2lEPTB;M{WyMlkzKG6P NF7wWWNUSU6JRWK=
GAMG MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDTVFJKSzVyPUO3NE45PSCwTR?= NHXqOIpUSU6JRWK=
CHL-1 NYjTcmxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPXUVNKSzVyPUO3PE43PSCwTR?= M4TIPXNCVkeHUh?=
NB7 NFr5VGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkOzTWM2OD1|OEmuPFMhdk1? NUPkVI45W0GQR1XS
MFE-280 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPFWI1vUUN3ME20NVgvOiCwTR?= MmLFV2FPT0WU
HL-60 NV;SZnBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR{NT63OUBvVQ>? NYrBV5l5W0GQR1XS
GCIY NYDRd255T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrQb2MyUUN3ME20N|MvQCCwTR?= NFHiTZpUSU6JRWK=
MDA-MB-361 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WwNGlEPTB;NEO5MlE{KG6P M3nOdHNCVkeHUh?=
LXF-289 NWTpU|Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTR2OD6yO{BvVQ>? NWS3NotnW0GQR1XS
NBsusSR MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37QcmlEPTB;NEi4Mlg2KG6P MVTTRW5ITVJ?
KU-19-19 NWjRco1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXPTWM2OD13MU[uNFchdk1? NUX2NnVlW0GQR1XS
A204 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjmcphKSzVyPUWyNk4{OyCwTR?= NES5Z5pUSU6JRWK=
LB1047-RCC MmrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLqNnk4UUN3ME21NlIvQTNibl2= NYC2VYI1W0GQR1XS
COLO-684 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTyOXJKSzVyPUWyN{4yOSCwTR?= M{i0dXNCVkeHUh?=
PA-1 M{jQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTV|Mj60NUBvVQ>? Mnn1V2FPT0WU
MG-63 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDYNGxYUUN3ME21OFEvOTFibl2= NX\5[XRWW0GQR1XS
BHT-101 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTV2ND65OEBvVQ>? MXLTRW5ITVJ?
NKM-1 NF;IboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPDSZlwUUN3ME21PVMvODlibl2= NGHhUWpUSU6JRWK=
T47D MnXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[xVIFmUUN3ME21PVcvPTZibl2= NHP4NGhUSU6JRWK=
MOLT-4 NYLTNIJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWxTWM2OD14MkOuOlIhdk1? NIe4bmRUSU6JRWK=
IGROV-1 NVn3ZWpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;3XYQ3UUN3ME22N|QvOzFibl2= NFGzT5ZUSU6JRWK=
ES4 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTZ|OT61OEBvVQ>? NULYbphQW0GQR1XS
HuO-3N1 M2m2OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTZ2Mj6zPEBvVQ>? NETZUoFUSU6JRWK=
NEC8 NGjLcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHsNFh6UUN3ME22OVMvPTdibl2= MmPhV2FPT0WU
HO-1-N-1 NV\3TGNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TYemlEPTB;NkW5MlE4KG6P MoDWV2FPT0WU
EPCL-272H NUf2TIpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWntd|FvUUN3ME22PFcvOjFibl2= M4LHe3NCVkeHUh?=
D-263MG Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTdzOD6xJI5O MV\TRW5ITVJ?
MV-4-11 NEHMeXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTd{ND6zNUBvVQ>? MWfTRW5ITVJ?
SK-NEP-1 NWnXTpJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTd{NT65OEBvVQ>? NWXT[HExW0GQR1XS
SW872 Mon3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC0XJA6UUN3ME23NlcvQDlibl2= MoHQV2FPT0WU
P30-OHK NVXKWm5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELCNWhKSzVyPUezNE44OSCwTR?= NHf6SGtUSU6JRWK=
OMC-1 M32wZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HpWGlEPTB;N{WxMlA6KG6P NVvIfHQ5W0GQR1XS
LoVo NV3kTGJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXuTWM2OD15N{euPUBvVQ>? NYTzT2p6W0GQR1XS
LNCaP-Clone-FGC NIC4[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;rWlFsUUN3ME23PVYvOzRibl2= M1vCcnNCVkeHUh?=
L-363 M2jPU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW1d2xGUUN3ME23PVgvPDJibl2= Ml\TV2FPT0WU
ES8 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHrUo8{UUN3ME24NVAvPTJibl2= M{PlcnNCVkeHUh?=
697 M1qyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTh|MT61OUBvVQ>? NHHCO3RUSU6JRWK=
HSC-3 NGfifJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTh|OT61OEBvVQ>? MYHTRW5ITVJ?
H4 NH3GVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnPbGRKSzVyPUi1NE45PSCwTR?= MV;TRW5ITVJ?
QIMR-WIL M2Kwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XzNWlEPTB;OE[1MlIhdk1? NGPZWphUSU6JRWK=
OAW-42 M3\BfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF22WnVKSzVyPUi3Nk4yQSCwTR?= MWDTRW5ITVJ?
MCF7 NWf3OWdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLZOGZKSzVyPUi5PE42QSCwTR?= M1jGWHNCVkeHUh?=
SCC-25 NF24U3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jjVGlEPTB;OUG0MlE6KG6P NWGx[HdMW0GQR1XS
NCI-H1563 MkL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3rSY5KSzVyPUmxOU46QSCwTR?= MXLTRW5ITVJ?
OVCAR-5 NYXRO2lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTl2MD6xO{BvVQ>? MXPTRW5ITVJ?
HDLM-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz1WpZQUUN3ME25OFkvOiCwTR?= NVfYZ2VlW0GQR1XS
NB5 NXfCW2R{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy0Z5hKSzVyPUm1Ok43KG6P NVHqR|dWW0GQR1XS
NCI-H292 M2i3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETKR2xKSzVyPUm3OE4{OiCwTR?= MV3TRW5ITVJ?
A101D MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorSTWM2OD17OUCuNVkhdk1? NWnGclNHW0GQR1XS
NCI-H1648 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPleFBtUUN3ME25PVgvPTFibl2= NXqwZ2ZQW0GQR1XS
EKVX NVvicW1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnVSZdKSzVyPUGuNFEzQSEQvF2= M2\5RnNCVkeHUh?=
SW1710 NI\EXlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XuZmlEPTB;MT6wOFI{OyEQvF2= MVjTRW5ITVJ?
WM-115 NXW5ZmluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LlVWlEPTB;MT6wOlY2PiEQvF2= M1TZUXNCVkeHUh?=
CAL-54 Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrFeoNKSzVyPUGuNFcxQDFizszN MWfTRW5ITVJ?
TGBC24TKB M1Xx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfGPJVFUUN3ME2xMlA5ODR3IN88US=> MVzTRW5ITVJ?
NCI-H520 M1jFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XFfGlEPTB;MT6wPFk3PyEQvF2= NUXHeWd[W0GQR1XS
D-423MG NU\vdHVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonqTWM2OD1zLkC5PVYzKM7:TR?= MlHuV2FPT0WU
BFTC-905 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TyOWlEPTB;MT6xN|Q1QSEQvF2= MUnTRW5ITVJ?
HT Mo[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfOTWM2OD1zLkGzOFc5KM7:TR?= M3n4fnNCVkeHUh?=
CTB-1 MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;iTWM2OD1zLkG0Nlk{KM7:TR?= NXrQTVVZW0GQR1XS
Hs-578-T NVv4SGtbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwMUm1OlUh|ryP M374fXNCVkeHUh?=
HuH-7 NH\Kc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMkC5OFkh|ryP MXrTRW5ITVJ?
LB996-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrLTWM2OD1zLkKyNVc4KM7:TR?= MWjTRW5ITVJ?
KYSE-270 MmW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnUSmoyUUN3ME2xMlI6PzN2IN88US=> MofIV2FPT0WU
A4-Fuk M{GwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTFwMkm5PVMh|ryP MWTTRW5ITVJ?
A498 M4\BeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnP[2ZvUUN3ME2xMlMxPDd2IN88US=> M3HON3NCVkeHUh?=
SK-MEL-1 NVPa[GhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHQdldKSzVyPUGuN|A3PzlizszN MlHLV2FPT0WU
AU565 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzrN49KSzVyPUGuN|E5PjNizszN NV3EOFVbW0GQR1XS
Saos-2 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr1bWJKSzVyPUGuN|MzODVizszN M{m4eHNCVkeHUh?=
A549 M4[4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj6d45FUUN3ME2xMlM6QTdizszN Mn3vV2FPT0WU
BFTC-909 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFwNEOzNFUh|ryP NVLycYx6W0GQR1XS
MDA-MB-415 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSxV21OUUN3ME2xMlQ5Pjl{IN88US=> M2mwcnNCVkeHUh?=
639-V M3TY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{W0cmlEPTB;MT61NFI1PSEQvF2= NIXmOW5USU6JRWK=
A704 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTFwNUC3PFUh|ryP MWrTRW5ITVJ?
PANC-03-27 NETQfpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwNUG0NFgh|ryP NGDZfW9USU6JRWK=
SK-MEL-28 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH3S3hKSzVyPUGuOVYxQDVizszN MlzvV2FPT0WU
Ramos-2G6-4C10 M2XqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LIcWlEPTB;MT62NFc1PiEQvF2= NFrmUndUSU6JRWK=
HuP-T4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILiNZFKSzVyPUGuOlA4PzhizszN MX3TRW5ITVJ?
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EFM-19 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofuTWM2OD1zLk[xPFEh|ryP MoPQV2FPT0WU
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D-566MG NF\k[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13oV2lEPTB;MT62NlU{KM7:TR?= NUjNdIN3W0GQR1XS
JVM-3 NYfhe4xST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\Hd2lEPTB;MT62OFg4PSEQvF2= NVvJbJJLW0GQR1XS
TK10 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nVfGlEPTB;MT62O|A5OyEQvF2= M17SWHNCVkeHUh?=
BT-20 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHoVJY2UUN3ME2xMlY5QTB{IN88US=> M331UHNCVkeHUh?=
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CAL-39 NG[1cYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXHW3FKSzVyPUKuNFMzQCEQvF2= MnvSV2FPT0WU
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D-502MG NIDqfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;SPW1ZUUN3ME2yMlMzPDZzIN88US=> M4fLXHNCVkeHUh?=
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Becker MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\DTVBKSzVyPUOuNVY5ODhizszN M{\iN3NCVkeHUh?=
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COR-L23 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\WS2lEPTB;Mz6zO|I4QSEQvF2= MkPIV2FPT0WU
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Mewo MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqxTWM2OD1|LkSyNVgzKM7:TR?= NWTMNGx5W0GQR1XS
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RPMI-2650 NGDQcpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3qTWM2OD1|Lk[wOlM4KM7:TR?= MlnzV2FPT0WU
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NCI-H747 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\aTWM2OD12LkC1OlM5KM7:TR?= MlHVV2FPT0WU
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8-MG-BA NH70[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPiTWhQUUN3ME20Mlg5PTV5IN88US=> MVPTRW5ITVJ?
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RPMI-8226 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj1cmJrUUN3ME21MlA2PDZzIN88US=> MVnTRW5ITVJ?
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CAL-62 M1ezb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfJUpNKSzVyPUWuNVgzPTlizszN NYL4WXROW0GQR1XS
NB10 NFfQWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX3fVc3UUN3ME21MlIzPzR2IN88US=> M3vQXXNCVkeHUh?=
OC-314 M3;ndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTVwM{e0OFQh|ryP NWf4fI81W0GQR1XS
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KGN MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXjV5lKSzVyPUS4MlMxPjNizszN MVfTRW5ITVJ?
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NCI-H358 NUG0WYtkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzRc5BZUUN3ME20PU4{ODF6IN88US=> M{O4[XNCVkeHUh?=
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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(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.64
Formula

C23H27N7O3S2

CAS No. 957054-30-7
Storage powder
in solvent
Synonyms RG7321

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

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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
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
NCT01240226 Completed Healthy Volunteer Genentech Inc. November 2010 Phase 1
NCT00999128 Completed Healthy Volunteers Genentech Inc. October 26 2009 Phase 1

Tech Support

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

Handling Instructions

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

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

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID