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 MXrLbY5ie2ViQYPzZZk> M{P1N|EhcA>? NHPD[I9FVVOR MX7Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGSnbIThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? MWGxPFc2PDZ3NB?=
Sf9 M13LXmtqdmG|ZTDBd5NigQ>? NHy4Tm8yKGh? M1:1WGROW09? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgTFExPDdvUjDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> MmjBNVg4PTR4NUS=
Sf9 M3XBeWtqdmG|ZTDBd5NigQ>? NVLPSlFqOSCq M3XzNGROW09? MoDGTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NXHZd3BnOTh5NUS2OVQ>
Sf9 MnHDT4lv[XOnIFHzd4F6 M3zTNlEhcA>? MYDEUXNQ MXTJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMEOzJO69VQ>? MVOxPFc2PDZ3NB?=
Sf9 NIfOUodMcW6jc3WgRZN{[Xl? NGDDUpIyKGh? NXnFOIFqTE2VTx?= M{jTdGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> NFP0[YoyQDd3NE[1OC=>
MDA-MB-361 NFu2ZoxHfW6ldHnvckBCe3OjeR?= NIjReIgzKGh? M{H6cGROW09? NVr5RlBLUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO MYSxPFc2PDZ3NB?=
PC3 NEnzcppHfW6ldHnvckBCe3OjeR?= NEnpWo0zKGh? NEThN|JFVVOR MoeyTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kAxNjB|NzFOwG0> MnjtNVg4PTR4NUS=
U87MG M4nPTWZ2dmO2aX;uJGF{e2G7 M3nlOlIhcA>? NF:2T5lFVVOR NGmzUpRKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFnDOVAhd2ZiMD6wOFYh|ryP MWKxPFc2PDZ3NB?=
MDA-MB-361 M{SxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS5OkBp M1PPNmROW09? M3TSfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvPzJizszN MmTzNVg4PTR4NUS=
A2780 MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\XPXA6PiCq NX;GcHNoTE2VTx?= MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IIfpeIghWEmNM1PBJIFv\CCSVFXOJI12fGG2aX;uJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? NYr6XFN[OTh5NUS2OVQ>
PC3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPuPVYhcA>? NET2T2ZFVVOR M13Fe2lEPTB;MD6yPEDPxE1? Ml\1NVg4PTR4NUS=
U87MG MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi5OkBp NVPKdnViTE2VTx?= MlGyTWM2OD1yLkm1JO69VQ>? MWqxPFc2PDZ3NB?=
Sf9 NILubJlMcW6jc3WgRZN{[Xl? NIHsSlM{OCCvaX6= M2O0SWROW09? NE\hUJRKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgZY1wfW62IH;mJGFVWCClb37zeY1m\CC5aYToJGlEPTBib3[gNE4xPDJizszN MUeyNlU1QDN2Mh?=
RAW 264.7 NXzSRXNUU2mwYYPlJGF{e2G7 NFnOZpo6OCCvaX6= NH\Ie3ZFVVOR NF32RW1KdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> M3faN|IzPTR6M{Sy
Sf9 MUjLbY5ie2ViQYPzZZk> MWKxJIg> M3P2RWlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tj\XSjIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVRkmgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODF5IN88US=> MlrSNlM2PDB4NEW=
Sf9 MkjUT4lv[XOnIFHzd4F6 M{LFWlEhcA>? NWH1eZhJUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> M3;1N|I{PTRyNkS1
Sf9 NVn4c2pFU2mwYYPlJGF{e2G7 NGTGdGwyKGh? MYXJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[4FudWFiZYjwdoV{e2Wm M4PDSVI{PTRyNkS1
Sf9 MmPHT4lv[XOnIFHzd4F6 MkXBNUBp MWjJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm MUKyN|U1ODZ2NR?=
SKOV3 NFjzNVVMcW6jc3WgRZN{[Xl? NXnmbYNSOSEQvF2= NFPSUHAyKGh? M33z[WROW09? MnG2TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? MWKyN|M3ODN2OB?=
MCF7 Mm\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\USI9COSEQvF2= M3XVbFk3KGh? M{DLNmROW09? MmPjS2k2OD1yLkC3NFIh|ryP NHe4dHEzOzN4MEO0PC=>
SKOV3 NWjWbHIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmm3NUDPxE1? NWTYV3hiQTZiaB?= MXTEUXNQ MWjHTVUxRTBwMUS3OkDPxE1? NF7CNogzOzN4MEO0PC=>
PC3 NHzINJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHpT|ZNPzJiaB?= M1e3bmROW09? MmraTWM2OD1yLkK4JO69VQ>? MWqyNVk5OTdzNB?=
MCF7.1 M2e4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:xNVB3PzJiaB?= Ml3PSG1UVw>? MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? M13J[lIyQThzN{G0
MCF7-neo/Her2 NXvWZ4FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnOdIRQPzJiaB?= NVzjNnFMTE2VTx?= NHPEe5hKSzVyPUCuNlkh|ryP M3fPNlI{PjZ{OUCz
MCF7-neo/Her2 M1TTZWtqdmG|ZTDBd5NigQ>? MlPlTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC5aYToJGlEPTBib3[gNE4xODdizszN MYGyN|Y3OjlyMx?=
PC3 M{G2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\wc3FUPzJiaB?= MUXEUXNQ MU\FR|UxRTBwM{Sg{txO NY\qUYVZOjF7OEW2N|k>
MCF7.1 M2TFTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17TRlczKGh? MoLaSG1UVw>? NGLp[FZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDFR|UxKG:oIECuN|kh|ryP M2PvT|IyQTh3NkO5
PC3 NVXZcphPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO3NkBp M3fhO2ROW09? NWjiT5p[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOg[IVncWOrZX70JIlvKFCWRV6ge4l1cCCLQ{WwJI9nKDBwM{mg{txO NXzORZV7OjByNUC2Olk>
MCF7.1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXxWoQ5PzJiaB?= MlSwSG1UVw>? MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCLQ{WwJI9nKDBwM{Sg{txO MYSyNFA2ODZ4OR?=
MCF7.1 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP0O|IhcA>? MoTkSWM2OD1yLkeyJO69VQ>? M3;CTVIxOzR4NkW2
NCI-H1975 MkP6R5l1d3SxeHnjJGF{e2G7 MonlO|IhcA>? NYDseYZ5UUN3ME2wMlI4KM7:TR?= NILhUYMzOzB3OUW0OS=>
H460 Ml7iR5l1d3SxeHnjJGF{e2G7 MlPQO|IhcA>? NH:2SZpKSzVyPUCuPFch|ryP M2DFXFI{ODV7NUS1
HT-29 M1PINGN6fG:2b4jpZ{BCe3OjeR?= NGnTRno4OiCq MWTJR|UxRTBwNk[g{txO MXWyN|A2QTV2NR?=
HepG2 NEizVZpEgXSxdH;4bYMhSXO|YYm= NWLyc|MzPzJiaB?= NUTQfIwyUUN3ME2xJO69VQ>? MoraNlMxPTl3NEW=
SGC7901 NXWxcpVtS3m2b4TvfIlkKEG|c3H5 NYjGblhnPzJiaB?= MVXJR|UxRTFwODFOwG0> NXrme4x1OjNyNUm1OFU>
NCI-H226 M{XZW2N6fG:2b4jpZ{BCe3OjeR?= MleyO|IhcA>? M4fBUmlEPTB;Mj65JO69VQ>? M4GzWVI{ODV7NUS1
A549 MXrDfZRwfG:6aXOgRZN{[Xl? MXe3NkBp NHHCc21KSzVyPU[uPUDPxE1? NVHQfmJYOjNyNUm1OFU>
U87MG MnXQR5l1d3SxeHnjJGF{e2G7 NHG5THQ4OiCq M2S2OGlEPTB;Nz63O{DPxE1? NVTSW4VROjNyNUm1OFU>
HBC4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDsc4dIUTVyPT22MlA{KE1? MoC4NlI{OzZ{NE[=
BSY1 M3jaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTsc4dIUTVyPT22MlkxKE1? MorHNlI{OzZ{NE[=
HBC5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[3dWVtd2eJSUWwQU03NjZyIF2= MVGyNlM{PjJ2Nh?=
MCF7 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDHcI9oT0l3ME2tO{4{OyCP MlHlNlI{OzZ{NE[=
MDA-MB-231 M{fmNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXlcI9oT0l3ME2tOU41PiCP M3LxfVIzOzN4MkS2
U251 NUnwOFhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTsc4dIUTVyPT21MlUxKE1? MYeyNlM{PjJ2Nh?=
SF268 NXe4RXdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzY[HQzdG:pR1m1NF0uPS5|OTDN MXWyNlM{PjJ2Nh?=
SF295 NGO4cJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmz[4Vtd2eJSUWwQU03NjN5IF2= NXfBeIVMOjJ|M{[yOFY>
SF539 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jDdIxw\0eLNUC9MVYvPTBiTR?= M1zifVIzOzN4MkS2
SNB75 NGj1[5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GzfIxw\0eLNUC9MVcvOTBiTR?= NX2zOIRZOjJ|M{[yOFY>
SNB78 M4rBdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXGwT5NOdG:pR1m1NF0uPi53MjDN MnT4NlI{OzZ{NE[=
HCC2998 MmW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInTWnptd2eJSUWwQU03NjJ7IF2= NX\zU5VXOjJ|M{[yOFY>
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HCT15 NH;IZ4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonocI9oT0l3ME2tOk4yOiCP M1i5TFIzOzN4MkS2
HCT116 M3jHeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;hcI9oT0l3ME2tOU45PyCP NFnnflEzOjN|NkK0Oi=>
NCI-H23 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojlcI9oT0l3ME2tOU44OyCP M{jGWlIzOzN4MkS2
NCI-H226 NFq3UFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfsc4dIUTVyPT22MlIyKE1? MX[yNlM{PjJ2Nh?=
NCI-H522 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXrS5FCdG:pR1m1NF0uPi53ODDN MUSyNlM{PjJ2Nh?=
NCI-H483 NIPHSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3NcXdtdG:pR1m1NF0uPi53NjDN NIjlNXgzOjN|NkK0Oi=>
A549 M4KxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\BcI9oT0l3ME2tOk4yPSCP M2C1clIzOzN4MkS2
DMS273 M{[ySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHK1dpdtd2eJSUWwQU03NjR|IF2= MWmyNlM{PjJ2Nh?=
DMS114 NWSxRldYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfsc4dIUTVyPT21MlkzKE1? MnvzNlI{OzZ{NE[=
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OVCAR3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnsc4dIUTVyPT22MlcyKE1? MUCyNlM{PjJ2Nh?=
OVCAR4 MmTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\sc4dIUTVyPT21Mlc3KE1? MmjaNlI{OzZ{NE[=
OVCAR5 MlLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnztcI9oT0l3ME2tOk4zPiCP Mn;5NlI{OzZ{NE[=
OVCAR8 NFHtOXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfocI9oT0l3ME2tOU44OyCP MX6yNlM{PjJ2Nh?=
SKOV3 M3Tufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\kcI9oT0l3ME2tOk42OiCP MX[yNlM{PjJ2Nh?=
RXF631L MnO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PLbYxw\0eLNUC9MVYvQDhiTR?= NVT2UHRJOjJ|M{[yOFY>
ACHN NWfPdZJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\tbYxw\0eLNUC9MVYvODdiTR?= MU[yNlM{PjJ2Nh?=
St-4 NHy1RpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSzcoJ4dG:pR1m1NF0uPS53NjDN M1PoelIzOzN4MkS2
MKN1 MmTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\aRldkdG:pR1m1NF0uPy5yODDN MVeyNlM{PjJ2Nh?=
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MKN28 MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor3cI9oT0l3ME2tOU42OiCP MVWyNlM{PjJ2Nh?=
MKN45 M4HUV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPjUnBtd2eJSUWwQU03NjV3IF2= MX2yNlM{PjJ2Nh?=
MKN74 NFrXdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\XcI9oT0l3ME2tOk4xOiCP MX:yNlM{PjJ2Nh?=
DU145 M1fy[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHLfWpqdG:pR1m1NF0uPS56NTDN M3HLPFIzOzN4MkS2
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ES5 NXfLVWU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTVyLkKxJI5O MnXiV2FPT0WU
HH MkC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojXTWM2OD1zMUGuNFghdk1? M2nlSHNCVkeHUh?=
MHH-PREB-1 M1LweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnLbXg3UUN3ME2xNVQvOyCwTR?= MWPTRW5ITVJ?
NCI-H1770 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[4e|JKSzVyPUGyN{45PiCwTR?= NIXRTmJUSU6JRWK=
HuO9 NYf4V2txT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S4emlEPTB;MkC2MlAzKG6P NIiwVXpUSU6JRWK=
HAL-01 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\ldYlLUUN3ME2yNFYvPzNibl2= NHjjWIVUSU6JRWK=
NOS-1 M2eyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHvfW5GUUN3ME2yNVEvQDJibl2= NX7aR4dkW0GQR1XS
HGC-27 NG\FSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDDTWM2OD1{MUKuOVchdk1? MUDTRW5ITVJ?
NB69 MkKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H6R2lEPTB;MkS1MlI4KG6P NUf0dnhOW0GQR1XS
RS4-11 NEPLXpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJ4MT63OkBvVQ>? M2TTeHNCVkeHUh?=
DOK NHjid4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInyN3ZKSzVyPUOwNU44KG6P M4iySnNCVkeHUh?=
LB2241-RCC NH;GVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTNyMz64OEBvVQ>? MWLTRW5ITVJ?
NCI-H1623 NVjrfIlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13rTWlEPTB;M{C0MlA5KG6P M1LscHNCVkeHUh?=
YH-13 MmXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr6TWM2OD1|MESuN|Ihdk1? NXfR[XlEW0GQR1XS
BPH-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jGfmlEPTB;M{G0JI5O NE\3SItUSU6JRWK=
AN3-CA MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN2MD6zO{BvVQ>? NVfQXWRtW0GQR1XS
ES7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uySGlEPTB;M{SxMlk6KG6P M3fKenNCVkeHUh?=
MDA-MB-175-VII MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN3Mj65NkBvVQ>? MVnTRW5ITVJ?
GAMG NGPsVXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnjdHZKSzVyPUO3NE45PSCwTR?= NEXsUYpUSU6JRWK=
CHL-1 NHjFc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN5OD62OUBvVQ>? MmHKV2FPT0WU
NB7 M{HERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLxdJRZUUN3ME2zPFkvQDNibl2= NVq2fHdCW0GQR1XS
MFE-280 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTRzOD6yJI5O MXLTRW5ITVJ?
HL-60 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTR{NT63OUBvVQ>? MXjTRW5ITVJ?
GCIY M2nxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHyeGtKSzVyPUSzN{45KG6P MVrTRW5ITVJ?
MDA-MB-361 MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrUPG9KSzVyPUSzPU4yOyCwTR?= NFLCTIJUSU6JRWK=
LXF-289 M4nXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTR2OD6yO{BvVQ>? M4S2OHNCVkeHUh?=
NBsusSR NVv4b2hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7C[YFEUUN3ME20PFgvQDVibl2= MmLVV2FPT0WU
KU-19-19 MnXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrpTmFoUUN3ME21NVYvODdibl2= MX\TRW5ITVJ?
A204 NVewc|lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M36yZmlEPTB;NUKyMlM{KG6P M4TzR3NCVkeHUh?=
LB1047-RCC NWW0bHFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PDT2lEPTB;NUKyMlk{KG6P M2q5WnNCVkeHUh?=
COLO-684 M3rDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K5NmlEPTB;NUKzMlEyKG6P MoHYV2FPT0WU
PA-1 NFHDeohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTV|Mj60NUBvVQ>? NWDHUopIW0GQR1XS
MG-63 M2fscmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rw[2lEPTB;NUSxMlEyKG6P Mmi2V2FPT0WU
BHT-101 NWLyZnlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTV2ND65OEBvVQ>? M{TEZnNCVkeHUh?=
NKM-1 M{nHT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG4TWM2OD13OUOuNFkhdk1? NIHiSVBUSU6JRWK=
T47D M3zBWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\rTWlEPTB;NUm3MlU3KG6P NUX0O2s1W0GQR1XS
MOLT-4 NXrOOlVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PXbGlEPTB;NkKzMlYzKG6P NWnyUlZ5W0GQR1XS
IGROV-1 NUC5b|lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXXTWM2OD14M{SuN|Ehdk1? NHfCTpNUSU6JRWK=
ES4 NFPLSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7sTWM2OD14M{muOVQhdk1? NInIZ3lUSU6JRWK=
HuO-3N1 NF3FSmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTZ2Mj6zPEBvVQ>? M33XO3NCVkeHUh?=
NEC8 NH;sOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\pfppKSzVyPU[1N{42PyCwTR?= MY\TRW5ITVJ?
HO-1-N-1 M13WTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLjTWM2OD14NUmuNVchdk1? NXnrUWdVW0GQR1XS
EPCL-272H MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXBbJFKSzVyPU[4O{4zOSCwTR?= NEXuNmNUSU6JRWK=
D-263MG M2HjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvhPI9KSzVyPUexPE4yKG6P Ml6xV2FPT0WU
MV-4-11 NIj1WXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTd{ND6zNUBvVQ>? MlXMV2FPT0WU
SK-NEP-1 NUXYV2ozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTd{NT65OEBvVQ>? NHG3SJFUSU6JRWK=
SW872 NEjxNohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX35cFBUUUN3ME23NlcvQDlibl2= M{L5SnNCVkeHUh?=
P30-OHK MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOwR|c2UUN3ME23N|AvPzFibl2= NXrISWlYW0GQR1XS
OMC-1 NEfGVmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK1TWM2OD15NUGuNFkhdk1? NIjOfXVUSU6JRWK=
LoVo Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVyySYZ5UUN3ME23O|cvQSCwTR?= NHnaZnlUSU6JRWK=
LNCaP-Clone-FGC NV\COmJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTd7Nj6zOEBvVQ>? MlTuV2FPT0WU
L-363 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTd7OD60NkBvVQ>? MlW3V2FPT0WU
ES8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonJTWM2OD16MUCuOVIhdk1? MVnTRW5ITVJ?
697 M2npUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\mTWM2OD16M{GuOVUhdk1? NILJTYNUSU6JRWK=
HSC-3 NFLTPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi0RWNpUUN3ME24N|kvPTRibl2= M{XyeXNCVkeHUh?=
H4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nNV2lEPTB;OEWwMlg2KG6P NIP3Z21USU6JRWK=
QIMR-WIL NWDoSoU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHhSXdUUUN3ME24OlUvOiCwTR?= MULTRW5ITVJ?
OAW-42 NFHHdlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGe3VFZKSzVyPUi3Nk4yQSCwTR?= NHPRNoVUSU6JRWK=
MCF7 NXjOO4hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfye5FqUUN3ME24PVgvPTlibl2= M1e5THNCVkeHUh?=
SCC-25 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoiyTWM2OD17MUSuNVkhdk1? M2X2NHNCVkeHUh?=
NCI-H1563 NXiwUVVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jQcGlEPTB;OUG1Mlk6KG6P NEf5TFlUSU6JRWK=
OVCAR-5 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTxTWM2OD17NECuNVchdk1? MX;TRW5ITVJ?
HDLM-2 M3\CTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1T1SmlEPTB;OUS5MlIhdk1? NFvTRnNUSU6JRWK=
NB5 M3rob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nTZ2lEPTB;OUW2MlYhdk1? NGnDSWJUSU6JRWK=
NCI-H292 NGrocphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnmTWM2OD17N{SuN|Ihdk1? NUX3eYx6W0GQR1XS
A101D NUnHXVhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrDO3lvUUN3ME25PVAvOTlibl2= MVPTRW5ITVJ?
NCI-H1648 MmPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTl7OD61NUBvVQ>? MWLTRW5ITVJ?
EKVX M1LnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLjN3ZxUUN3ME2xMlAyOjlizszN MXjTRW5ITVJ?
SW1710 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LxV2lEPTB;MT6wOFI{OyEQvF2= NVzGXWNxW0GQR1XS
WM-115 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILpOGdKSzVyPUGuNFY3PTZizszN NIr5O2dUSU6JRWK=
CAL-54 NVHxXlViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jofWlEPTB;MT6wO|A5OSEQvF2= M{G2U3NCVkeHUh?=
TGBC24TKB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm4TWM2OD1zLkC4NFQ2KM7:TR?= MYnTRW5ITVJ?
NCI-H520 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTFwMEi5Olch|ryP MV7TRW5ITVJ?
D-423MG NGOwVIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zIN2lEPTB;MT6wPVk3OiEQvF2= MX7TRW5ITVJ?
BFTC-905 NXS5TY5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfyb5ZKSzVyPUGuNVM1PDlizszN NH;udpRUSU6JRWK=
HT NX3JWIFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUToc4dkUUN3ME2xMlE{PDd6IN88US=> M1zCN3NCVkeHUh?=
CTB-1 NHXHNldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnlc21[UUN3ME2xMlE1Ojl|IN88US=> NIjNXmxUSU6JRWK=
Hs-578-T NIHBTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LrNWlEPTB;MT6xPVU3PSEQvF2= M4nrZXNCVkeHUh?=
HuH-7 NEjhPZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\PO2lEPTB;MT6yNFk1QSEQvF2= MU\TRW5ITVJ?
LB996-RCC MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXCOVdKSzVyPUGuNlIyPzdizszN M{C5VXNCVkeHUh?=
KYSE-270 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPhTZFKSzVyPUGuNlk4OzRizszN MXzTRW5ITVJ?
A4-Fuk MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX6OogzUUN3ME2xMlI6QTl|IN88US=> MkC2V2FPT0WU
A498 NFf6bGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK0TWM2OD1zLkOwOFc1KM7:TR?= MVzTRW5ITVJ?
SK-MEL-1 NGj5R4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvXO4lKSzVyPUGuN|A3PzlizszN MXPTRW5ITVJ?
AU565 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLURZZHUUN3ME2xMlMyQDZ|IN88US=> MW\TRW5ITVJ?
Saos-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkixTWM2OD1zLkOzNlA2KM7:TR?= M2PPSnNCVkeHUh?=
A549 NV;oTHVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq5OVZ1UUN3ME2xMlM6QTdizszN MYfTRW5ITVJ?
BFTC-909 NYXNPGpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXviNWl4UUN3ME2xMlQ{OzB3IN88US=> M3HBb3NCVkeHUh?=
MDA-MB-415 NVTadVVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFwNEi2PVIh|ryP NYWxe4RmW0GQR1XS
639-V M{j0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD1WmpsUUN3ME2xMlUxOjR3IN88US=> MlHVV2FPT0WU
A704 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDTWWlKSzVyPUGuOVA4QDVizszN NWHt[HhuW0GQR1XS
PANC-03-27 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHMTWM2OD1zLkWxOFA5KM7:TR?= M1iyWHNCVkeHUh?=
SK-MEL-28 M2HzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7wTWM2OD1zLkW2NFg2KM7:TR?= MXnTRW5ITVJ?
Ramos-2G6-4C10 MmTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX3N5NKSzVyPUGuOlA4PDZizszN NX33fZJSW0GQR1XS
HuP-T4 MmfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TKfmlEPTB;MT62NFc4QCEQvF2= MXvTRW5ITVJ?
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RKO NF;wcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q2bWlEPTB;Mk[uO|Y{OiEQvF2= NUTNc2tmW0GQR1XS
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NCI-H2452 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fYdGlEPTB;MkeuO|cyPiEQvF2= M1nDSnNCVkeHUh?=
NCI-H1395 NF3TUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\Ke2lEPTB;MkeuO|g{OyEQvF2= MYPTRW5ITVJ?
KYSE-450 NHjSO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\YN4tKSzVyPUK3Mlk5PjJizszN NIThPXVUSU6JRWK=
S-117 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2W4NWlEPTB;MkmuN|g2PyEQvF2= NYjQe2c2W0GQR1XS
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ES3 NYXocHlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7UNZFKSzVyPUOwMlM4OzNizszN MVvTRW5ITVJ?
HCT-116 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLMRYRKSzVyPUOwMlU2PTRizszN MVjTRW5ITVJ?
NCI-H1693 NWH0emFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNyLkW5OFIh|ryP NXjzUI9xW0GQR1XS
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NCI-H2170 M33URmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DLZ2lEPTB;M{GuOVc5PCEQvF2= NV\yRWhsW0GQR1XS
ALL-PO Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq5TWM2OD1|MT64OFI5KM7:TR?= NWLabZJlW0GQR1XS
NCI-H661 NVP5N2ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LZ[2lEPTB;M{KuNFYzOyEQvF2= NVGwS2F5W0GQR1XS
NCI-H2347 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\PUpJKSzVyPUOyMlQ5OzdizszN NEn1bFRUSU6JRWK=
FTC-133 MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTN{LkewOkDPxE1? M4rzU3NCVkeHUh?=
COLO-829 NV7TeJBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzNTWM2OD1|Mz6zOFY4KM7:TR?= NV;BOlN7W0GQR1XS
GOTO MnzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoixTWM2OD1|Mz61NlU5KM7:TR?= MWjTRW5ITVJ?
YAPC M{DTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjoTWM2OD1|Mz64NVU6KM7:TR?= NGL1[oNUSU6JRWK=
LCLC-103H NYDUSGNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjWPXlKSzVyPUO0MlE3OjRizszN MV7TRW5ITVJ?
SiHa MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLhN3M2UUN3ME2zOE4{QDF5IN88US=> NU[1Z41KW0GQR1XS
LK-2 NVXmWZZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DrWGlEPTB;M{SuOVcxQCEQvF2= MnPLV2FPT0WU
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NCI-SNU-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTN3LkG3PUDPxE1? MULTRW5ITVJ?
KNS-81-FD M13zO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XYUmlEPTB;M{WuOlY{KM7:TR?= NXrzfFNQW0GQR1XS
SCC-9 NH[yN2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTUTWM2OD1|Nj63NVQ3KM7:TR?= M4fjVnNCVkeHUh?=
SH-4 NEL4dmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzrd5FKSzVyPUO2Mlc{KM7:TR?= NUPRVIJOW0GQR1XS
HCC-1954 NV\JOIVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7MepJKSzVyPUO3MlI4OjlizszN NGC4PVRUSU6JRWK=
BALL-1 NVzGNmw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjDXGlFUUN3ME2zO{42OzF4IN88US=> M{jBOnNCVkeHUh?=
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COLO-678 NXzjOnBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTBTWM2OD1|Nz65OFM4KM7:TR?= MWnTRW5ITVJ?
SK-MEL-3 M3i4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3iZ2R6UUN3ME2zPE4zOzl5IN88US=> NIXHfnpUSU6JRWK=
OAW-28 NUPDUZljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHJNZNKSzVyPUO4MlY{QSEQvF2= NI\LWllUSU6JRWK=
CAMA-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjHTWM2OD1|OD65OlkyKM7:TR?= MV\TRW5ITVJ?
C2BBe1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:zVHpKSzVyPUO5MlgyQCEQvF2= MoLOV2FPT0WU
A3-KAW NXrzd5lOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTRyLkO2OlEh|ryP MmHNV2FPT0WU
SK-MEL-24 M1H3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17ydWlEPTB;NECuOVk{OSEQvF2= MlHqV2FPT0WU
KYSE-140 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\RXIZOUUN3ME20NE44OTZ3IN88US=> M4LkUHNCVkeHUh?=
MOLT-16 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPDTWM2OD12MT6xOVM3KM7:TR?= NVnidGRTW0GQR1XS
CFPAC-1 NYriNG9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC3TWM2OD12Mj61NlEyKM7:TR?= M1PhfnNCVkeHUh?=
NB14 NH3FO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR{LkewNlch|ryP M4fFVXNCVkeHUh?=
COLO-792 NF\tUVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjRTWM2OD12Mj64PVYyKM7:TR?= MoXRV2FPT0WU
RH-1 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW5TWM2OD12Mz60PFM3KM7:TR?= MVfTRW5ITVJ?
NCI-H522 NFT4TnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe3S4ZKSzVyPUS0MlM2PjhizszN MVPTRW5ITVJ?
Ca-Ski M1rNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[5Z2lEPTB;NESuPFEyPCEQvF2= NIXLRVFUSU6JRWK=
KGN NIm2SnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17FOWlEPTB;NEiuN|A3OyEQvF2= NHHvW3FUSU6JRWK=
UACC-62 M3H3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTR6LkSwO|Ih|ryP NWT2U3dSW0GQR1XS
NCI-H358 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDJWnhZUUN3ME20PU4{ODF6IN88US=> M3TxWnNCVkeHUh?=
LS-411N M3fZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrKSIVZUUN3ME20PU4{OTF6IN88US=> MkG4V2FPT0WU
IST-MES1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILEdIZKSzVyPUS5MlU3OjVizszN NX7Qfo9xW0GQR1XS

... 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).

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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
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT00999128 Completed Healthy Volunteers Genentech Inc. October 26 2009 Phase 1
NCT01918306 Terminated Estrogen Receptor Negative Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Triple Negative Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer|Triple-negative Breast Cancer Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Genentech Inc. September 2013 Phase 1|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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID