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 M{ntN2tqdmG|ZTDBd5NigQ>? NVjCeGE4OSCq MX;EUXNQ M2G1fmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= NGfaTZAyQDd3NE[1OC=>
Sf9 MVLLbY5ie2ViQYPzZZk> NILnW5EyKGh? NXTifHhuTE2VTx?= NVvoNo1LUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? M1\QdVE5PzV2NkW0
Sf9 M1LJcGtqdmG|ZTDBd5NigQ>? Mnf5NUBp NX3TOYhnTE2VTx?= M4P6VWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBGPTR3LVugcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> MnTjNVg4PTR4NUS=
Sf9 M4X3[2tqdmG|ZTDBd5NigQ>? NXvEfIVSOSCq MV;EUXNQ M4i0bmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wN|Mh|ryP M1jMclE5PzV2NkW0
Sf9 MoDVT4lv[XOnIFHzd4F6 MX[xJIg> NXPQZVF2TE2VTx?= NWj0e2MyUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[Q>? MUexPFc2PDZ3NB?=
MDA-MB-361 MX;GeY5kfGmxbjDBd5NigQ>? NE\NO2ozKGh? M2HJb2ROW09? MXHJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlAzQCEQvF2= M{XDXFE5PzV2NkW0
PC3 MVvGeY5kfGmxbjDBd5NigQ>? NYn6c4doOiCq NInVSHpFVVOR NVvyO4FRUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gVGM{KGOnbHzzJJdqfGhiSVO1NEBw\iByLkCzO{DPxE1? NHLkZlkyQDd3NE[1OC=>
U87MG MXfGeY5kfGmxbjDBd5NigQ>? MXiyJIg> Mn6zSG1UVw>? M2PDSGlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? NGLSRokyQDd3NE[1OC=>
MDA-MB-361 M4TxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TXV|k3KGh? NGLifYVFVVOR MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlczKM7:TR?= NEfISI8yQDd3NE[1OC=>
A2780 NHfnVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHmcGs6PiCq NF3Qc41FVVOR NITqWHRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= NGfTXnAyQDd3NE[1OC=>
PC3 NUe3VI9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvuV|ZoQTZiaB?= NHHjRYdFVVOR NEjxW|ZKSzVyPUCuNlgh|ryP M3v0WVE5PzV2NkW0
U87MG MnfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13wSFk3KGh? NYOydGJFTE2VTx?= M2TpRWlEPTB;MD65OUDPxE1? NHrWXncyQDd3NE[1OC=>
Sf9 NX\Bbmt7U2mwYYPlJGF{e2G7 MXezNEBucW5? NH[we2RFVVOR MUnJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiYX3veY51KG:oIFHUVEBkd26|dX3l[EB4cXSqIFnDOVAhd2ZiMD6wOFIh|ryP MmHtNlI2PDh|NEK=
RAW 264.7 M171dGtqdmG|ZTDBd5NigQ>? Mmf3PVAhdWmw NVfVXYh4TE2VTx?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlI6QCEQvF2= M37hfFIzPTR6M{Sy
Sf9 NGrz[mFMcW6jc3WgRZN{[Xl? NWSzWYdqOSCq NWjiZ|VwUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2KndHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPGPUBk\WyuczD3bZRpKEmFNUCgc4YhOC5yMUeg{txO Mk\yNlM2PDB4NEW=
Sf9 M1vqRWtqdmG|ZTDBd5NigQ>? NYX4[WRWOSCq M1TiNGlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= NH\4fHUzOzV2ME[0OS=>
Sf9 MXLLbY5ie2ViQYPzZZk> MkH4NUBp MonCTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4didW2jIHX4dJJme3OnZB?= M4D0fVI{PTRyNkS1
Sf9 NXzUXGVGU2mwYYPlJGF{e2G7 NXL3N3J6OSCq MoPWTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZB?= M4nLdFI{PTRyNkS1
SKOV3 NF;qXXBMcW6jc3WgRZN{[Xl? MV[xJO69VQ>? MXKxJIg> MX;EUXNQ MlroTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? NUXHSWM2OjN|NkCzOFg>
MCF7 NEe3cpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxJO69VQ>? Ml\3PVYhcA>? NXTQUFJXTE2VTx?= NUXrSZRQT0l3ME2wMlA4ODJizszN NXXudXVKOjN|NkCzOFg>
SKOV3 M33O[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPtWnlyOSEQvF2= M{D2SFk3KGh? NX65bVZjTE2VTx?= MoXJS2k2OD1yLkG0O|Yh|ryP MV[yN|M3ODN2OB?=
PC3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDxVFM4OiCq MYrEUXNQ MnW3TWM2OD1yLkK4JO69VQ>? NWjtbWgxOjF7OEG3NVQ>
MCF7.1 NID6TpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK2cm44OiCq MXjEUXNQ MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? MUKyNVk5OTdzNB?=
MCF7-neo/Her2 NYHENmlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rBclczKGh? NFW2WmdFVVOR NXnMPZNqUUN3ME2wMlI6KM7:TR?= MoLMNlM3PjJ7MEO=
MCF7-neo/Her2 M1K1[mtqdmG|ZTDBd5NigQ>? M4rkXGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> MW[yN|Y3OjlyMx?=
PC3 MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MomyO|IhcA>? MoP0SG1UVw>? NFnzdHJGSzVyPUCuN|Qh|ryP NEnNe5UzOTl6NU[zPS=>
MCF7.1 NGq5bZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe3NkBp MonzSG1UVw>? MnviRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? NWT1e5I1OjF7OEW2N|k>
PC3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL1OVJ[PzJiaB?= MVTEUXNQ MkLoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiZHXmbYNq\W62IHnuJHBVTU5id3n0bEBKSzVyIH;mJFAvOzlizszN M2DGS|IxODVyNk[5
MCF7.1 M2\KVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp MWnEUXNQ MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJHBKO0ujbIDoZUBufXSjboSge4l1cCCLQ{WwJI9nKDBwM{Sg{txO MmTtNlAxPTB4Nkm=
MCF7.1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVu3NkBp MnnPSWM2OD1yLkeyJO69VQ>? NEi5d2MzODN2Nk[1Oi=>
NCI-H1975 MVrDfZRwfG:6aXOgRZN{[Xl? M{O5cVczKGh? NGG2OpZKSzVyPUCuNlch|ryP MV6yN|A2QTV2NR?=
H460 MWLDfZRwfG:6aXOgRZN{[Xl? MUi3NkBp NFv3eZZKSzVyPUCuPFch|ryP NEL1cnczOzB3OUW0OS=>
HT-29 NXvNW3hWS3m2b4TvfIlkKEG|c3H5 MVu3NkBp NV\ZdFhJUUN3ME2wMlY3KM7:TR?= MoX1NlMxPTl3NEW=
HepG2 NXL0WWZzS3m2b4TvfIlkKEG|c3H5 M17kWVczKGh? NXzRXnp5UUN3ME2xJO69VQ>? Mmj4NlMxPTl3NEW=
SGC7901 M2\DcmN6fG:2b4jpZ{BCe3OjeR?= MX[3NkBp NIrQZ|ZKSzVyPUGuPEDPxE1? NVrXZXJROjNyNUm1OFU>
NCI-H226 NWPpSJpYS3m2b4TvfIlkKEG|c3H5 NH7ENFU4OiCq NFvtcGFKSzVyPUKuPUDPxE1? M1\Gb|I{ODV7NUS1
A549 MUPDfZRwfG:6aXOgRZN{[Xl? NFThVZo4OiCq M{W3d2lEPTB;Nj65JO69VQ>? MoPyNlMxPTl3NEW=
U87MG MWHDfZRwfG:6aXOgRZN{[Xl? NYPp[XRrPzJiaB?= M4rzU2lEPTB;Nz63O{DPxE1? MYWyN|A2QTV2NR?=
HBC4 NW\jPJZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\lWWZtd2eJSUWwQU03NjB|IF2= MlvPNlI{OzZ{NE[=
BSY1 M2XOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjsc4dIUTVyPT22MlkxKE1? MoLINlI{OzZ{NE[=
HBC5 NH;CSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnmOoNzdG:pR1m1NF0uPi54MDDN M{LEUVIzOzN4MkS2
MCF7 M4HwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnsc4dIUTVyPT23MlM{KE1? M1K0c|IzOzN4MkS2
MDA-MB-231 M4HHSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLsc4dIUTVyPT21MlQ3KE1? MWCyNlM{PjJ2Nh?=
U251 M{DiZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrSNoltd2eJSUWwQU02NjVyIF2= MV:yNlM{PjJ2Nh?=
SF268 NVjxbXV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3sc4dIUTVyPT21MlM6KE1? NXLsZZBwOjJ|M{[yOFY>
SF295 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;2d5Ntd2eJSUWwQU03NjN5IF2= M4LEOFIzOzN4MkS2
SF539 NXnkR4I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHlVXdtdG:pR1m1NF0uPi53MDDN NX\Bc2pMOjJ|M{[yOFY>
SNB75 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHOcI9oT0l3ME2tO{4yOCCP MX2yNlM{PjJ2Nh?=
SNB78 NUK3W2xRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3ocI9oT0l3ME2tOk42OiCP MlHuNlI{OzZ{NE[=
HCC2998 NXfYeoJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTLcGRtd2eJSUWwQU03NjJ7IF2= NH7ONIQzOjN|NkK0Oi=>
KM12 NE\UZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nNeoxw\0eLNUC9MVUvPzZiTR?= MYmyNlM{PjJ2Nh?=
HT-29 MoDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{P6d4xw\0eLNUC9MVYvOzBiTR?= MnHtNlI{OzZ{NE[=
HCT15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\MZpBNdG:pR1m1NF0uPi5zMjDN MWWyNlM{PjJ2Nh?=
HCT116 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTkOZl4dG:pR1m1NF0uPS56NzDN MkLVNlI{OzZ{NE[=
NCI-H23 NUDGfnFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHsc4dIUTVyPT21Mlc{KE1? M1vVfVIzOzN4MkS2
NCI-H226 M{j2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrsc4dIUTVyPT22MlIyKE1? MYeyNlM{PjJ2Nh?=
NCI-H522 MmTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P1coxw\0eLNUC9MVYvPThiTR?= M{nYZVIzOzN4MkS2
NCI-H483 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TLSoxw\0eLNUC9MVYvPTZiTR?= M17TeVIzOzN4MkS2
A549 M2izWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG3cI9oT0l3ME2tOk4yPSCP NVXjVphUOjJ|M{[yOFY>
DMS273 M2rDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvsc4dIUTVyPT22MlQ{KE1? MUWyNlM{PjJ2Nh?=
DMS114 NFjWTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnsc4dIUTVyPT21MlkzKE1? MoLiNlI{OzZ{NE[=
LOXIMVI M1\STWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;ZN2Ntd2eJSUWwQU03NjJ7IF2= MYiyNlM{PjJ2Nh?=
OVCAR3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK0bItpdG:pR1m1NF0uPi55MTDN NFTK[JIzOjN|NkK0Oi=>
OVCAR4 M1r5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K4Roxw\0eLNUC9MVUvPzZiTR?= M{e2UFIzOzN4MkS2
OVCAR5 MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvsc4dIUTVyPT22MlI3KE1? NUnX[GIxOjJ|M{[yOFY>
OVCAR8 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfRcI9oT0l3ME2tOU44OyCP NUfTVXpnOjJ|M{[yOFY>
SKOV3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrZcI9oT0l3ME2tOk42OiCP NID4PYczOjN|NkK0Oi=>
RXF631L M3XYOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDC[GVGdG:pR1m1NF0uPi56ODDN NF7LbYMzOjN|NkK0Oi=>
ACHN NE\YWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPwcI9oT0l3ME2tOk4xPyCP MUGyNlM{PjJ2Nh?=
St-4 NVHNXGJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37UN4xw\0eLNUC9MVUvPTZiTR?= M4C1[lIzOzN4MkS2
MKN1 NY\ONIRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLOcI9oT0l3ME2tO{4xQCCP MnPkNlI{OzZ{NE[=
MKN7 NG\LVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ZOYxw\0eLNUC9MVYvPTBiTR?= MkjXNlI{OzZ{NE[=
MKN28 NYHwfFJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37Oe4xw\0eLNUC9MVUvPTJiTR?= Moi2NlI{OzZ{NE[=
MKN45 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fSbIxw\0eLNUC9MVYvPTViTR?= M3zobVIzOzN4MkS2
MKN74 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfCTZdtd2eJSUWwQU03NjB{IF2= MmL6NlI{OzZ{NE[=
DU145 NYWzXJBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPsc4dIUTVyPT21Mlg2KE1? MV6yNlM{PjJ2Nh?=
PC3 NVrEXllzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSzbZptd2eJSUWwQU03NjZ4IF2= NGrkd5YzOjN|NkK0Oi=>
ES5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHRVotKSzVyPUWwMlIyKG6P NXPHWVJCW0GQR1XS
HH MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInTUHpKSzVyPUGxNU4xQCCwTR?= MlHJV2FPT0WU
MHH-PREB-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ybGlEPTB;MUG0MlMhdk1? Mly2V2FPT0WU
NCI-H1770 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF{Mz64OkBvVQ>? M4m0S3NCVkeHUh?=
HuO9 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofpTWM2OD1{ME[uNFIhdk1? MULTRW5ITVJ?
HAL-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Tyb2lEPTB;MkC2Mlc{KG6P MmiwV2FPT0WU
NOS-1 NF3UVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;RUng4UUN3ME2yNVEvQDJibl2= MWPTRW5ITVJ?
HGC-27 MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHJTWM2OD1{MUKuOVchdk1? NUHyVHpmW0GQR1XS
NB69 NFm3XYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHOz[VhKSzVyPUK0OU4zPyCwTR?= MojtV2FPT0WU
RS4-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzLVJRYUUN3ME2yOlEvPzZibl2= MlnzV2FPT0WU
DOK NED5eoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTNyMT63JI5O MY\TRW5ITVJ?
LB2241-RCC M2SxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\iTWM2OD1|MEOuPFQhdk1? MVLTRW5ITVJ?
NCI-H1623 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC3RXRKSzVyPUOwOE4xQCCwTR?= NIXiUIRUSU6JRWK=
YH-13 NEjadlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXGTWM2OD1|MESuN|Ihdk1? M4DnUHNCVkeHUh?=
BPH-1 NFPHOlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTNzNDDuUS=> MkTuV2FPT0WU
AN3-CA M2HCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i4dWlEPTB;M{SwMlM4KG6P MUPTRW5ITVJ?
ES7 NEDNNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTN2MT65PUBvVQ>? M2TlUnNCVkeHUh?=
MDA-MB-175-VII NFLvWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlH0TWM2OD1|NUKuPVIhdk1? NWrCNIhyW0GQR1XS
GAMG MlvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojXTWM2OD1|N{CuPFUhdk1? M4LwfXNCVkeHUh?=
CHL-1 M3TBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ixRmlEPTB;M{e4MlY2KG6P NIHsc5RUSU6JRWK=
NB7 NUnDRpYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTN6OT64N{BvVQ>? NEfWSFZUSU6JRWK=
MFE-280 M3zWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v1T2lEPTB;NEG4MlIhdk1? NFfFeFFUSU6JRWK=
HL-60 M1zjbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjtSI1KSzVyPUSyOU44PSCwTR?= MUPTRW5ITVJ?
GCIY Ml;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXwbHNOUUN3ME20N|MvQCCwTR?= MXXTRW5ITVJ?
MDA-MB-361 NEmxb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR|OT6xN{BvVQ>? NGPvb3NUSU6JRWK=
LXF-289 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR2OD6yO{BvVQ>? MVvTRW5ITVJ?
NBsusSR M2PJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvGW2J1UUN3ME20PFgvQDVibl2= NVTnfXRyW0GQR1XS
KU-19-19 M4HyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXTWM2OD13MU[uNFchdk1? MVrTRW5ITVJ?
A204 M4DhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTV{Mj6zN{BvVQ>? MXnTRW5ITVJ?
LB1047-RCC M2O3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KxXmlEPTB;NUKyMlk{KG6P MXzTRW5ITVJ?
COLO-684 NV7rfJp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPLWo9EUUN3ME21NlMvOTFibl2= M2TySHNCVkeHUh?=
PA-1 NGPLPZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXkeoZKSzVyPUWzNk41OSCwTR?= NF\3SYFUSU6JRWK=
MG-63 NF7tc2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\zW2ZFUUN3ME21OFEvOTFibl2= Mn3DV2FPT0WU
BHT-101 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rYbmlEPTB;NUS0Mlk1KG6P M3u2RXNCVkeHUh?=
NKM-1 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVThSnI2UUN3ME21PVMvODlibl2= NYfQR4VHW0GQR1XS
T47D NEnVR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TyV2lEPTB;NUm3MlU3KG6P MkLQV2FPT0WU
MOLT-4 M1[wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PsO2lEPTB;NkKzMlYzKG6P MXrTRW5ITVJ?
IGROV-1 NI\UcFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPITWM2OD14M{SuN|Ehdk1? NH\uS3JUSU6JRWK=
ES4 M3rDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEixdldKSzVyPU[zPU42PCCwTR?= M4j3dHNCVkeHUh?=
HuO-3N1 MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PheWlEPTB;NkSyMlM5KG6P M1LaNnNCVkeHUh?=
NEC8 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Xj[GlEPTB;NkWzMlU4KG6P MVXTRW5ITVJ?
HO-1-N-1 NYrPOpNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknCTWM2OD14NUmuNVchdk1? MoXGV2FPT0WU
EPCL-272H MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTZ6Nz6yNUBvVQ>? NFHVSW9USU6JRWK=
D-263MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37CWWlEPTB;N{G4MlEhdk1? MX7TRW5ITVJ?
MV-4-11 NFG4NWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTd{ND6zNUBvVQ>? MYHTRW5ITVJ?
SK-NEP-1 M2XSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED5TXJKSzVyPUeyOU46PCCwTR?= NIPnW3pUSU6JRWK=
SW872 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC2U2lHUUN3ME23NlcvQDlibl2= NFfyW2xUSU6JRWK=
P30-OHK NGP0OJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGr0VmNKSzVyPUezNE44OSCwTR?= NG\h[ZlUSU6JRWK=
OMC-1 NXPS[Y5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DxUWlEPTB;N{WxMlA6KG6P MYfTRW5ITVJ?
LoVo NVvRR|Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPjTWM2OD15N{euPUBvVQ>? MlrxV2FPT0WU
LNCaP-Clone-FGC MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{O0RWlEPTB;N{m2MlM1KG6P MXfTRW5ITVJ?
L-363 NVi1RoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfkTWM2OD15OUiuOFIhdk1? MnHYV2FPT0WU
ES8 NXu3U3pxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRThzMD61NkBvVQ>? Mme5V2FPT0WU
697 NYnrcHFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP1cWFKSzVyPUizNU42PSCwTR?= NFHQc|VUSU6JRWK=
HSC-3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTh|OT61OEBvVQ>? MmrBV2FPT0WU
H4 NIPXPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PoVGlEPTB;OEWwMlg2KG6P NGLReZFUSU6JRWK=
QIMR-WIL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXvTWM2OD16NkWuNkBvVQ>? NHTzXIpUSU6JRWK=
OAW-42 NE\yelJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XPTGlEPTB;OEeyMlE6KG6P NWHnRpVjW0GQR1XS
MCF7 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PEe2lEPTB;OEm4MlU6KG6P NFP0[5pUSU6JRWK=
SCC-25 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLMTWM2OD17MUSuNVkhdk1? NGrYfYFUSU6JRWK=
NCI-H1563 NHK1RotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTlzNT65PUBvVQ>? M4\ZPXNCVkeHUh?=
OVCAR-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES3RYVKSzVyPUm0NE4yPyCwTR?= MYLTRW5ITVJ?
HDLM-2 MnH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fUVmlEPTB;OUS5MlIhdk1? MVLTRW5ITVJ?
NB5 NYLUNFU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O3cGlEPTB;OUW2MlYhdk1? NIm2dYVUSU6JRWK=
NCI-H292 M1PUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTl5ND6zNkBvVQ>? NW\w[nJvW0GQR1XS
A101D M2jxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTl7MD6xPUBvVQ>? M{jBe3NCVkeHUh?=
NCI-H1648 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[wc|hKSzVyPUm5PE42OSCwTR?= NIDQVYtUSU6JRWK=
EKVX MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMEGyPUDPxE1? M{SwOXNCVkeHUh?=
SW1710 M1THXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwMESyN|Mh|ryP Mnz1V2FPT0WU
WM-115 M3rkcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTFwME[2OVYh|ryP M{faTHNCVkeHUh?=
CAL-54 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PicmlEPTB;MT6wO|A5OSEQvF2= NU\mUHViW0GQR1XS
TGBC24TKB NY\6c5VMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe2Z4JKSzVyPUGuNFgxPDVizszN MXPTRW5ITVJ?
NCI-H520 MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDVZ|M1UUN3ME2xMlA5QTZ5IN88US=> NX\EcHFYW0GQR1XS
D-423MG NWPrcnRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnywTWM2OD1zLkC5PVYzKM7:TR?= NUD1eVd1W0GQR1XS
BFTC-905 M{TXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTFwMUO0OFkh|ryP MnzMV2FPT0WU
HT MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwMUO0O|gh|ryP NHPWS|dUSU6JRWK=
CTB-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPnTWM2OD1zLkG0Nlk{KM7:TR?= MYfTRW5ITVJ?
Hs-578-T M3G4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTCWWFJUUN3ME2xMlE6PTZ3IN88US=> NVPGO4hnW0GQR1XS
HuH-7 M2[2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFwMkC5OFkh|ryP M{PZdXNCVkeHUh?=
LB996-RCC NIXhbHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXn5UodUUUN3ME2xMlIzOTd5IN88US=> MWTTRW5ITVJ?
KYSE-270 MnnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPhTWM2OD1zLkK5O|M1KM7:TR?= MV\TRW5ITVJ?
A4-Fuk MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrpSmxKSzVyPUGuNlk6QTNizszN NHP5WItUSU6JRWK=
A498 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DCSmlEPTB;MT6zNFQ4PCEQvF2= MXHTRW5ITVJ?
SK-MEL-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjZOGtxUUN3ME2xMlMxPjd7IN88US=> M2jJUnNCVkeHUh?=
AU565 NVz5V|lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzS[25iUUN3ME2xMlMyQDZ|IN88US=> NUDyUFRqW0GQR1XS
Saos-2 NVLqPWxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFwM{OyNFUh|ryP Mn\wV2FPT0WU
A549 NF7U[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFwM{m5O{DPxE1? M{Pme3NCVkeHUh?=
BFTC-909 NV3ndIFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7D[XVKSzVyPUGuOFM{ODVizszN Mmn2V2FPT0WU
MDA-MB-415 NUD4PWY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTSPZhTUUN3ME2xMlQ5Pjl{IN88US=> M2HMNnNCVkeHUh?=
639-V M1mwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXzTWM2OD1zLkWwNlQ2KM7:TR?= NULmRm52W0GQR1XS
A704 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFwNUC3PFUh|ryP M{m0VHNCVkeHUh?=
PANC-03-27 M4i4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLETWM2OD1zLkWxOFA5KM7:TR?= Mm\rV2FPT0WU
SK-MEL-28 MoLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwNU[wPFUh|ryP NHL1RYhUSU6JRWK=
Ramos-2G6-4C10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vTPWlEPTB;MT62NFc1PiEQvF2= NFPpWpVUSU6JRWK=
HuP-T4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLG[W5YUUN3ME2xMlYxPzd6IN88US=> M1e4e3NCVkeHUh?=
VA-ES-BJ NV20U5h{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHnU5FvUUN3ME2xMlYyOjdizszN MnjUV2FPT0WU
EFM-19 MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvnOYdKSzVyPUGuOlE5OSEQvF2= MYrTRW5ITVJ?
G-401 NGHSWXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjFcWNKSzVyPUGuOlIyPjRizszN NUPjOoxQW0GQR1XS
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NB14 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTR{LkewNlch|ryP M4P6WXNCVkeHUh?=
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UACC-62 NFzF[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP3TWM2OD12OD60NFczKM7:TR?= MWnTRW5ITVJ?
NCI-H358 NGn6NIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTR7LkOwNVgh|ryP MlT5V2FPT0WU
LS-411N Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrPTWM2OD12OT6zNVE5KM7:TR?= NUnxd3Z4W0GQR1XS
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... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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:

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

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Clinical Trial Information

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

Tech Support

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

Handling Instructions

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID