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 NHTsPJZMcW6jc3WgRZN{[Xl? NYfJd|MxOSCq NXzKWoROTE2VTx?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGSnbIThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NF;SWI0yQDd3NE[1OC=>
Sf9 MnnMT4lv[XOnIFHzd4F6 M1rqZVEhcA>? NGPWXHJFVVOR MoHSTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGgyODR5LWKgcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> MnHUNVg4PTR4NUS=
Sf9 Ml\KT4lv[XOnIFHzd4F6 NXrrdnhHOSCq NEXwRmlFVVOR NEfnXVJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEhTTV2NT3LJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO NVXReGNFOTh5NUS2OVQ>
Sf9 NITQVo5McW6jc3WgRZN{[Xl? MWexJIg> NHTTdW1FVVOR MkDnTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCzN{DPxE1? M3zPPVE5PzV2NkW0
Sf9 NW\xUo5ZU2mwYYPlJGF{e2G7 NYnOUVlwOSCq MVzEUXNQ M4nJO2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> MnfiNVg4PTR4NUS=
MDA-MB-361 M4f4fmZ2dmO2aX;uJGF{e2G7 MlfQNkBp Mnz5SG1UVw>? M2rRdmlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvODJ6IN88US=> NWj2RY95OTh5NUS2OVQ>
PC3 MlLCSpVv[3Srb36gRZN{[Xl? MkPNNkBp NUHBT285TE2VTx?= NGX0V3hKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? NFLqfW8yQDd3NE[1OC=>
U87MG NISxd3JHfW6ldHnvckBCe3OjeR?= M1TnS|IhcA>? MmfESG1UVw>? MmDlTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? M2TlblE5PzV2NkW0
MDA-MB-361 NYnoZ2h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\SbVduQTZiaB?= NHjXUYhFVVOR NETrdnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> MkHVNVg4PTR4NUS=
A2780 MoL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL6fIY6PiCq NFzUVG1FVVOR NULZUItoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= MlPjNVg4PTR4NUS=
PC3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXwPVYhcA>? MWrEUXNQ NFPue4JKSzVyPUCuNlgh|ryP M{DqNlE5PzV2NkW0
U87MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjlW486PiCq MXjEUXNQ Mm\5TWM2OD1yLkm1JO69VQ>? NFnwcZkyQDd3NE[1OC=>
Sf9 NFvrZlJMcW6jc3WgRZN{[Xl? M4\adlMxKG2rbh?= MkD4SG1UVw>? MlXWTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= NFq0XFkzOjV2OEO0Ni=>
RAW 264.7 MXTLbY5ie2ViQYPzZZk> NHXDWm86OCCvaX6= Mln2SG1UVw>? NF3uToJKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> NIXCPVIzOjV2OEO0Ni=>
Sf9 M4XISGtqdmG|ZTDBd5NigQ>? NGHXUXkyKGh? NUDnXppUUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2KndHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPGPUBk\WyuczD3bZRpKEmFNUCgc4YhOC5yMUeg{txO M{HYeVI{PTRyNkS1
Sf9 NXfhTFdEU2mwYYPlJGF{e2G7 NGnhSlUyKGh? MlnKTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= NUC0TVVwOjN3NEC2OFU>
Sf9 NEeyeXpMcW6jc3WgRZN{[Xl? NVTIc45FOSCq MV7Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[4FudWFiZYjwdoV{e2Wm MYiyN|U1ODZ2NR?=
Sf9 MYnLbY5ie2ViQYPzZZk> M4flSFEhcA>? MkG0TY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZB?= NFXMR3czOzV2ME[0OS=>
SKOV3 Mkj6T4lv[XOnIFHzd4F6 NYD2cJJHOSEQvF2= M2TDWlEhcA>? M2HYOWROW09? Mke3TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? NWjzZ3NLOjN|NkCzOFg>
MCF7 M4H3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu5NUDPxE1? MWG5OkBp MmHTSG1UVw>? M3X2O2dKPTB;MD6wO|AzKM7:TR?= MmnCNlM{PjB|NEi=
SKOV3 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fpTlEh|ryP M4TR[|k3KGh? NVO5cYQ2TE2VTx?= NELacVVIUTVyPUCuNVQ4PiEQvF2= MYqyN|M3ODN2OB?=
PC3 MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\EOWd7PzJiaB?= Mn3LSG1UVw>? M2\sR2lEPTB;MD6yPEDPxE1? NWqzZmZVOjF7OEG3NVQ>
MCF7.1 MkHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH5fXlFPzJiaB?= M{Xo[WROW09? NI\RW5JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKEiHUkKg[4Vv\SC5aYToJGlEPTBib3[gNE4zQCEQvF2= MWeyNVk5OTdzNB?=
MCF7-neo/Her2 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnodGo4OiCq NUnuWXc3TE2VTx?= MWXJR|UxRTBwMkmg{txO M2nuOFI{PjZ{OUCz
MCF7-neo/Her2 Mn;WT4lv[XOnIFHzd4F6 NYK2Zo1NUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO NWrv[WkxOjN4NkK5NFM>
PC3 NEfzXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXMVWo4OiCq Ml;kSG1UVw>? M4rObWVEPTB;MD6zOEDPxE1? MViyNVk5PTZ|OR?=
MCF7.1 M3nWTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp NVz0T2Z1TE2VTx?= NVHSdJZCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigSWM2OCCxZjCwMlM6KM7:TR?= NVTIZ3NROjF7OEW2N|k>
PC3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jF[VczKGh? M2X1WGROW09? M4\GfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> M3\hWVIxODVyNk[5
MCF7.1 M2fCbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHZZoQ4OiCq NUPKe2twTE2VTx?= MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCLQ{WwJI9nKDBwM{Sg{txO M{jYUVIxODVyNk[5
MCF7.1 M4nWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzuO|IhcA>? M2nKRWVEPTB;MD63NkDPxE1? NWf5TWt3OjB|NE[2OVY>
NCI-H1975 NYO4W2pPS3m2b4TvfIlkKEG|c3H5 NFTUd|c4OiCq NUDJTIRWUUN3ME2wMlI4KM7:TR?= NWjHWWdYOjNyNUm1OFU>
H460 NWKxRmxbS3m2b4TvfIlkKEG|c3H5 NFrOcIE4OiCq NUnycGhVUUN3ME2wMlg4KM7:TR?= MYCyN|A2QTV2NR?=
HT-29 M3r1bGN6fG:2b4jpZ{BCe3OjeR?= NGDlXlU4OiCq M{nDNGlEPTB;MD62OkDPxE1? M3\6PFI{ODV7NUS1
HepG2 NXvWOpc{S3m2b4TvfIlkKEG|c3H5 MlPRO|IhcA>? M2rPOmlEPTB;MTFOwG0> NG\Cc4ozOzB3OUW0OS=>
SGC7901 NWnhN2l[S3m2b4TvfIlkKEG|c3H5 NEnONoU4OiCq NYnuemxrUUN3ME2xMlgh|ryP NYfYeWZMOjNyNUm1OFU>
NCI-H226 MlzYR5l1d3SxeHnjJGF{e2G7 M2n5O|czKGh? MWDJR|UxRTJwOTFOwG0> NUDlOmNoOjNyNUm1OFU>
A549 MXLDfZRwfG:6aXOgRZN{[Xl? NWnBW2J3PzJiaB?= MkLaTWM2OD14Lkmg{txO NHzWVWMzOzB3OUW0OS=>
U87MG MYrDfZRwfG:6aXOgRZN{[Xl? NUHyZXFNPzJiaB?= MX3JR|UxRTdwN{eg{txO NHPDcWgzOzB3OUW0OS=>
HBC4 NGDnSW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rrRYxw\0eLNUC9MVYvODNiTR?= MUWyNlM{PjJ2Nh?=
BSY1 NE\PXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULsc4dIUTVyPT22MlkxKE1? MnzNNlI{OzZ{NE[=
HBC5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDsc4dIUTVyPT22MlYxKE1? MnS3NlI{OzZ{NE[=
MCF7 MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrqcI9oT0l3ME2tO{4{OyCP MUCyNlM{PjJ2Nh?=
MDA-MB-231 MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7sc4dIUTVyPT21MlQ3KE1? MW[yNlM{PjJ2Nh?=
U251 M{P5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3BcI9oT0l3ME2tOU42OCCP M170W|IzOzN4MkS2
SF268 NGf2dVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTUWHVtd2eJSUWwQU02NjN7IF2= MljpNlI{OzZ{NE[=
SF295 M1\6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrsc4dIUTVyPT22MlM4KE1? MnnsNlI{OzZ{NE[=
SF539 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHwU5BHdG:pR1m1NF0uPi53MDDN NIn5WpkzOjN|NkK0Oi=>
SNB75 M2nYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTmcGhtd2eJSUWwQU04NjFyIF2= NE\6[mwzOjN|NkK0Oi=>
SNB78 NXX5bHVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPvcI9oT0l3ME2tOk42OiCP M1y2UlIzOzN4MkS2
HCC2998 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrHdnNCdG:pR1m1NF0uPi5{OTDN NGTHTIkzOjN|NkK0Oi=>
KM12 NH6w[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzsc4dIUTVyPT21Mlc3KE1? M{nSSlIzOzN4MkS2
HT-29 M4nBOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzZUGFldG:pR1m1NF0uPi5|MDDN MojYNlI{OzZ{NE[=
HCT15 MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXsc4dIUTVyPT22MlEzKE1? NXjNcY83OjJ|M{[yOFY>
HCT116 NEjCNnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq0cI9oT0l3ME2tOU45PyCP NVv1WGpVOjJ|M{[yOFY>
NCI-H23 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL1Xmltd2eJSUWwQU02Njd|IF2= NUXaOVl7OjJ|M{[yOFY>
NCI-H226 MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL1OYNwdG:pR1m1NF0uPi5{MTDN MWOyNlM{PjJ2Nh?=
NCI-H522 NETOcYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ruWYxw\0eLNUC9MVYvPThiTR?= MUSyNlM{PjJ2Nh?=
NCI-H483 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvscI9oT0l3ME2tOk42PiCP MUeyNlM{PjJ2Nh?=
A549 NX\wXlVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fNU4xw\0eLNUC9MVYvOTViTR?= M2XtS|IzOzN4MkS2
DMS273 NYiz[FRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DQRoxw\0eLNUC9MVYvPDNiTR?= Mnv4NlI{OzZ{NE[=
DMS114 M2DBSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\sc4dIUTVyPT21MlkzKE1? M2HlV|IzOzN4MkS2
LOXIMVI M{SzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXwTYZtd2eJSUWwQU03NjJ7IF2= MnnjNlI{OzZ{NE[=
OVCAR3 NVru[ld1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILs[GNtd2eJSUWwQU03NjdzIF2= NH7UO2szOjN|NkK0Oi=>
OVCAR4 MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DGOIxw\0eLNUC9MVUvPzZiTR?= NIDwSJAzOjN|NkK0Oi=>
OVCAR5 NWrpPHVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnsc4dIUTVyPT22MlI3KE1? NGH2TFAzOjN|NkK0Oi=>
OVCAR8 NWjSOJlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTsc4dIUTVyPT21Mlc{KE1? NVTOOWlOOjJ|M{[yOFY>
SKOV3 NYi5WlRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXwcI9oT0l3ME2tOk42OiCP MXyyNlM{PjJ2Nh?=
RXF631L NUXk[Wh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3scI9oT0l3ME2tOk45QCCP M{PS[|IzOzN4MkS2
ACHN M{S2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjmUWNjdG:pR1m1NF0uPi5yNzDN NV7Ld2k1OjJ|M{[yOFY>
St-4 Ml7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTNZ3BOdG:pR1m1NF0uPS53NjDN NFvKO3EzOjN|NkK0Oi=>
MKN1 M1;ad2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO3cXRtd2eJSUWwQU04NjB6IF2= NHL1cVkzOjN|NkK0Oi=>
MKN7 M{flOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1riZYxw\0eLNUC9MVYvPTBiTR?= NHnRVnMzOjN|NkK0Oi=>
MKN28 M2XOfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTsc4dIUTVyPT21MlUzKE1? NUDEZ29NOjJ|M{[yOFY>
MKN45 M4TweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXscI9oT0l3ME2tOk42PSCP Ml:5NlI{OzZ{NE[=
MKN74 NXvhfZlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXsc4dIUTVyPT22MlAzKE1? M4\uflIzOzN4MkS2
DU145 M{\4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjNNWtOdG:pR1m1NF0uPS56NTDN MkfrNlI{OzZ{NE[=
PC3 M2n0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTrcI9oT0l3ME2tOk43PiCP MlvENlI{OzZ{NE[=
ES5 M2LQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTVyLkKxJI5O MWXTRW5ITVJ?
HH M3vs[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrjTWM2OD1zMUGuNFghdk1? NFz1cWFUSU6JRWK=
MHH-PREB-1 NIrjR41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFzND6zJI5O MWTTRW5ITVJ?
NCI-H1770 M4LiW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTFbo02UUN3ME2xNlMvQDZibl2= MlXlV2FPT0WU
HuO9 M13wPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETwdXFKSzVyPUKwOk4xOiCwTR?= MofJV2FPT0WU
HAL-01 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorzTWM2OD1{ME[uO|Mhdk1? MXPTRW5ITVJ?
NOS-1 NFTobWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;RVmlEPTB;MkGxMlgzKG6P M4rkUHNCVkeHUh?=
HGC-27 M{ThdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPZeo1sUUN3ME2yNVIvPTdibl2= M4H5SHNCVkeHUh?=
NB69 NIDLWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ2NT6yO{BvVQ>? M3PuU3NCVkeHUh?=
RS4-11 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXKxZVhNUUN3ME2yOlEvPzZibl2= MmPlV2FPT0WU
DOK M{XrOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jRTGlEPTB;M{CxMlchdk1? NY\xPFJ6W0GQR1XS
LB2241-RCC M4DCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjrNVFKSzVyPUOwN{45PCCwTR?= NFPqZWJUSU6JRWK=
NCI-H1623 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO4TWM2OD1|MESuNFghdk1? NEPUO5NUSU6JRWK=
YH-13 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr6TWM2OD1|MESuN|Ihdk1? MnPnV2FPT0WU
BPH-1 NGjyT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNzNDDuUS=> M1zIcXNCVkeHUh?=
AN3-CA NEXFdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLjTWM2OD1|NECuN|chdk1? NUj1WJJ5W0GQR1XS
ES7 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK3WodKSzVyPUO0NU46QSCwTR?= M1nGb3NCVkeHUh?=
MDA-MB-175-VII MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPZUZJvUUN3ME2zOVIvQTJibl2= Mny0V2FPT0WU
GAMG MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\UdGdOUUN3ME2zO|AvQDVibl2= M2rZOnNCVkeHUh?=
CHL-1 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfhWotKSzVyPUO3PE43PSCwTR?= NYOyN4ZVW0GQR1XS
NB7 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LMbGlEPTB;M{i5Mlg{KG6P MV7TRW5ITVJ?
MFE-280 M3rLdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrieXRKSzVyPUSxPE4zKG6P MXfTRW5ITVJ?
HL-60 NUXXbnY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC3OWt[UUN3ME20NlUvPzVibl2= M1[wfHNCVkeHUh?=
GCIY MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrK[nhUUUN3ME20N|MvQCCwTR?= MY\TRW5ITVJ?
MDA-MB-361 M3zDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR|OT6xN{BvVQ>? NE\FT4NUSU6JRWK=
LXF-289 NH7xPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR2OD6yO{BvVQ>? MXnTRW5ITVJ?
NBsusSR NYjHfHRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3JSHlKSzVyPUS4PE45PSCwTR?= MYHTRW5ITVJ?
KU-19-19 Mo\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT4TWM2OD13MU[uNFchdk1? MlzmV2FPT0WU
A204 M1LRNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K2b2lEPTB;NUKyMlM{KG6P NFjaSIxUSU6JRWK=
LB1047-RCC NV7yb|NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H6UWlEPTB;NUKyMlk{KG6P MVrTRW5ITVJ?
COLO-684 NX;WV25sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfFUWZKSzVyPUWyN{4yOSCwTR?= MoHhV2FPT0WU
PA-1 NXqx[mFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\NbWlEPTB;NUOyMlQyKG6P M1XHbXNCVkeHUh?=
MG-63 M2jyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4exSmlEPTB;NUSxMlEyKG6P M3PoUnNCVkeHUh?=
BHT-101 Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\uVG9KSzVyPUW0OE46PCCwTR?= M3LVcXNCVkeHUh?=
NKM-1 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXlNY1uUUN3ME21PVMvODlibl2= Ml3VV2FPT0WU
T47D MlP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTV7Nz61OkBvVQ>? NEDSUoxUSU6JRWK=
MOLT-4 NYTJUWNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13OTWlEPTB;NkKzMlYzKG6P M1nFd3NCVkeHUh?=
IGROV-1 MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;GdGlEPTB;NkO0MlMyKG6P M2\INHNCVkeHUh?=
ES4 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTZ|OT61OEBvVQ>? MXPTRW5ITVJ?
HuO-3N1 MkDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPaTWM2OD14NEKuN|ghdk1? MV;TRW5ITVJ?
NEC8 NF\ZfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvwelFMUUN3ME22OVMvPTdibl2= Mn;HV2FPT0WU
HO-1-N-1 NWP3VHk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTZ3OT6xO{BvVQ>? M1;HdnNCVkeHUh?=
EPCL-272H M325SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TLdmlEPTB;Nki3MlIyKG6P NFrEfWVUSU6JRWK=
D-263MG M4PXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nJemlEPTB;N{G4MlEhdk1? MkDOV2FPT0WU
MV-4-11 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHQ[GdKSzVyPUeyOE4{OSCwTR?= MXLTRW5ITVJ?
SK-NEP-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTd{NT65OEBvVQ>? MnjxV2FPT0WU
SW872 MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NISwXo9KSzVyPUeyO{45QSCwTR?= NYrjV5BWW0GQR1XS
P30-OHK Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDiTWM2OD15M{CuO|Ehdk1? MWTTRW5ITVJ?
OMC-1 M2DwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[0[HpVUUN3ME23OVEvODlibl2= NXm4N5ZKW0GQR1XS
LoVo NF3xcmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH5VlZlUUN3ME23O|cvQSCwTR?= M2jqOnNCVkeHUh?=
LNCaP-Clone-FGC M1\2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTd7Nj6zOEBvVQ>? NHnRWlZUSU6JRWK=
L-363 M1XwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrLSZN7UUN3ME23PVgvPDJibl2= M4HMSHNCVkeHUh?=
ES8 MmnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnuV4diUUN3ME24NVAvPTJibl2= M1jqUnNCVkeHUh?=
697 M{DWUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn72TWM2OD16M{GuOVUhdk1? M1nRWnNCVkeHUh?=
HSC-3 NWDaU3NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmD4TWM2OD16M{muOVQhdk1? MlPTV2FPT0WU
H4 M2XBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITyc5RKSzVyPUi1NE45PSCwTR?= NW[wVFloW0GQR1XS
QIMR-WIL MkO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTh4NT6yJI5O NVm4U3lPW0GQR1XS
OAW-42 M1rSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoH3TWM2OD16N{KuNVkhdk1? M1fzOnNCVkeHUh?=
MCF7 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTh7OD61PUBvVQ>? NVLufodZW0GQR1XS
SCC-25 M4\FVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7ZTWM2OD17MUSuNVkhdk1? MmXZV2FPT0WU
NCI-H1563 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELQOpZKSzVyPUmxOU46QSCwTR?= NV31fGRWW0GQR1XS
OVCAR-5 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfiTWM2OD17NECuNVchdk1? NXHMTXJlW0GQR1XS
HDLM-2 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTl2OT6yJI5O MmjUV2FPT0WU
NB5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlroTWM2OD17NU[uOkBvVQ>? MVvTRW5ITVJ?
NCI-H292 MnrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTl5ND6zNkBvVQ>? NHvk[4tUSU6JRWK=
A101D MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTuRXdYUUN3ME25PVAvOTlibl2= MY\TRW5ITVJ?
NCI-H1648 NH30UG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTl7OD61NUBvVQ>? NYLVUHBLW0GQR1XS
EKVX Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwMEGyPUDPxE1? NGT4SoVUSU6JRWK=
SW1710 M{TEZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3DTWM2OD1zLkC0NlM{KM7:TR?= MmHIV2FPT0WU
WM-115 NHjkc21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFwME[2OVYh|ryP NETLU3FUSU6JRWK=
CAL-54 MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvMc3ZkUUN3ME2xMlA4ODhzIN88US=> M{iwdXNCVkeHUh?=
TGBC24TKB MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwMEiwOFUh|ryP NFLPV2dUSU6JRWK=
NCI-H520 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDtTWM2OD1zLkC4PVY4KM7:TR?= MlHPV2FPT0WU
D-423MG Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\XTWM2OD1zLkC5PVYzKM7:TR?= Mn2xV2FPT0WU
BFTC-905 MkS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWraWJFYUUN3ME2xMlE{PDR7IN88US=> NWrSTVFoW0GQR1XS
HT NUfFfodlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TXSWlEPTB;MT6xN|Q4QCEQvF2= NEnaOY5USU6JRWK=
CTB-1 NXrOeYhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;1[JBjUUN3ME2xMlE1Ojl|IN88US=> Mkn3V2FPT0WU
Hs-578-T MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnjTWM2OD1zLkG5OVY2KM7:TR?= NVfLWJBGW0GQR1XS
HuH-7 NI\sPGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFwMkC5OFkh|ryP NY\3R5VFW0GQR1XS
LB996-RCC NGm1SlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXUS3pKSzVyPUGuNlIyPzdizszN NXO3S5BNW0GQR1XS
KYSE-270 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\I[4xKSzVyPUGuNlk4OzRizszN Ml\TV2FPT0WU
A4-Fuk MmPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGxepRYUUN3ME2xMlI6QTl|IN88US=> Mlq0V2FPT0WU
A498 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwM{C0O|Qh|ryP MnLLV2FPT0WU
SK-MEL-1 Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLOV3VKSzVyPUGuN|A3PzlizszN M1jWOHNCVkeHUh?=
AU565 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfjbG9KSzVyPUGuN|E5PjNizszN M1\Hb3NCVkeHUh?=
Saos-2 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTDVINOUUN3ME2xMlM{OjB3IN88US=> MoXOV2FPT0WU
A549 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmS2TWM2OD1zLkO5PVch|ryP MY\TRW5ITVJ?
BFTC-909 M2nVOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwNEOzNFUh|ryP MmfUV2FPT0WU
MDA-MB-415 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwNEi2PVIh|ryP MXXTRW5ITVJ?
639-V M1P2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zu[2lEPTB;MT61NFI1PSEQvF2= M{LyNnNCVkeHUh?=
A704 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPaTWM2OD1zLkWwO|g2KM7:TR?= M3XlUHNCVkeHUh?=
PANC-03-27 M2m4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4izV2lEPTB;MT61NVQxQCEQvF2= MojUV2FPT0WU
SK-MEL-28 NY\tVJFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3HS|FKSzVyPUGuOVYxQDVizszN NVPsNpNjW0GQR1XS
Ramos-2G6-4C10 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny0TWM2OD1zLk[wO|Q3KM7:TR?= M4rNOXNCVkeHUh?=
HuP-T4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XJZ2lEPTB;MT62NFc4QCEQvF2= NHrFfphUSU6JRWK=
VA-ES-BJ MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXTVmtKSzVyPUGuOlEzPyEQvF2= NUTObWJ5W0GQR1XS
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MDA-MB-453 MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXmXWdKSzVyPUG3MlAxODNizszN MnXGV2FPT0WU
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NCI-H1793 NEfFfmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVWxU5hGUUN3ME2xPE4yPThzIN88US=> NVHTbpdEW0GQR1XS
HCC1395 NYe0eJhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\DfmlEPTB;MUiuOVYyOSEQvF2= MXnTRW5ITVJ?
NUGC-3 Mn;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ixUGlEPTB;MUiuOlU5PCEQvF2= MlPkV2FPT0WU
BB65-RCC NGribo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTXUFQ5UUN3ME2xPE43PjlizszN MlHxV2FPT0WU
RMG-I MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTTTWM2OD1zOD63N|gzKM7:TR?= M1LCNnNCVkeHUh?=
LS-513 M3HJe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF6LkmyNlgh|ryP M1fpd3NCVkeHUh?=
MFM-223 M2S4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXe4[lNQUUN3ME2xPU4xPzF4IN88US=> NWX2dIVyW0GQR1XS
NCI-H727 NFrac4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXuUIVKSzVyPUG5MlMzQTVizszN MXLTRW5ITVJ?
KP-4 NIrTcohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HaPGlEPTB;MUmuPFU{OSEQvF2= MmL4V2FPT0WU
NB13 NFHxR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTVRnY6UUN3ME2xPU45QDN7IN88US=> M4nSbHNCVkeHUh?=
UACC-893 MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iwSmlEPTB;MUmuPVc2PyEQvF2= NGHiWIlUSU6JRWK=
HT-1197 Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy1UppKSzVyPUKwMlI6PThizszN NWfIdJdxW0GQR1XS
NCI-H2029 NFP3UVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf1R4hmUUN3ME2yNE4{OjZ4IN88US=> NF34[GVUSU6JRWK=
GI-ME-N Moe3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jzbGlEPTB;MkCuN|M4OyEQvF2= M37NV3NCVkeHUh?=
OVCAR-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XmeWlEPTB;MkCuOVgzOiEQvF2= NIrlZlBUSU6JRWK=
HD-MY-Z NHTwbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fxRmlEPTB;MkGuN|Y6PiEQvF2= NWLB[4xTW0GQR1XS
NTERA-S-cl-D1 NHjqW5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\3TWM2OD1{MT62O|IzKM7:TR?= NIPtNI9USU6JRWK=
SCH NX2wNYhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJ{LkS5OkDPxE1? NUXy[nhwW0GQR1XS
KARPAS-299 NWThT|NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn1XYdKSzVyPUKzMlM5QDdizszN NHP1[5hUSU6JRWK=
NCI-H1650 M2jE[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;RfJpKSzVyPUKzMlkzPDFizszN M3;xXHNCVkeHUh?=
ACHN MkGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInIToFKSzVyPUK0MlQ3PTZizszN MVPTRW5ITVJ?
M059J NIi0VYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ2LkW2N|Qh|ryP NWSze|JFW0GQR1XS
AM-38 M4[wV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHXUnZiUUN3ME2yOU41QDFizszN M1rTfXNCVkeHUh?=
KG-1 MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILaOIZKSzVyPUK1MlU1QTRizszN NVG5OHBwW0GQR1XS
COLO-824 M4\kbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml73TWM2OD1{NT61OVk6KM7:TR?= NHPmXGlUSU6JRWK=
NCI-H1155 M{nUZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf6dJlKSzVyPUK1MlU5PDdizszN NInHNXZUSU6JRWK=
NCI-H441 NGTiVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4OzdmlEPTB;MkWuO|Q3PSEQvF2= MWLTRW5ITVJ?
J-RT3-T3-5 NVnYS2lUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jHS2lEPTB;Mk[uN|AzPyEQvF2= M3rr[3NCVkeHUh?=
JEG-3 M3O5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrDSotKSzVyPUK2MlY5ODVizszN MVXTRW5ITVJ?
RKO M{\zUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWWwT3A1UUN3ME2yOk44PjN{IN88US=> MV7TRW5ITVJ?
CAL-85-1 MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXUdm9KSzVyPUK3MlIyOThizszN MoXQV2FPT0WU
CAL-120 M2\1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnMXYdbUUN3ME2yO{43QTF2IN88US=> M3fJeHNCVkeHUh?=
NCI-H2452 NHvre5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn60TWM2OD1{Nz63O|E3KM7:TR?= MkXnV2FPT0WU
NCI-H1395 M4HsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTUTWM2OD1{Nz63PFM{KM7:TR?= NXH4VFd5W0GQR1XS
KYSE-450 M2C0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfVdFdlUUN3ME2yO{46QDZ{IN88US=> MUfTRW5ITVJ?
S-117 NHHWbolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnXUZZKSzVyPUK5MlM5PTdizszN NV75bG9CW0GQR1XS
SW13 NGjlSnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\ZVYlKSzVyPUK5Mlg2OTlizszN NIPFbY1USU6JRWK=
ES3 Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTNyLkO3N|Mh|ryP NX\VRm5wW0GQR1XS
HCT-116 MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETvc|dKSzVyPUOwMlU2PTRizszN MU\TRW5ITVJ?
NCI-H1693 NGLWR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTNyLkW5OFIh|ryP NXnkOWpiW0GQR1XS
VM-CUB-1 NGTMPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNyLk[0NVMh|ryP NWHI[ItXW0GQR1XS
NCI-H2170 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTNzLkW3PFQh|ryP Mmj6V2FPT0WU
ALL-PO MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTNzLki0Nlgh|ryP MXTTRW5ITVJ?
NCI-H661 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TWZWlEPTB;M{KuNFYzOyEQvF2= NIPNTYRUSU6JRWK=
NCI-H2347 NFfYbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TCemlEPTB;M{KuOFg{PyEQvF2= M3jxRnNCVkeHUh?=
FTC-133 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S1VmlEPTB;M{KuO|A3KM7:TR?= NX\3OXQ1W0GQR1XS
COLO-829 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLLTWM2OD1|Mz6zOFY4KM7:TR?= NXrUPGVDW0GQR1XS
GOTO NH\RN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDmTWM2OD1|Mz61NlU5KM7:TR?= MV\TRW5ITVJ?
YAPC MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHMR5BNUUN3ME2zN{45OTV7IN88US=> M4n4bnNCVkeHUh?=
LCLC-103H M4LISGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\nbVRDUUN3ME2zOE4yPjJ2IN88US=> MVXTRW5ITVJ?
SiHa M3LrNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDQTWM2OD1|ND6zPFE4KM7:TR?= MUnTRW5ITVJ?
LK-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7YeYNKSzVyPUO0MlU4ODhizszN NVLtUlJNW0GQR1XS
KP-N-YS MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TJNmlEPTB;M{SuO|IxOiEQvF2= NH65[2pUSU6JRWK=
NCI-SNU-1 NUD5ToFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrZTWM2OD1|NT6xO|kh|ryP NWTscmJHW0GQR1XS
KNS-81-FD MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTN3Lk[2N{DPxE1? NVrTOYZnW0GQR1XS
SCC-9 M3G0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPCdHFKSzVyPUO2MlcyPDZizszN NXGxTlg1W0GQR1XS
SH-4 M{LTOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN4LkezJO69VQ>? NFO2eHBUSU6JRWK=
HCC-1954 NF\UcXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rmeGlEPTB;M{euNlczQSEQvF2= MXLTRW5ITVJ?
BALL-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTN5LkWzNVYh|ryP MYnTRW5ITVJ?
BE-13 MnS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XoeGlEPTB;M{euO|AyQCEQvF2= NWfrXWZ7W0GQR1XS
COLO-678 NYe4NHhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG1PWpKSzVyPUO3Mlk1OzdizszN MUTTRW5ITVJ?
SK-MEL-3 NH\pcW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTN6LkKzPVch|ryP M37LWnNCVkeHUh?=
OAW-28 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvQTWM2OD1|OD62N|kh|ryP Mmi5V2FPT0WU
CAMA-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jaUGlEPTB;M{iuPVY6OSEQvF2= NFTxeVZUSU6JRWK=
C2BBe1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XiNGlEPTB;M{muPFE5KM7:TR?= MVjTRW5ITVJ?
A3-KAW NGDO[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrjNpFtUUN3ME20NE4{PjZzIN88US=> NInwSHVUSU6JRWK=
SK-MEL-24 NXH3W3ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPiTWM2OD12MD61PVMyKM7:TR?= MlvYV2FPT0WU
KYSE-140 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLBTWM2OD12MD63NVY2KM7:TR?= MV;TRW5ITVJ?
MOLT-16 MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TSVGlEPTB;NEGuNVU{PiEQvF2= MmPGV2FPT0WU
CFPAC-1 NH;mc45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTR{LkWyNVEh|ryP NHHk[otUSU6JRWK=
NB14 M4jm[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\5TWM2OD12Mj63NFI4KM7:TR?= NYnMcolJW0GQR1XS
COLO-792 M4LWOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrVSFlDUUN3ME20Nk45QTZzIN88US=> M4P4R3NCVkeHUh?=
RH-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\jTWM2OD12Mz60PFM3KM7:TR?= MnjYV2FPT0WU
NCI-H522 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXI[2dKUUN3ME20OE4{PTZ6IN88US=> MnfvV2FPT0WU
Ca-Ski NXjEPI5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml74TWM2OD12ND64NVE1KM7:TR?= MV7TRW5ITVJ?
KGN NIfNNldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR6LkOwOlMh|ryP MmnzV2FPT0WU
UACC-62 M4XnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXaem5nUUN3ME20PE41ODd{IN88US=> NULFOW9UW0GQR1XS
NCI-H358 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6xTWM2OD12OT6zNFE5KM7:TR?= M{P5VXNCVkeHUh?=
LS-411N MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTR7LkOxNVgh|ryP MX;TRW5ITVJ?
IST-MES1 M4HOU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[zTWM2OD12OT61OlI2KM7:TR?= MXHTRW5ITVJ?

... 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:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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
NCT02092831 Completed Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01474668 Completed Healthy Volunteer Genentech Inc. October 2011 Phase 1
NCT01437566 Completed Breast Cancer Genentech Inc. October 2011 Phase 2

Tech Support

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

Handling Instructions

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

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

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID