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 58 Publications

8 Customer Reviews

  • 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.. 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 M1jXd2tqdmG|ZTDBd5NigQ>? MWixJIg> MnXISG1UVw>? NHfKTJhKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHTlcJRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlAxOyEQvF2= MnWwNVg4PTR4NUS=
Sf9 NGLKSotMcW6jc3WgRZN{[Xl? MlixNUBp NFi4PJVFVVOR NVPTendnUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? M{H4XVE5PzV2NkW0
Sf9 MXfLbY5ie2ViQYPzZZk> NGK5c5gyKGh? NVT1cXJ2TE2VTx?= MoXjTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NWm1dGh6OTh5NUS2OVQ>
Sf9 MmPOT4lv[XOnIFHzd4F6 M3Llb|EhcA>? NVfsOnc1TE2VTx?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMEOzJO69VQ>? M2DpRVE5PzV2NkW0
Sf9 Ml;BT4lv[XOnIFHzd4F6 M4CxfFEhcA>? NEfzS2JFVVOR MnyyTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> MUOxPFc2PDZ3NB?=
MDA-MB-361 NYO3PFlMTnWwY4Tpc44hSXO|YYm= MVSyJIg> MWrEUXNQ MWPJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlAzQCEQvF2= MYCxPFc2PDZ3NB?=
PC3 NEixR|FHfW6ldHnvckBCe3OjeR?= MV[yJIg> NVztWYsyTE2VTx?= NYHvWVVjUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gVGM{KGOnbHzzJJdqfGhiSVO1NEBw\iByLkCzO{DPxE1? NHPr[msyQDd3NE[1OC=>
U87MG NWnjdo5XTnWwY4Tpc44hSXO|YYm= M1vvVVIhcA>? MWjEUXNQ M1zXUmlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? NF;DOXMyQDd3NE[1OC=>
MDA-MB-361 MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHHPVYhcA>? MVTEUXNQ NVOxbFVpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC55MjFOwG0> NHTEXI8yQDd3NE[1OC=>
A2780 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXrTmU6PiCq NVTrUHhoTE2VTx?= NYTXTHJ5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= Moq0NVg4PTR4NUS=
PC3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTU[|Q6PiCq M1;oSGROW09? NWKxNHlvUUN3ME2wMlI5KM7:TR?= NIjpU2IyQDd3NE[1OC=>
U87MG NVPm[3d3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUe5OkBp MXLEUXNQ MmTtTWM2OD1yLkm1JO69VQ>? M2XCVFE5PzV2NkW0
Sf9 NVy4b3NlU2mwYYPlJGF{e2G7 M4XDPVMxKG2rbh?= MX;EUXNQ MkDQTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= MlfaNlI2PDh|NEK=
RAW 264.7 NXjvcYoyU2mwYYPlJGF{e2G7 M{Lhc|kxKG2rbh?= NWfP[nFmTE2VTx?= NGCzOINKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> MUOyNlU1QDN2Mh?=
Sf9 M4S3dmtqdmG|ZTDBd5NigQ>? NXjyS4RNOSCq MYPJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZoV1[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW0Z7IHPlcIx{KHerdHigTWM2OCCxZjCwMlAyPyEQvF2= MXOyN|U1ODZ2NR?=
Sf9 M1[4SGtqdmG|ZTDBd5NigQ>? NVvYUm1POSCq M2DTOWlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= MlXzNlM2PDB4NEW=
Sf9 NUjtVm5xU2mwYYPlJGF{e2G7 M375[|EhcA>? MmDMTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4didW2jIHX4dJJme3OnZB?= MnPlNlM2PDB4NEW=
Sf9 NIPEc|BMcW6jc3WgRZN{[Xl? NITG[JoyKGh? NY\4bJI{UW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2GucHjhJIV5eHKnc4Pl[C=> NHXXTm0zOzV2ME[0OS=>
SKOV3 M3jTdmtqdmG|ZTDBd5NigQ>? MkD4NUDPxE1? MljaNUBp MUnEUXNQ NF3FNFBKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w MXiyN|M3ODN2OB?=
MCF7 NYi0NXJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHUcHV6OSEQvF2= M2ro[lk3KGh? NX7GVZFHTE2VTx?= NYXtVWhNT0l3ME2wMlA4ODJizszN NVfXNlZCOjN|NkCzOFg>
SKOV3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:5XlEh|ryP MW[5OkBp MoTISG1UVw>? MUjHTVUxRTBwMUS3OkDPxE1? M2fwUVI{OzZyM{S4
PC3 NFrqRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPXO4I4OiCq MU\EUXNQ NV3JUIdsUUN3ME2wMlI5KM7:TR?= Ml3xNlE6QDF5MUS=
MCF7.1 NWj6cWlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfJO|IhcA>? MnfsSG1UVw>? Mn7URY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BJTVJ{IHflcoUhf2m2aDDJR|UxKG:oIECuNlgh|ryP NYDiVW5ROjF7OEG3NVQ>
MCF7-neo/Her2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe3NkBp M170dWROW09? MnnYTWM2OD1yLkK5JO69VQ>? NXLSSoNiOjN4NkK5NFM>
MCF7-neo/Her2 M{LLTGtqdmG|ZTDBd5NigQ>? MYLJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDTOFc{KHerdHigTWM2OCCxZjCwMlAxPyEQvF2= M323d|I{PjZ{OUCz
PC3 MlnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLJPJY4OiCq MVHEUXNQ MVjFR|UxRTBwM{Sg{txO MWiyNVk5PTZ|OR?=
MCF7.1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzkSYc4OiCq M4XIVWROW09? MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCHQ{WwJI9nKDBwM{mg{txO MXGyNVk5PTZ|OR?=
PC3 M{f0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\N[|Q4OiCq M{LNUGROW09? NIDieXpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> M1TReVIxODVyNk[5
MCF7.1 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17zOVczKGh? M2XuUmROW09? M1\rN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFnDOVAhd2ZiMD6zOEDPxE1? M2r0NVIxODVyNk[5
MCF7.1 NIDuNJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKwO|IhcA>? M2TSUGVEPTB;MD63NkDPxE1? MlrqNlA{PDZ4NU[=
NCI-H1975 NWTVfZU1S3m2b4TvfIlkKEG|c3H5 MWq3NkBp NXrHPGlTUUN3ME2wMlI4KM7:TR?= MmPONlMxPTl3NEW=
H460 M1LBemN6fG:2b4jpZ{BCe3OjeR?= M2fyTFczKGh? M2TBXWlEPTB;MD64O{DPxE1? MmT2NlMxPTl3NEW=
HT-29 M1TDNmN6fG:2b4jpZ{BCe3OjeR?= MWS3NkBp MoTLTWM2OD1yLk[2JO69VQ>? NUf2[lIzOjNyNUm1OFU>
HepG2 MXvDfZRwfG:6aXOgRZN{[Xl? M2\3dFczKGh? MYHJR|UxRTFizszN MUCyN|A2QTV2NR?=
SGC7901 NX3ud|JKS3m2b4TvfIlkKEG|c3H5 M13SOVczKGh? MmXoTWM2OD1zLkig{txO MVGyN|A2QTV2NR?=
NCI-H226 M3iwWmN6fG:2b4jpZ{BCe3OjeR?= M{K5W|czKGh? NG[1XWZKSzVyPUKuPUDPxE1? MkT2NlMxPTl3NEW=
A549 NHv0UFREgXSxdH;4bYMhSXO|YYm= MkDSO|IhcA>? NFPBfFNKSzVyPU[uPUDPxE1? NHnFe|MzOzB3OUW0OS=>
U87MG M2fnU2N6fG:2b4jpZ{BCe3OjeR?= MoD0O|IhcA>? MoTHTWM2OD15Lke3JO69VQ>? MoLZNlMxPTl3NEW=
HBC4 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jaeoxw\0eLNUC9MVYvODNiTR?= MmjVNlI{OzZ{NE[=
BSY1 NYrlVIxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rGRYxw\0eLNUC9MVYvQTBiTR?= NFqzboMzOjN|NkK0Oi=>
HBC5 M3;icGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfHcI9oT0l3ME2tOk43OCCP MkDnNlI{OzZ{NE[=
MCF7 NIfySI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e4Voxw\0eLNUC9MVcvOzNiTR?= NXfVSHZPOjJ|M{[yOFY>
MDA-MB-231 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rUboxw\0eLNUC9MVUvPDZiTR?= MWWyNlM{PjJ2Nh?=
U251 M3nXeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPUR3dtd2eJSUWwQU02NjVyIF2= MVuyNlM{PjJ2Nh?=
SF268 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnuUYttd2eJSUWwQU02NjN7IF2= NHuw[W8zOjN|NkK0Oi=>
SF295 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXCcI9oT0l3ME2tOk4{PyCP MXyyNlM{PjJ2Nh?=
SF539 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTsc4dIUTVyPT22MlUxKE1? NHW0d4wzOjN|NkK0Oi=>
SNB75 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HMcoxw\0eLNUC9MVcvOTBiTR?= NF3ES3czOjN|NkK0Oi=>
SNB78 M4T1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7CN5Rtd2eJSUWwQU03NjV{IF2= M4TUOFIzOzN4MkS2
HCC2998 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTuXlBtd2eJSUWwQU03NjJ7IF2= MkfBNlI{OzZ{NE[=
KM12 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Trfoxw\0eLNUC9MVUvPzZiTR?= NGrwbngzOjN|NkK0Oi=>
HT-29 MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTsc4dIUTVyPT22MlMxKE1? MkL0NlI{OzZ{NE[=
HCT15 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXzW|A4dG:pR1m1NF0uPi5zMjDN Mn[2NlI{OzZ{NE[=
HCT116 NE\we2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLsc4dIUTVyPT21Mlg4KE1? NHW3bngzOjN|NkK0Oi=>
NCI-H23 NUH5PVJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXwTYltd2eJSUWwQU02Njd|IF2= NEHXOYgzOjN|NkK0Oi=>
NCI-H226 M3vMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLwO3Ftd2eJSUWwQU03NjJzIF2= MV6yNlM{PjJ2Nh?=
NCI-H522 M33JSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLIcI9oT0l3ME2tOk42QCCP NEDxZmQzOjN|NkK0Oi=>
NCI-H483 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\He2xJdG:pR1m1NF0uPi53NjDN MlTTNlI{OzZ{NE[=
A549 NGfxcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOwcI9oT0l3ME2tOk4yPSCP MlK3NlI{OzZ{NE[=
DMS273 NXfVPFlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHxSoVtd2eJSUWwQU03NjR|IF2= MlL2NlI{OzZ{NE[=
DMS114 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfPcI9oT0l3ME2tOU46OiCP MUGyNlM{PjJ2Nh?=
LOXIMVI NXrTPY5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jlTYxw\0eLNUC9MVYvOjliTR?= NGjDV4wzOjN|NkK0Oi=>
OVCAR3 NYfaZXh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF63bHZtd2eJSUWwQU03NjdzIF2= MVeyNlM{PjJ2Nh?=
OVCAR4 MnjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrqVINtd2eJSUWwQU02Njd4IF2= NYrmZm9FOjJ|M{[yOFY>
OVCAR5 M33NVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEC0TYltd2eJSUWwQU03NjJ4IF2= NGrLRmkzOjN|NkK0Oi=>
OVCAR8 MoDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Toeoxw\0eLNUC9MVUvPzNiTR?= Mof2NlI{OzZ{NE[=
SKOV3 NXPwOI5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXO2XY9bdG:pR1m1NF0uPi53MjDN M1;Ye|IzOzN4MkS2
RXF631L NXmxW3F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;vcWVtd2eJSUWwQU03Njh6IF2= M1\jT|IzOzN4MkS2
ACHN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\sc4dIUTVyPT22MlA4KE1? M13jS|IzOzN4MkS2
St-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTqcI9oT0l3ME2tOU42PiCP MkK0NlI{OzZ{NE[=
MKN1 NIf6d4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;sc4dIUTVyPT23MlA5KE1? M3XXRVIzOzN4MkS2
MKN7 NITTcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjrcI9oT0l3ME2tOk42OCCP MVqyNlM{PjJ2Nh?=
MKN28 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPYSGttd2eJSUWwQU02NjV{IF2= NY\hRoNXOjJ|M{[yOFY>
MKN45 NYnoZVNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3exZoxw\0eLNUC9MVYvPTViTR?= MXiyNlM{PjJ2Nh?=
MKN74 M2nCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TyUYxw\0eLNUC9MVYvODJiTR?= MWWyNlM{PjJ2Nh?=
DU145 NEn3cWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\sc4dIUTVyPT21Mlg2KE1? NELuelIzOjN|NkK0Oi=>
PC3 NGj4fYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPLUGRtd2eJSUWwQU03NjZ4IF2= MUeyNlM{PjJ2Nh?=
ES5 MkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvMWnljUUN3ME21NE4zOSCwTR?= MX;TRW5ITVJ?
HH NX\OTm54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFzMT6wPEBvVQ>? MXjTRW5ITVJ?
MHH-PREB-1 NVHWemtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKzTWM2OD1zMUSuN{BvVQ>? M4jVUHNCVkeHUh?=
NCI-H1770 M17NTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j6OmlEPTB;MUKzMlg3KG6P MmTwV2FPT0WU
HuO9 MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXuTWM2OD1{ME[uNFIhdk1? M4DxbHNCVkeHUh?=
HAL-01 M3TtWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJyNj63N{BvVQ>? NWnicYhGW0GQR1XS
NOS-1 MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\BWmlEPTB;MkGxMlgzKG6P MkCyV2FPT0WU
HGC-27 M{Ho[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH3XpRKSzVyPUKxNk42PyCwTR?= M1vBb3NCVkeHUh?=
NB69 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn6cmtKSzVyPUK0OU4zPyCwTR?= NV7DSXFpW0GQR1XS
RS4-11 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJ4MT63OkBvVQ>? MmPxV2FPT0WU
DOK NGP5c4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\icYxKSzVyPUOwNU44KG6P NHzhOmRUSU6JRWK=
LB2241-RCC NVLpXGNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHOx[phKSzVyPUOwN{45PCCwTR?= NWDLUpJPW0GQR1XS
NCI-H1623 NEfIVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrmR5JIUUN3ME2zNFQvODhibl2= M{nZT3NCVkeHUh?=
YH-13 NW\3fVBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfKUVdKSzVyPUOwOE4{OiCwTR?= NWDTSGVoW0GQR1XS
BPH-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPtU|ZUUUN3ME2zNVQhdk1? MYnTRW5ITVJ?
AN3-CA M{LQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXn2WVQ5UUN3ME2zOFAvOzdibl2= NI\xdWxUSU6JRWK=
ES7 M2i1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTN2MT65PUBvVQ>? NFv3cZhUSU6JRWK=
MDA-MB-175-VII MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C0fmlEPTB;M{WyMlkzKG6P M1e1ZXNCVkeHUh?=
GAMG MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTN5MD64OUBvVQ>? MV7TRW5ITVJ?
CHL-1 M3LyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN5OD62OUBvVQ>? MVPTRW5ITVJ?
NB7 M3iwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTHVFRKSzVyPUO4PU45OyCwTR?= M2\KXnNCVkeHUh?=
MFE-280 NUDJSllDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTRzOD6yJI5O NHv3TmZUSU6JRWK=
HL-60 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTDSJhKSzVyPUSyOU44PSCwTR?= MUTTRW5ITVJ?
GCIY NWL5R5c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mne0TWM2OD12M{OuPEBvVQ>? NULod3J6W0GQR1XS
MDA-MB-361 M1nMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvMbpVwUUN3ME20N|kvOTNibl2= NEjNfnlUSU6JRWK=
LXF-289 M4rnN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vzR2lEPTB;NES4MlI4KG6P M33LZXNCVkeHUh?=
NBsusSR NUDieIZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX0TJNKSzVyPUS4PE45PSCwTR?= MkjVV2FPT0WU
KU-19-19 Mn;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC4TWM2OD13MU[uNFchdk1? NY\GbVdpW0GQR1XS
A204 NITaRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPXTWM2OD13MkKuN|Mhdk1? NIDweGhUSU6JRWK=
LB1047-RCC NInqWHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXVU3hnUUN3ME21NlIvQTNibl2= NUnmWWVxW0GQR1XS
COLO-684 NVjNcFRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLlfopKSzVyPUWyN{4yOSCwTR?= NF\vZmVUSU6JRWK=
PA-1 NEDQVlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfsZWZKSzVyPUWzNk41OSCwTR?= MnuzV2FPT0WU
MG-63 NXrCSFlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTV2MT6xNUBvVQ>? NEDhWFBUSU6JRWK=
BHT-101 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfVZ5VKSzVyPUW0OE46PCCwTR?= MmDaV2FPT0WU
NKM-1 NHPheXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHRY9KSzVyPUW5N{4xQSCwTR?= MknhV2FPT0WU
T47D NGHlRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTiVVV{UUN3ME21PVcvPTZibl2= M2\nSHNCVkeHUh?=
MOLT-4 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTZ{Mz62NkBvVQ>? MnTtV2FPT0WU
IGROV-1 NHLLPJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{D1bGlEPTB;NkO0MlMyKG6P NUHEbYd[W0GQR1XS
ES4 M2S5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTZ|OT61OEBvVQ>? NWDQTHU4W0GQR1XS
HuO-3N1 NVrq[IlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPLUGdKSzVyPU[0Nk4{QCCwTR?= NWXmcFd{W0GQR1XS
NEC8 NUHadY94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4j5W2lEPTB;NkWzMlU4KG6P Mme5V2FPT0WU
HO-1-N-1 NIr6WnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL6WXNYUUN3ME22OVkvOTdibl2= MVnTRW5ITVJ?
EPCL-272H NVLEUYROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TF[GlEPTB;Nki3MlIyKG6P M{HPOnNCVkeHUh?=
D-263MG NEezZ3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTdzOD6xJI5O NY\KcnNwW0GQR1XS
MV-4-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfITWM2OD15MkSuN|Ehdk1? Mor5V2FPT0WU
SK-NEP-1 M2nCdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3RTWM2OD15MkWuPVQhdk1? Mn[xV2FPT0WU
SW872 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTd{Nz64PUBvVQ>? Mlz1V2FPT0WU
P30-OHK M1TPfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTd|MD63NUBvVQ>? NYPXT3l6W0GQR1XS
OMC-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLYTWM2OD15NUGuNFkhdk1? M2DDZXNCVkeHUh?=
LoVo NF7WUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH1TWM2OD15N{euPUBvVQ>? MmTmV2FPT0WU
LNCaP-Clone-FGC NEPhR4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTd7Nj6zOEBvVQ>? MnnCV2FPT0WU
L-363 NYHDO2htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfBS5FkUUN3ME23PVgvPDJibl2= MnfSV2FPT0WU
ES8 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\pTWM2OD16MUCuOVIhdk1? M4HN[nNCVkeHUh?=
697 NX7B[pVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLrS5p2UUN3ME24N|EvPTVibl2= MmPlV2FPT0WU
HSC-3 NInHNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTh|OT61OEBvVQ>? MX3TRW5ITVJ?
H4 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe5[|NKSzVyPUi1NE45PSCwTR?= NUjXTGtSW0GQR1XS
QIMR-WIL NEP1fFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M364dmlEPTB;OE[1MlIhdk1? MoXmV2FPT0WU
OAW-42 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H0b2lEPTB;OEeyMlE6KG6P MXLTRW5ITVJ?
MCF7 M36w[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\zTWM2OD16OUiuOVkhdk1? M{jUWnNCVkeHUh?=
SCC-25 NWTIRXR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTlzND6xPUBvVQ>? NVfmVYlkW0GQR1XS
NCI-H1563 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LDdGlEPTB;OUG1Mlk6KG6P Mn;nV2FPT0WU
OVCAR-5 NXGzT3k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTl2MD6xO{BvVQ>? NETKcHRUSU6JRWK=
HDLM-2 MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETRUI9KSzVyPUm0PU4zKG6P NFf3WpBUSU6JRWK=
NB5 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3JTWM2OD17NU[uOkBvVQ>? NYLGcoVJW0GQR1XS
NCI-H292 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTl5ND6zNkBvVQ>? MmnjV2FPT0WU
A101D NXn0U3ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXnVm9KSzVyPUm5NE4yQSCwTR?= NX32bGozW0GQR1XS
NCI-H1648 NEnaXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfkTWM2OD17OUiuOVEhdk1? NG\weI5USU6JRWK=
EKVX NH7zU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7DSVRKSzVyPUGuNFEzQSEQvF2= NEjXNpZUSU6JRWK=
SW1710 NFPxXotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fWWGlEPTB;MT6wOFI{OyEQvF2= NEG1R3FUSU6JRWK=
WM-115 NXzYNoU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\qVmlEPTB;MT6wOlY2PiEQvF2= NXe0d5FkW0GQR1XS
CAL-54 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETOZlRKSzVyPUGuNFcxQDFizszN MUnTRW5ITVJ?
TGBC24TKB NXK1WJpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS5TYhKSzVyPUGuNFgxPDVizszN NX24[21{W0GQR1XS
NCI-H520 M17iZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn1fVZ{UUN3ME2xMlA5QTZ5IN88US=> M3zuWXNCVkeHUh?=
D-423MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnDS3JlUUN3ME2xMlA6QTZ{IN88US=> NGe4SHdUSU6JRWK=
BFTC-905 NUntbGYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwMUO0OFkh|ryP MYPTRW5ITVJ?
HT M{Dl[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwMUO0O|gh|ryP NIjzRY9USU6JRWK=
CTB-1 NH7xUndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[2TWM2OD1zLkG0Nlk{KM7:TR?= MYLTRW5ITVJ?
Hs-578-T M2C4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPKWGcyUUN3ME2xMlE6PTZ3IN88US=> MV7TRW5ITVJ?
HuH-7 MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3CV4NKUUN3ME2xMlIxQTR7IN88US=> M3;1NXNCVkeHUh?=
LB996-RCC NImybnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7COWdZUUN3ME2xMlIzOTd5IN88US=> MWLTRW5ITVJ?
KYSE-270 NFnXU|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDWN45KSzVyPUGuNlk4OzRizszN M{PmNHNCVkeHUh?=
A4-Fuk M3;IbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33mcGlEPTB;MT6yPVk6OyEQvF2= NVXGTGpyW0GQR1XS
A498 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL1TWM2OD1zLkOwOFc1KM7:TR?= M{LRTHNCVkeHUh?=
SK-MEL-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonxTWM2OD1zLkOwOlc6KM7:TR?= M4fFN3NCVkeHUh?=
AU565 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTjU4JwUUN3ME2xMlMyQDZ|IN88US=> NGPKOo1USU6JRWK=
Saos-2 MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\BVYEzUUN3ME2xMlM{OjB3IN88US=> M2q2SHNCVkeHUh?=
A549 M{LZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkniTWM2OD1zLkO5PVch|ryP Mlm5V2FPT0WU
BFTC-909 NUCyZXN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\UPWlEPTB;MT60N|MxPSEQvF2= NH7CUmlUSU6JRWK=
MDA-MB-415 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHY[2tKSzVyPUGuOFg3QTJizszN NFK4UY9USU6JRWK=
639-V NHO4d5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjHTWM2OD1zLkWwNlQ2KM7:TR?= NFTBVm9USU6JRWK=
A704 M4GzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDUVWlKSzVyPUGuOVA4QDVizszN NIfxRYlUSU6JRWK=
PANC-03-27 NV;abHF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7WXmhKSzVyPUGuOVE1ODhizszN MnXlV2FPT0WU
SK-MEL-28 M2rkWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnSZodKSzVyPUGuOVYxQDVizszN MnLZV2FPT0WU
Ramos-2G6-4C10 NXzSN5BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzmUXRKSzVyPUGuOlA4PDZizszN Mn\TV2FPT0WU
HuP-T4 NUna[HpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLmOGNKSzVyPUGuOlA4PzhizszN M1LsfHNCVkeHUh?=
VA-ES-BJ NG\ifJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFwNkGyO{DPxE1? MnLoV2FPT0WU
EFM-19 NYfuZYJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjuTWtKSzVyPUGuOlE5OSEQvF2= NVPrTnVVW0GQR1XS
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SK-MES-1 NF60dFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHie4RKSzVyPUKuNFE{OzJizszN MXHTRW5ITVJ?
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LAMA-84 NH61WVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJwMEK2PFkh|ryP NHLjbXVUSU6JRWK=
CAL-39 M1HwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjtTlBKUUN3ME2yMlA{OjhizszN NVXSXFJoW0GQR1XS
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NH-12 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnLZVhKSzVyPUKuNFU1OjRizszN NH[wOYRUSU6JRWK=
NCI-H1048 NGeyV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV6wSGZiUUN3ME2yMlExPTJizszN MmPDV2FPT0WU
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EW-22 NYLFdIYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr5bmx1UUN3ME2yMlI2ODZ5IN88US=> NGHke3NUSU6JRWK=
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NCI-H1666 M2TLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LrfmlEPTB;Mj61NVExPCEQvF2= Mon1V2FPT0WU
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LCLC-97TM1 NYDCWoViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[x[ZRKSzVyPUKuOlkzPjdizszN MojHV2FPT0WU
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MDA-MB-157 NELHPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLHN3RUUUN3ME2yMlgzODJ|IN88US=> MX\TRW5ITVJ?
NB12 NVK1cXE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJwOES5NVQh|ryP M4[xfXNCVkeHUh?=
DMS-273 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XQNWlEPTB;Mj64OlQ4KM7:TR?= MXfTRW5ITVJ?
HCC70 NIHRSFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF2xXY1KSzVyPUKuPFY2QDlizszN NE\NXFNUSU6JRWK=
YKG-1 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG4TWM2OD1|LkCzO|g4KM7:TR?= M{XjNXNCVkeHUh?=
NCI-H28 M3z6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDrWGVQUUN3ME2zMlA2OjlzIN88US=> NH;sZWtUSU6JRWK=
HN MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmS2TWM2OD1|LkC2OlM3KM7:TR?= MlLFV2FPT0WU
HT-1080 MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1e4PGlEPTB;Mz6wPFYxPiEQvF2= M4jPTnNCVkeHUh?=
HPAF-II NWfycoFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfCW49ZUUN3ME2zMlExODZ6IN88US=> M3;hO3NCVkeHUh?=
U-2-OS MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi4TGhlUUN3ME2zMlE{Pzh{IN88US=> NYjj[ZM3W0GQR1XS
SNU-387 NEnNXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOwTWM2OD1|LkG2N|Y1KM7:TR?= MUXTRW5ITVJ?
Becker NIq0PG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrtTWM2OD1|LkG2PFA5KM7:TR?= M2TB[nNCVkeHUh?=
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HTC-C3 NIrFPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP6TWM2OD1|LkK5N|UzKM7:TR?= NUe5dIlYW0GQR1XS
M14 NIHTblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnkc3ZyUUN3ME2zMlMxPjZ|IN88US=> NVTvOJk5W0GQR1XS
COR-L23 NFLSSodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX6TWM2OD1|LkO3Nlc6KM7:TR?= MmLSV2FPT0WU
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Mewo NGTHcWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjBTJRwUUN3ME2zMlQzOTh{IN88US=> MWnTRW5ITVJ?
TE-8 MkT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqzTWM2OD1|LkS4NlU6KM7:TR?= M1XUe3NCVkeHUh?=
RPMI-2650 NXi3OI9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LJ[WlEPTB;Mz62NFY{PyEQvF2= NXXxRldFW0GQR1XS
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NCI-H747 MljQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf0U3B3UUN3ME20MlA2PjN6IN88US=> MYTTRW5ITVJ?
LN-405 NHrpOWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTRwMUW3Nlgh|ryP MWLTRW5ITVJ?
OVCAR-8 MkXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTRwMkK1OFMh|ryP M1;0bHNCVkeHUh?=
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CAL-12T M2\rRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzsdlRwUUN3ME20MlQyPDF|IN88US=> M1\acXNCVkeHUh?=
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NCI-H1355 NHr6SmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHXTWM2OD12LkW1NVQ3KM7:TR?= M1rGbXNCVkeHUh?=
RPMI-7951 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q1UWlEPTB;ND61O|AxOiEQvF2= NGPiTohUSU6JRWK=
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IA-LM M3\lb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OyVGlEPTB;ND65PVQ{PSEQvF2= M4e3NHNCVkeHUh?=
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RPMI-8226 NYrFOXN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW5WoVKSzVyPUWuNFU1PjFizszN NYTDcZI3W0GQR1XS
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CAL-62 M2\KVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTVwMUiyOVkh|ryP NIL3XlJUSU6JRWK=
NB10 M{PKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfCXVNKSzVyPUWuNlI4PDRizszN M1XDUnNCVkeHUh?=
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GR-ST NE\Ud5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHTUnNHUUN3ME21MlM5OzJ{IN88US=> NGj3VpNUSU6JRWK=
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NCI-H1092 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP0[3JKSzVyPUWuOFEyPDhizszN Mn22V2FPT0WU
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SW13 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ7Lki1NVkh|ryP M2XyV3NCVkeHUh?=
ES3 NHX0epZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPpd|ZKSzVyPUOwMlM4OzNizszN MVvTRW5ITVJ?
HCT-116 M2XHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTNyLkW1OVQh|ryP MkO0V2FPT0WU
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NCI-H2170 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTNzLkW3PFQh|ryP NX;uSmwzW0GQR1XS
ALL-PO MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHFTWM2OD1|MT64OFI5KM7:TR?= NUTVb3c{W0GQR1XS
NCI-H661 Ml\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7R[YVyUUN3ME2zNk4xPjJ|IN88US=> MWLTRW5ITVJ?
NCI-H2347 M{KxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPuZ4xbUUN3ME2zNk41QDN5IN88US=> NWXFdHdYW0GQR1XS
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YAPC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:5TWM2OD1|Mz64NVU6KM7:TR?= NI[2c5FUSU6JRWK=
LCLC-103H MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTN2LkG2NlQh|ryP MYjTRW5ITVJ?
SiHa MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXiSI86UUN3ME2zOE4{QDF5IN88US=> NG\mVnRUSU6JRWK=
LK-2 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jWOmlEPTB;M{SuOVcxQCEQvF2= NWO1SFU1W0GQR1XS
KP-N-YS NGC5XZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3KwNmlEPTB;M{SuO|IxOiEQvF2= NFLGbnhUSU6JRWK=
NCI-SNU-1 M1jtUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLnTWM2OD1|NT6xO|kh|ryP NFvrdFNUSU6JRWK=
KNS-81-FD M{HMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTuNpZFUUN3ME2zOU43PjNizszN MofRV2FPT0WU
SCC-9 NFXMdVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn0W3BKSzVyPUO2MlcyPDZizszN MkTLV2FPT0WU
SH-4 NYXEXmNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33mTWlEPTB;M{[uO|Mh|ryP NVjRR4tLW0GQR1XS
HCC-1954 NYL6SWlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[0[G43UUN3ME2zO{4zPzJ7IN88US=> NFHxUmpUSU6JRWK=
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BE-13 NUXRXW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHCPItUUUN3ME2zO{44ODF6IN88US=> M4qxXXNCVkeHUh?=
COLO-678 M2TsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPzTWM2OD1|Nz65OFM4KM7:TR?= NELvboFUSU6JRWK=
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OAW-28 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;RTWM2OD1|OD62N|kh|ryP NVG0Z4VRW0GQR1XS
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A3-KAW MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn1cnRlUUN3ME20NE4{PjZzIN88US=> NVjDd2FiW0GQR1XS
SK-MEL-24 NGL3cVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTRyLkW5N|Eh|ryP NFi5e|JUSU6JRWK=
KYSE-140 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTRyLkexOlUh|ryP M1vOTnNCVkeHUh?=
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NB14 Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjmbWhvUUN3ME20Nk44ODJ5IN88US=> MojNV2FPT0WU
COLO-792 MmPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTR{Lki5OlEh|ryP MoDtV2FPT0WU
RH-1 MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTR|LkS4N|Yh|ryP NYTqVHpNW0GQR1XS
NCI-H522 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7mc4p4UUN3ME20OE4{PTZ6IN88US=> M4m0e3NCVkeHUh?=
Ca-Ski NVm3[mZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInQ[3RKSzVyPUS0MlgyOTRizszN NYryVI5RW0GQR1XS
KGN NUjkcms2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nDOmlEPTB;NEiuN|A3OyEQvF2= M{\jTnNCVkeHUh?=
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NCI-H358 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr3[JZKSzVyPUS5MlMxOThizszN M4C2[3NCVkeHUh?=
LS-411N NY\FOG16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W2e2lEPTB;NEmuN|EyQCEQvF2= NW\s[nloW0GQR1XS
IST-MES1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUH4NHAyUUN3ME20PU42PjJ3IN88US=> M1vCWXNCVkeHUh?=

... Click to View More Cell Line Experimental Data
In vivo 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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O		 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
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:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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

The Serial Dilution Calculator 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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PI3K Signaling Pathway Map

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  • FDA-approved PI3K Inhibitor

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    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147) New

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317 New

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • LY294002

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.

  • Idelalisib (CAL-101, GS-1101)

    Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

  • Wortmannin

    Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

  • Dactolisib (BEZ235, NVP-BEZ235)

    Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

  • Buparlisib (BKM120, NVP-BKM120)

    Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

  • Alpelisib (BYL719)

    Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID