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 M3XpVGtqdmG|ZTDBd5NigQ>? MV6xJIg> NIrLT|BFVVOR NYC4d3hVUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDk[Yx1[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN NVXVfVNLOTh5NUS2OVQ>
Sf9 NULhfFQxU2mwYYPlJGF{e2G7 MlvTNUBp MnKzSG1UVw>? NWHOd3NsUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? MYexPFc2PDZ3NB?=
Sf9 NXrxO|lSU2mwYYPlJGF{e2G7 MmrMNUBp MkPlSG1UVw>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN M{m4VFE5PzV2NkW0
Sf9 MnHiT4lv[XOnIFHzd4F6 MVuxJIg> NH\4ZWVFVVOR MYDJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMEOzJO69VQ>? MWqxPFc2PDZ3NB?=
Sf9 NX\HfFV7U2mwYYPlJGF{e2G7 MWCxJIg> NWfrSIlVTE2VTx?= MXnJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGGucHjhJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjh MojINVg4PTR4NUS=
MDA-MB-361 NXrDTVJTTnWwY4Tpc44hSXO|YYm= M2DiOlIhcA>? MlTFSG1UVw>? M1zMeWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvODJ6IN88US=> NFK0eWQyQDd3NE[1OC=>
PC3 NXrFfY5uTnWwY4Tpc44hSXO|YYm= M1i5NFIhcA>? M4iybmROW09? MUTJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCSQ{OgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODN5IN88US=> M4PIclE5PzV2NkW0
U87MG NVTTO2l6TnWwY4Tpc44hSXO|YYm= MUmyJIg> MUnEUXNQ NHPHSY1KdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFnDOVAhd2ZiMD6wOFYh|ryP M1HxO|E5PzV2NkW0
MDA-MB-361 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLYUXBkQTZiaB?= MWXEUXNQ MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlczKM7:TR?= MlLINVg4PTR4NUS=
A2780 NWTEcpNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVG5OkBp NXv5XZlFTE2VTx?= NUPl[WZ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= NICzNnkyQDd3NE[1OC=>
PC3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:5OkBp MYTEUXNQ MVHJR|UxRTBwMkig{txO MV6xPFc2PDZ3NB?=
U87MG NEWwXnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rsUlk3KGh? NYf3WHp[TE2VTx?= NI[zWXVKSzVyPUCuPVUh|ryP M13kblE5PzV2NkW0
Sf9 NYDM[pBJU2mwYYPlJGF{e2G7 MXezNEBucW5? MYHEUXNQ M1WyTGlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDhcY92dnRib3[gRXRRKGOxboP1cYVlKHerdHigTWM2OCCxZjCwMlA1OiEQvF2= M3XKdFIzPTR6M{Sy
RAW 264.7 NYfUbXNjU2mwYYPlJGF{e2G7 M2PJSFkxKG2rbh?= NILMSnFFVVOR NIW2SXNKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> NWHzN49ROjJ3NEizOFI>
Sf9 M2S5SWtqdmG|ZTDBd5NigQ>? M{fXe|EhcA>? MljLTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4JmfGFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOIOTDj[YxteyC5aYToJGlEPTBib3[gNE4xOTdizszN MYGyN|U1ODZ2NR?=
Sf9 NH;6T3JMcW6jc3WgRZN{[Xl? NWH5[HpWOSCq NX\rXYtKUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> MWOyN|U1ODZ2NR?=
Sf9 M17sXmtqdmG|ZTDBd5NigQ>? NUjTdVdROSCq M3PHe2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= NH;kUHYzOzV2ME[0OS=>
Sf9 NW\sNnRNU2mwYYPlJGF{e2G7 MmXUNUBp NUW3U4w3UW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2GucHjhJIV5eHKnc4Pl[C=> M3XPT|I{PTRyNkS1
SKOV3 M13DTWtqdmG|ZTDBd5NigQ>? MUSxJO69VQ>? MV:xJIg> NGrMfYVFVVOR Mn\rTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? MoDsNlM{PjB|NEi=
MCF7 NX3EU4hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L4clEh|ryP MoPnPVYhcA>? Mmf3SG1UVw>? NXfTfFM1T0l3ME2wMlA4ODJizszN M2DFXlI{OzZyM{S4
SKOV3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{S4blEh|ryP M13O[lk3KGh? NX7VWHJGTE2VTx?= NVHB[pRrT0l3ME2wMlE1PzZizszN NV3mUZdIOjN|NkCzOFg>
PC3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHSO|IhcA>? MX\EUXNQ NFfF[GRKSzVyPUCuNlgh|ryP MVyyNVk5OTdzNB?=
MCF7.1 M1fHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfOR2d2PzJiaB?= MYXEUXNQ MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? NV3rOVlzOjF7OEG3NVQ>
MCF7-neo/Her2 NXjVZmVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTKO|IhcA>? MVjEUXNQ M{DWXWlEPTB;MD6yPUDPxE1? MYeyN|Y3OjlyMx?=
MCF7-neo/Her2 MknQT4lv[XOnIFHzd4F6 NUfVclNkUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO NWL2SpRWOjN4NkK5NFM>
PC3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PRblczKGh? NUS3emhRTE2VTx?= NYnGO|YyTUN3ME2wMlM1KM7:TR?= M{Die|IyQTh3NkO5
MCF7.1 M4\HSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm5WIh4PzJiaB?= MmTUSG1UVw>? MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCHQ{WwJI9nKDBwM{mg{txO MnL1NlE6QDV4M{m=
PC3 NEL0OmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL3O|IhcA>? NYCyXnBKTE2VTx?= NWHud2JiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOg[IVncWOrZX70JIlvKFCWRV6ge4l1cCCLQ{WwJI9nKDBwM{mg{txO NUjIWIZsOjByNUC2Olk>
MCF7.1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TXd|czKGh? M3PKOmROW09? NWPRb4NxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigTWM2OCCxZjCwMlM1KM7:TR?= NVm4[HlZOjByNUC2Olk>
MCF7.1 Mli5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PvcFczKGh? M13XNWVEPTB;MD63NkDPxE1? MnPzNlA{PDZ4NU[=
NCI-H1975 M2rtb2N6fG:2b4jpZ{BCe3OjeR?= NUXLWYVoPzJiaB?= NH;M[mZKSzVyPUCuNlch|ryP M3fWVlI{ODV7NUS1
H460 NGfiWlNEgXSxdH;4bYMhSXO|YYm= NVTlWXZ7PzJiaB?= MWrJR|UxRTBwOEeg{txO NX7yT5kyOjNyNUm1OFU>
HT-29 MkT0R5l1d3SxeHnjJGF{e2G7 NIHHbpg4OiCq MVzJR|UxRTBwNk[g{txO NX36cpBmOjNyNUm1OFU>
HepG2 NI\4VHJEgXSxdH;4bYMhSXO|YYm= NEDp[XY4OiCq MV\JR|UxRTFizszN MkTzNlMxPTl3NEW=
SGC7901 Mo\WR5l1d3SxeHnjJGF{e2G7 MY[3NkBp MkP4TWM2OD1zLkig{txO MVGyN|A2QTV2NR?=
NCI-H226 M2H4WmN6fG:2b4jpZ{BCe3OjeR?= MnXMO|IhcA>? NGHyXlhKSzVyPUKuPUDPxE1? MVmyN|A2QTV2NR?=
A549 NWHLd5hpS3m2b4TvfIlkKEG|c3H5 NVfZO4VpPzJiaB?= MoX4TWM2OD14Lkmg{txO M2PmeFI{ODV7NUS1
U87MG M{DoN2N6fG:2b4jpZ{BCe3OjeR?= NVTmTIszPzJiaB?= Mnf6TWM2OD15Lke3JO69VQ>? NH3sSGszOzB3OUW0OS=>
HBC4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXsc4dIUTVyPT22MlA{KE1? NIjGT2ozOjN|NkK0Oi=>
BSY1 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljlcI9oT0l3ME2tOk46OCCP NFjYbIkzOjN|NkK0Oi=>
HBC5 M2fiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHsc4dIUTVyPT22MlYxKE1? M3XjcFIzOzN4MkS2
MCF7 NGPXfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nhOoxw\0eLNUC9MVcvOzNiTR?= M3nYOlIzOzN4MkS2
MDA-MB-231 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzYbpdtd2eJSUWwQU02NjR4IF2= M3;Gb|IzOzN4MkS2
U251 M1e3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LjNIxw\0eLNUC9MVUvPTBiTR?= MlzHNlI{OzZ{NE[=
SF268 NFrHcIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ToV4xw\0eLNUC9MVUvOzliTR?= Mn3BNlI{OzZ{NE[=
SF295 M{nXVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljvcI9oT0l3ME2tOk4{PyCP M4TOUlIzOzN4MkS2
SF539 NYj5ZXpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL3dWJtd2eJSUWwQU03NjVyIF2= MoO1NlI{OzZ{NE[=
SNB75 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXsc4dIUTVyPT23MlExKE1? NWHBV4M4OjJ|M{[yOFY>
SNB78 NEfCeHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HINoxw\0eLNUC9MVYvPTJiTR?= NV\vXY5LOjJ|M{[yOFY>
HCC2998 NUi5d2F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HNbIxw\0eLNUC9MVYvOjliTR?= NF3ySZAzOjN|NkK0Oi=>
KM12 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDqTINtd2eJSUWwQU02Njd4IF2= MXqyNlM{PjJ2Nh?=
HT-29 M2DMV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLxcI9oT0l3ME2tOk4{OCCP NGLaNoUzOjN|NkK0Oi=>
HCT15 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\0bWJsdG:pR1m1NF0uPi5zMjDN MnrENlI{OzZ{NE[=
HCT116 NIWzXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\sc4dIUTVyPT21Mlg4KE1? NWj4XXRbOjJ|M{[yOFY>
NCI-H23 M2XFZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnsc4dIUTVyPT21Mlc{KE1? MkewNlI{OzZ{NE[=
NCI-H226 MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPBcI9oT0l3ME2tOk4zOSCP NEf1b|IzOjN|NkK0Oi=>
NCI-H522 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zQPYxw\0eLNUC9MVYvPThiTR?= MorUNlI{OzZ{NE[=
NCI-H483 M{T0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LtZ4xw\0eLNUC9MVYvPTZiTR?= MnLCNlI{OzZ{NE[=
A549 MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PWOYxw\0eLNUC9MVYvOTViTR?= MX:yNlM{PjJ2Nh?=
DMS273 M1vNPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLFcI9oT0l3ME2tOk41OyCP MV[yNlM{PjJ2Nh?=
DMS114 M2m4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXUcI9oT0l3ME2tOU46OiCP MWKyNlM{PjJ2Nh?=
LOXIMVI M3Gwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLQcI9oT0l3ME2tOk4zQSCP NHjQfIgzOjN|NkK0Oi=>
OVCAR3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;YcI9oT0l3ME2tOk44OSCP M37EV|IzOzN4MkS2
OVCAR4 NFSwT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnwV2k3dG:pR1m1NF0uPS55NjDN MX6yNlM{PjJ2Nh?=
OVCAR5 M3;IU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrYW3h3dG:pR1m1NF0uPi5{NjDN NXi1TIxKOjJ|M{[yOFY>
OVCAR8 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnYcI9oT0l3ME2tOU44OyCP NEDtR3ozOjN|NkK0Oi=>
SKOV3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrsc4dIUTVyPT22MlUzKE1? NYXEWpVWOjJ|M{[yOFY>
RXF631L NIr0enBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzqcI9oT0l3ME2tOk45QCCP MV2yNlM{PjJ2Nh?=
ACHN Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrCcI9oT0l3ME2tOk4xPyCP MmXWNlI{OzZ{NE[=
St-4 NIXoV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITl[3dtd2eJSUWwQU02NjV4IF2= NV;QTWl2OjJ|M{[yOFY>
MKN1 M1nGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLycpdtd2eJSUWwQU04NjB6IF2= NFTWdZMzOjN|NkK0Oi=>
MKN7 NEXUbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3LcI9oT0l3ME2tOk42OCCP M3WzbVIzOzN4MkS2
MKN28 MnLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{KwbYxw\0eLNUC9MVUvPTJiTR?= MYSyNlM{PjJ2Nh?=
MKN45 M2LX[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPsc4dIUTVyPT22MlU2KE1? MkPUNlI{OzZ{NE[=
MKN74 NWOzU4hbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;hWYM4dG:pR1m1NF0uPi5yMjDN MWSyNlM{PjJ2Nh?=
DU145 NXL2TFgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP3bIVtd2eJSUWwQU02Njh3IF2= NIjmRVEzOjN|NkK0Oi=>
PC3 M3LjXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljIcI9oT0l3ME2tOk43PiCP M{fvWFIzOzN4MkS2
ES5 NVXUZ|dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr6TWM2OD13MD6yNUBvVQ>? NFPSeYZUSU6JRWK=
HH MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFzMT6wPEBvVQ>? NV3UcpVDW0GQR1XS
MHH-PREB-1 NUTYXYlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XRXmlEPTB;MUG0MlMhdk1? M33pc3NCVkeHUh?=
NCI-H1770 M{Tpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjIZmlKSzVyPUGyN{45PiCwTR?= MYLTRW5ITVJ?
HuO9 NWrSOnl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLRUXdNUUN3ME2yNFYvODJibl2= M{fpcnNCVkeHUh?=
HAL-01 M{\rdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLlTWM2OD1{ME[uO|Mhdk1? M2SxO3NCVkeHUh?=
NOS-1 NF;jfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHITWM2OD1{MUGuPFIhdk1? NEHIWHZUSU6JRWK=
HGC-27 NVnXeJFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HZZmlEPTB;MkGyMlU4KG6P NFHYSpNUSU6JRWK=
NB69 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ2NT6yO{BvVQ>? MmXIV2FPT0WU
RS4-11 NUXqOppLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\iT2lEPTB;Mk[xMlc3KG6P NEe2RZRUSU6JRWK=
DOK NGDTcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HDN2lEPTB;M{CxMlchdk1? MkXnV2FPT0WU
LB2241-RCC M3vTNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTNyMz64OEBvVQ>? MYTTRW5ITVJ?
NCI-H1623 NVHLXVIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGq0SINKSzVyPUOwOE4xQCCwTR?= MmrBV2FPT0WU
YH-13 MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqwTWM2OD1|MESuN|Ihdk1? MWLTRW5ITVJ?
BPH-1 NXq0[XQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELTNndKSzVyPUOxOEBvVQ>? NYDONXREW0GQR1XS
AN3-CA MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN2MD6zO{BvVQ>? MkHRV2FPT0WU
ES7 M1fhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;4NohvUUN3ME2zOFEvQTlibl2= MonKV2FPT0WU
MDA-MB-175-VII MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;rV5E4UUN3ME2zOVIvQTJibl2= MXzTRW5ITVJ?
GAMG MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v0emlEPTB;M{ewMlg2KG6P NE\3OndUSU6JRWK=
CHL-1 NXvK[|VjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPpPZc5UUN3ME2zO|gvPjVibl2= MUfTRW5ITVJ?
NB7 NUHxPXBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1[0dmlEPTB;M{i5Mlg{KG6P NIDa[mJUSU6JRWK=
MFE-280 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLLS2NsUUN3ME20NVgvOiCwTR?= M1:wWXNCVkeHUh?=
HL-60 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfpTWM2OD12MkWuO|Uhdk1? NHXKbGdUSU6JRWK=
GCIY MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTR|Mz64JI5O NEP6TXNUSU6JRWK=
MDA-MB-361 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR|OT6xN{BvVQ>? MmPkV2FPT0WU
LXF-289 NI\RenNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTLTW5GUUN3ME20OFgvOjdibl2= MV7TRW5ITVJ?
NBsusSR NIXidotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTR6OD64OUBvVQ>? M{D0VXNCVkeHUh?=
KU-19-19 NG\ieWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrofpRKSzVyPUWxOk4xPyCwTR?= MljKV2FPT0WU
A204 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;aelRKSzVyPUWyNk4{OyCwTR?= M2X3XXNCVkeHUh?=
LB1047-RCC MoHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjOcZVvUUN3ME21NlIvQTNibl2= NIDLXGhUSU6JRWK=
COLO-684 M1LvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\wTWM2OD13MkOuNVEhdk1? MmfhV2FPT0WU
PA-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzFbVFKSzVyPUWzNk41OSCwTR?= MUPTRW5ITVJ?
MG-63 M13mSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFz2VIZKSzVyPUW0NU4yOSCwTR?= NIroeXhUSU6JRWK=
BHT-101 M{fFZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7X[mczUUN3ME21OFQvQTRibl2= MoqyV2FPT0WU
NKM-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTV7Mz6wPUBvVQ>? MknTV2FPT0WU
T47D M2OyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTV7Nz61OkBvVQ>? Mm\0V2FPT0WU
MOLT-4 NHW0[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf1ZVJKSzVyPU[yN{43OiCwTR?= NETleVlUSU6JRWK=
IGROV-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkj0TWM2OD14M{SuN|Ehdk1? Ml2xV2FPT0WU
ES4 NYfKfndZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXwNIpKSzVyPU[zPU42PCCwTR?= MkPFV2FPT0WU
HuO-3N1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTZ2Mj6zPEBvVQ>? NIPTb3FUSU6JRWK=
NEC8 NEH6VJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTZWpBoUUN3ME22OVMvPTdibl2= NY\mU5V3W0GQR1XS
HO-1-N-1 NEHWc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvNTWM2OD14NUmuNVchdk1? Ml7tV2FPT0WU
EPCL-272H M1vGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[zPYlFUUN3ME22PFcvOjFibl2= NFToZpBUSU6JRWK=
D-263MG NFXBXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Dh[GlEPTB;N{G4MlEhdk1? MWDTRW5ITVJ?
MV-4-11 NH;Cd|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnk[Hk2UUN3ME23NlQvOzFibl2= NGniT5RUSU6JRWK=
SK-NEP-1 M2rISWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe5XHpKSzVyPUeyOU46PCCwTR?= Mmj0V2FPT0WU
SW872 NVm3[opwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTd{Nz64PUBvVQ>? MYXTRW5ITVJ?
P30-OHK MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH5RnMxUUN3ME23N|AvPzFibl2= MXHTRW5ITVJ?
OMC-1 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\YUlVLUUN3ME23OVEvODlibl2= M1fEPHNCVkeHUh?=
LoVo MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnjT21QUUN3ME23O|cvQSCwTR?= M3K2TnNCVkeHUh?=
LNCaP-Clone-FGC NInId3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK4PXdKSzVyPUe5Ok4{PCCwTR?= NGDDTlhUSU6JRWK=
L-363 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf1NnFKSzVyPUe5PE41OiCwTR?= MWjTRW5ITVJ?
ES8 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnSe5F{UUN3ME24NVAvPTJibl2= MV3TRW5ITVJ?
697 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfrTWM2OD16M{GuOVUhdk1? NV;IdHFIW0GQR1XS
HSC-3 NGOy[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{npNWlEPTB;OEO5MlU1KG6P MnP3V2FPT0WU
H4 M3;W[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXsTW5KSzVyPUi1NE45PSCwTR?= NYrqT3VSW0GQR1XS
QIMR-WIL MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PTemlEPTB;OE[1MlIhdk1? MUHTRW5ITVJ?
OAW-42 M4TBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTh5Mj6xPUBvVQ>? NUDwfo9LW0GQR1XS
MCF7 NVnaNIFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHETWM2OD16OUiuOVkhdk1? MlrmV2FPT0WU
SCC-25 M1nn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTlzND6xPUBvVQ>? MlTGV2FPT0WU
NCI-H1563 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTlzNT65PUBvVQ>? M33BcXNCVkeHUh?=
OVCAR-5 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTl2MD6xO{BvVQ>? MVnTRW5ITVJ?
HDLM-2 M3LHZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC0UmNKSzVyPUm0PU4zKG6P NUj3NZJDW0GQR1XS
NB5 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv2RnlvUUN3ME25OVYvPiCwTR?= MX7TRW5ITVJ?
NCI-H292 MlHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTTTWM2OD17N{SuN|Ihdk1? NYnwe|lKW0GQR1XS
A101D M1fWemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLmTZlZUUN3ME25PVAvOTlibl2= MofHV2FPT0WU
NCI-H1648 MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz0fnpKSzVyPUm5PE42OSCwTR?= M4jkUnNCVkeHUh?=
EKVX NWe3e3liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXMR4pKSzVyPUGuNFEzQSEQvF2= MkS4V2FPT0WU
SW1710 M3j0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTqTWM2OD1zLkC0NlM{KM7:TR?= M3T4fXNCVkeHUh?=
WM-115 MlXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3KTXhKSzVyPUGuNFY3PTZizszN Mmj6V2FPT0WU
CAL-54 M3naTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zrfmlEPTB;MT6wO|A5OSEQvF2= NY\3ZndpW0GQR1XS
TGBC24TKB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInWUphKSzVyPUGuNFgxPDVizszN NVjIXYVbW0GQR1XS
NCI-H520 NEPGOoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnQflk3UUN3ME2xMlA5QTZ5IN88US=> Mnn1V2FPT0WU
D-423MG M1\6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Hj[WlEPTB;MT6wPVk3OiEQvF2= NGGxUZZUSU6JRWK=
BFTC-905 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHMTWM2OD1zLkGzOFQ6KM7:TR?= NYTVfJRbW0GQR1XS
HT MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7TPI9KSzVyPUGuNVM1PzhizszN Mo\IV2FPT0WU
CTB-1 NGXvbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1zLkG0Nlk{KM7:TR?= MUDTRW5ITVJ?
Hs-578-T MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3sU3lkUUN3ME2xMlE6PTZ3IN88US=> MYXTRW5ITVJ?
HuH-7 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTFwMkC5OFkh|ryP MYDTRW5ITVJ?
LB996-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwMkKxO|ch|ryP NHjIUoZUSU6JRWK=
KYSE-270 MofiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC4V5N2UUN3ME2xMlI6PzN2IN88US=> M{fNeHNCVkeHUh?=
A4-Fuk NVTEblJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn76TWM2OD1zLkK5PVk{KM7:TR?= NInGWnhUSU6JRWK=
A498 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zLdWlEPTB;MT6zNFQ4PCEQvF2= MUDTRW5ITVJ?
SK-MEL-1 MmrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlqxTWM2OD1zLkOwOlc6KM7:TR?= NFezU3ZUSU6JRWK=
AU565 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;3bGlEPTB;MT6zNVg3OyEQvF2= MYrTRW5ITVJ?
Saos-2 M{[2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTvZVllUUN3ME2xMlM{OjB3IN88US=> M33WenNCVkeHUh?=
A549 NX3we2IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuwPHJKSzVyPUGuN|k6PyEQvF2= MXvTRW5ITVJ?
BFTC-909 NVznVmZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;FTWM2OD1zLkSzN|A2KM7:TR?= NIj3Rm5USU6JRWK=
MDA-MB-415 NXLjR4YxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTFwNEi2PVIh|ryP M1XGdXNCVkeHUh?=
639-V NUn5fFhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTFwNUCyOFUh|ryP NXXBXmhTW0GQR1XS
A704 NU\mb5lNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\XPWlEPTB;MT61NFc5PSEQvF2= NELkdmlUSU6JRWK=
PANC-03-27 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LnbWlEPTB;MT61NVQxQCEQvF2= NF;ZemxUSU6JRWK=
SK-MEL-28 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon2TWM2OD1zLkW2NFg2KM7:TR?= MkG5V2FPT0WU
Ramos-2G6-4C10 MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwNkC3OFYh|ryP NEjJcmZUSU6JRWK=
HuP-T4 M4XBO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3flNGlEPTB;MT62NFc4QCEQvF2= NUnpOGJjW0GQR1XS
VA-ES-BJ NH2ySY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37kNWlEPTB;MT62NVI4KM7:TR?= NEXYem5USU6JRWK=
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LCLC-103H NF7Kc2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT2XmFOUUN3ME2zOE4yPjJ2IN88US=> NWPSRmZsW0GQR1XS
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KYSE-140 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTRyLkexOlUh|ryP NVXleXF3W0GQR1XS
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COLO-792 Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTR{Lki5OlEh|ryP MmTHV2FPT0WU
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Ca-Ski MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTR2LkixNVQh|ryP NULC[Y1CW0GQR1XS
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NCI-H358 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e2Z2lEPTB;NEmuN|AyQCEQvF2= NUXnT2x1W0GQR1XS
LS-411N M3rrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TLN2lEPTB;NEmuN|EyQCEQvF2= MYTTRW5ITVJ?
IST-MES1 M2HJUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13ydmlEPTB;NEmuOVYzPSEQvF2= MWDTRW5ITVJ?

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

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Clinical Trial Information

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

Tech Support

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

Handling Instructions

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID