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 NIC0dWFMcW6jc3WgRZN{[Xl? NVTCO|hCOSCq MWjEUXNQ MlLYTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCmZXz0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wNFMh|ryP NFLqOIkyQDd3NE[1OC=>
Sf9 NWPYOHhvU2mwYYPlJGF{e2G7 MkHxNUBp M2PCbmROW09? NVq4T2c2UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? M3f3[FE5PzV2NkW0
Sf9 MWLLbY5ie2ViQYPzZZk> NEDqN2MyKGh? MlXZSG1UVw>? MlzLTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NXraNlFZOTh5NUS2OVQ>
Sf9 MVLLbY5ie2ViQYPzZZk> MUCxJIg> MVfEUXNQ NGrofY5KdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFM{KM7:TR?= MljGNVg4PTR4NUS=
Sf9 NXrmZZhDU2mwYYPlJGF{e2G7 M{CxO|EhcA>? MkHVSG1UVw>? M3X4TGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> Mo[5NVg4PTR4NUS=
MDA-MB-361 MVLGeY5kfGmxbjDBd5NigQ>? MUiyJIg> M4fUdWROW09? MlnQTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPRFGtUWIuOzZzIHPlcIx{KHerdHigVGlMO0ODIFW1OFUuUyCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4xOjhizszN NGqwbJIyQDd3NE[1OC=>
PC3 NXLLNGJCTnWwY4Tpc44hSXO|YYm= NFzWSJQzKGh? MVrEUXNQ Mki4TY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kAxNjB|NzFOwG0> NFW2TJUyQDd3NE[1OC=>
U87MG NVTaOmJkTnWwY4Tpc44hSXO|YYm= MUKyJIg> MVjEUXNQ MXXJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yNE[g{txO M4HRRVE5PzV2NkW0
MDA-MB-361 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK1PVYhcA>? NWLM[JpTTE2VTx?= M4TEW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvPzJizszN NXXncnRsOTh5NUS2OVQ>
A2780 M4nESGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojZPVYhcA>? NYey[|VYTE2VTx?= M{nF[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCSSVuzR2Eh[W6mIGDUSW4hdXW2YYTpc44hf2m2aDDJR|UxKG:oIECuNVQh|ryP M2HTOlE5PzV2NkW0
PC3 MorjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT2Z406PiCq MlLzSG1UVw>? M2PEPGlEPTB;MD6yPEDPxE1? M4DiTFE5PzV2NkW0
U87MG M1OxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnYPVYhcA>? MnrCSG1UVw>? NIXWcHBKSzVyPUCuPVUh|ryP NH\nUHQyQDd3NE[1OC=>
Sf9 MoHOT4lv[XOnIFHzd4F6 NWT0WZpxOzBibXnu NVrwNlM2TE2VTx?= NIDNNlBKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgZY1wfW62IH;mJGFVWCClb37zeY1m\CC5aYToJGlEPTBib3[gNE4xPDJizszN MmDONlI2PDh|NEK=
RAW 264.7 MV;LbY5ie2ViQYPzZZk> NVv2XW9qQTBibXnu NULHSW5XTE2VTx?= NFjjboFKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> MlnRNlI2PDh|NEK=
Sf9 NF;Yb5VMcW6jc3WgRZN{[Xl? MWOxJIg> NIDXfndKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> M{TFeFI{PTRyNkS1
Sf9 M{GzeGtqdmG|ZTDBd5NigQ>? NIG5S2YyKGh? MnLxTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= MXiyN|U1ODZ2NR?=
Sf9 M2ThfWtqdmG|ZTDBd5NigQ>? NYqxe45zOSCq M3vXV2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= M2PFRlI{PTRyNkS1
Sf9 MUfLbY5ie2ViQYPzZZk> MoL1NUBp NGfXVnJKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[WyyaHGg[ZhxemW|c3Xk NGr3b20zOzV2ME[0OS=>
SKOV3 MojBT4lv[XOnIFHzd4F6 NELLXpIyKM7:TR?= NEDxXYMyKGh? NUDLW2tbTE2VTx?= M{nHR2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25? MWmyN|M3ODN2OB?=
MCF7 NU[1fnhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj0SJo1OSEQvF2= Ml74PVYhcA>? MUTEUXNQ MmSzS2k2OD1yLkC3NFIh|ryP MoLrNlM{PjB|NEi=
SKOV3 M2SxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnjdJBnOSEQvF2= M1K0[lk3KGh? NX\xc4hGTE2VTx?= MnTUS2k2OD1yLkG0O|Yh|ryP MmXzNlM{PjB|NEi=
PC3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPYe244OiCq M1PRU2ROW09? NEDoVVFKSzVyPUCuNlgh|ryP NV;FSppqOjF7OEG3NVQ>
MCF7.1 NXL0PFRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW2O|IhcA>? M2fpbWROW09? M1rLd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochUEWUMjDn[Y5mKHerdHigTWM2OCCxZjCwMlI5KM7:TR?= NHXUbnozOTl6MUexOC=>
MCF7-neo/Her2 NF\C[ndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L0eVczKGh? MorpSG1UVw>? NYnVWXA{UUN3ME2wMlI6KM7:TR?= MkDQNlM3PjJ7MEO=
MCF7-neo/Her2 NGfTc|BMcW6jc3WgRZN{[Xl? NUHz[oUyUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO Mn7uNlM3PjJ7MEO=
PC3 Mm[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[3O|IhcA>? MoSxSG1UVw>? M2Xqe2VEPTB;MD6zOEDPxE1? MUKyNVk5PTZ|OR?=
MCF7.1 M2XqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[zPXU4OiCq NVzXdWlETE2VTx?= Mlj0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? M4Tx[lIyQTh3NkO5
PC3 NGSwW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP4XHE4OiCq NHrscW9FVVOR MoXsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiZHXmbYNq\W62IHnuJHBVTU5id3n0bEBKSzVyIH;mJFAvOzlizszN MXSyNFA2ODZ4OR?=
MCF7.1 Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEeweFY4OiCq NYrPcW5NTE2VTx?= MlPjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? NUXFeHVrOjByNUC2Olk>
MCF7.1 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYG3NkBp MXfFR|UxRTBwN{Kg{txO M2jTWFIxOzR4NkW2
NCI-H1975 MnPER5l1d3SxeHnjJGF{e2G7 NVjTU41sPzJiaB?= MkLITWM2OD1yLkK3JO69VQ>? NWn5bWp2OjNyNUm1OFU>
H460 MUPDfZRwfG:6aXOgRZN{[Xl? NIizOYQ4OiCq M2TNfWlEPTB;MD64O{DPxE1? MYWyN|A2QTV2NR?=
HT-29 M4H3bGN6fG:2b4jpZ{BCe3OjeR?= Mnv6O|IhcA>? MW\JR|UxRTBwNk[g{txO NWnxd3VvOjNyNUm1OFU>
HepG2 M17oZWN6fG:2b4jpZ{BCe3OjeR?= M1ruPFczKGh? NVi1Wo5iUUN3ME2xJO69VQ>? M4WyVlI{ODV7NUS1
SGC7901 NILTcGREgXSxdH;4bYMhSXO|YYm= M1n1cVczKGh? NIS0WZFKSzVyPUGuPEDPxE1? NYHyVJFYOjNyNUm1OFU>
NCI-H226 M3POcGN6fG:2b4jpZ{BCe3OjeR?= M3HEOFczKGh? MUHJR|UxRTJwOTFOwG0> NYK0dpRVOjNyNUm1OFU>
A549 MWLDfZRwfG:6aXOgRZN{[Xl? M1PKblczKGh? NWHESJRYUUN3ME22Mlkh|ryP NWfFSHB[OjNyNUm1OFU>
U87MG NEPhNpNEgXSxdH;4bYMhSXO|YYm= NFLEVo44OiCq Mn\GTWM2OD15Lke3JO69VQ>? NFjPcIczOzB3OUW0OS=>
HBC4 NGXDTFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHiXoRXdG:pR1m1NF0uPi5yMzDN NXHCcVdQOjJ|M{[yOFY>
BSY1 M4PLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfLb5hPdG:pR1m1NF0uPi57MDDN M2PVS|IzOzN4MkS2
HBC5 NY\1SGJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rUdIxw\0eLNUC9MVYvPjBiTR?= MkTRNlI{OzZ{NE[=
MCF7 NVPOcotTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUmzVJRIdG:pR1m1NF0uPy5|MzDN NYPZXW9vOjJ|M{[yOFY>
MDA-MB-231 NX3KOZN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TxZYxw\0eLNUC9MVUvPDZiTR?= NFW3UoIzOjN|NkK0Oi=>
U251 NF\mWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP2d3p3dG:pR1m1NF0uPS53MDDN NXHo[Hk3OjJ|M{[yOFY>
SF268 M2q1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\TcI9oT0l3ME2tOU4{QSCP M4foSVIzOzN4MkS2
SF295 M1jmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HxSIxw\0eLNUC9MVYvOzdiTR?= MYOyNlM{PjJ2Nh?=
SF539 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fLWoxw\0eLNUC9MVYvPTBiTR?= MWKyNlM{PjJ2Nh?=
SNB75 NVnueXhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3uzZ4xw\0eLNUC9MVcvOTBiTR?= MUmyNlM{PjJ2Nh?=
SNB78 NXfvc4s3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrp[oN4dG:pR1m1NF0uPi53MjDN NHvYc3UzOjN|NkK0Oi=>
HCC2998 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3FeFVtd2eJSUWwQU03NjJ7IF2= NEiwepQzOjN|NkK0Oi=>
KM12 NXzi[4FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\WTIxw\0eLNUC9MVUvPzZiTR?= MoO2NlI{OzZ{NE[=
HT-29 MlnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTLcI9oT0l3ME2tOk4{OCCP NHTLToczOjN|NkK0Oi=>
HCT15 NUW2[YFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTjXXNtd2eJSUWwQU03NjF{IF2= NEPzRo4zOjN|NkK0Oi=>
HCT116 NEO0OW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnWbJVtd2eJSUWwQU02Njh5IF2= MUmyNlM{PjJ2Nh?=
NCI-H23 NUfNZXZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfTcI9oT0l3ME2tOU44OyCP NXW1cWZLOjJ|M{[yOFY>
NCI-H226 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nMNIxw\0eLNUC9MVYvOjFiTR?= NX3XTJhoOjJ|M{[yOFY>
NCI-H522 NGrJS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX5cI9oT0l3ME2tOk42QCCP NV7CSYtuOjJ|M{[yOFY>
NCI-H483 MmDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXsc4dIUTVyPT22MlU3KE1? MUWyNlM{PjJ2Nh?=
A549 NEP4c5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7kO3hCdG:pR1m1NF0uPi5zNTDN M4j1OFIzOzN4MkS2
DMS273 MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLsc4dIUTVyPT22MlQ{KE1? M3fYelIzOzN4MkS2
DMS114 NVThbW5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O3NYxw\0eLNUC9MVUvQTJiTR?= MUiyNlM{PjJ2Nh?=
LOXIMVI NIP6SJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHRcI9oT0l3ME2tOk4zQSCP MlnFNlI{OzZ{NE[=
OVCAR3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPsc4dIUTVyPT22MlcyKE1? M3jueFIzOzN4MkS2
OVCAR4 NVvpcIFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfOeYtxdG:pR1m1NF0uPS55NjDN M3HtR|IzOzN4MkS2
OVCAR5 NYHRUJBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLjUIxmdG:pR1m1NF0uPi5{NjDN MYOyNlM{PjJ2Nh?=
OVCAR8 NEjzNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHYcI9oT0l3ME2tOU44OyCP MViyNlM{PjJ2Nh?=
SKOV3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfsc4dIUTVyPT22MlUzKE1? NHPZbpczOjN|NkK0Oi=>
RXF631L MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HVbIxw\0eLNUC9MVYvQDhiTR?= MlzDNlI{OzZ{NE[=
ACHN M{P0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\H[VNEdG:pR1m1NF0uPi5yNzDN M2XFSVIzOzN4MkS2
St-4 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnacI9oT0l3ME2tOU42PiCP M2fudlIzOzN4MkS2
MKN1 NX61N5VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3IcI9oT0l3ME2tO{4xQCCP Mn35NlI{OzZ{NE[=
MKN7 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Taeoxw\0eLNUC9MVYvPTBiTR?= NFrnS4QzOjN|NkK0Oi=>
MKN28 NYnTdnlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTsc4dIUTVyPT21MlUzKE1? M1;j[VIzOzN4MkS2
MKN45 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknEcI9oT0l3ME2tOk42PSCP NFr6UnozOjN|NkK0Oi=>
MKN74 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\sc4dIUTVyPT22MlAzKE1? NETxS2YzOjN|NkK0Oi=>
DU145 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz0UIptd2eJSUWwQU02Njh3IF2= MX:yNlM{PjJ2Nh?=
PC3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrVd|B[dG:pR1m1NF0uPi54NjDN NYjjVZdzOjJ|M{[yOFY>
ES5 NI\YWllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\OS2FKSzVyPUWwMlIyKG6P MnTLV2FPT0WU
HH MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnwWWJKSzVyPUGxNU4xQCCwTR?= MljnV2FPT0WU
MHH-PREB-1 M1TOPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W4UWlEPTB;MUG0MlMhdk1? NXXFZnZMW0GQR1XS
NCI-H1770 NHfaOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDUR2g5UUN3ME2xNlMvQDZibl2= Ml3mV2FPT0WU
HuO9 M1K1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJyNj6wNkBvVQ>? NXX2NFVQW0GQR1XS
HAL-01 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W3RmlEPTB;MkC2Mlc{KG6P M{nsN3NCVkeHUh?=
NOS-1 M{PFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJzMT64NkBvVQ>? M{TVVnNCVkeHUh?=
HGC-27 NIXl[FNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S1NWlEPTB;MkGyMlU4KG6P Mnm1V2FPT0WU
NB69 NX3kbXB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm4TWM2OD1{NEWuNlchdk1? MmrnV2FPT0WU
RS4-11 MlvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ4MT63OkBvVQ>? MljWV2FPT0WU
DOK M17x[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTTd2M1UUN3ME2zNFEvPyCwTR?= NYe4c4dHW0GQR1XS
LB2241-RCC NG\3SIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;LcHdsUUN3ME2zNFMvQDRibl2= MljIV2FPT0WU
NCI-H1623 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoftTWM2OD1|MESuNFghdk1? M2DtZ3NCVkeHUh?=
YH-13 NH72eYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;2TWM2OD1|MESuN|Ihdk1? NGW2e|NUSU6JRWK=
BPH-1 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTNzNDDuUS=> NV:weJRXW0GQR1XS
AN3-CA NXPVVGZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN2MD6zO{BvVQ>? MnfkV2FPT0WU
ES7 NYqweHFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPOTWM2OD1|NEGuPVkhdk1? M3HL[XNCVkeHUh?=
MDA-MB-175-VII MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTN3Mj65NkBvVQ>? NF\uWYhUSU6JRWK=
GAMG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;tN2lEPTB;M{ewMlg2KG6P MoS1V2FPT0WU
CHL-1 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTSPYRKSzVyPUO3PE43PSCwTR?= NHPPbHRUSU6JRWK=
NB7 M3SzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;McWlEPTB;M{i5Mlg{KG6P M3PKSXNCVkeHUh?=
MFE-280 NVm5Rnl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX0V2ZKSzVyPUSxPE4zKG6P MWrTRW5ITVJ?
HL-60 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPnO5JKSzVyPUSyOU44PSCwTR?= M375XnNCVkeHUh?=
GCIY NFL2UYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\ONGN7UUN3ME20N|MvQCCwTR?= M333NXNCVkeHUh?=
MDA-MB-361 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv3TWM2OD12M{muNVMhdk1? M13HWXNCVkeHUh?=
LXF-289 NVP3XYozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHxTWM2OD12NEiuNlchdk1? M2ju[3NCVkeHUh?=
NBsusSR MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjZTWM2OD12OEiuPFUhdk1? NXXiRVVsW0GQR1XS
KU-19-19 NHG2b4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDke5pwUUN3ME21NVYvODdibl2= M1fJPXNCVkeHUh?=
A204 MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jRV2lEPTB;NUKyMlM{KG6P M3H1WnNCVkeHUh?=
LB1047-RCC NGqwVnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTV{Mj65N{BvVQ>? NVPEVWtjW0GQR1XS
COLO-684 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTV{Mz6xNUBvVQ>? M3qwWnNCVkeHUh?=
PA-1 M2P3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTV|Mj60NUBvVQ>? NV7zdWdFW0GQR1XS
MG-63 NWfKOHJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTV2MT6xNUBvVQ>? Mn[4V2FPT0WU
BHT-101 NYDLc5JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTV2ND65OEBvVQ>? Mm\YV2FPT0WU
NKM-1 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Xxe2lEPTB;NUmzMlA6KG6P NHq2[YtUSU6JRWK=
T47D NHTpe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\6bVBwUUN3ME21PVcvPTZibl2= MWDTRW5ITVJ?
MOLT-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i5[WlEPTB;NkKzMlYzKG6P MlTLV2FPT0WU
IGROV-1 NXnoW5FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7CTWM2OD14M{SuN|Ehdk1? NVfkdFNYW0GQR1XS
ES4 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrmTWM2OD14M{muOVQhdk1? MkXsV2FPT0WU
HuO-3N1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjhTWM2OD14NEKuN|ghdk1? NXPaNWFqW0GQR1XS
NEC8 NEnaWVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTZ3Mz61O{BvVQ>? MnvXV2FPT0WU
HO-1-N-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTEeJRKSzVyPU[1PU4yPyCwTR?= NUHnO4FQW0GQR1XS
EPCL-272H MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojCTWM2OD14OEeuNlEhdk1? MXnTRW5ITVJ?
D-263MG M1\iVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX3WFVbUUN3ME23NVgvOSCwTR?= NGHjbYJUSU6JRWK=
MV-4-11 NWH1NJY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTd{ND6zNUBvVQ>? Ml;4V2FPT0WU
SK-NEP-1 NWPaeYI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7NTWM2OD15MkWuPVQhdk1? MY\TRW5ITVJ?
SW872 NX35N2VPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTd{Nz64PUBvVQ>? NUnCNotkW0GQR1XS
P30-OHK MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33PemlEPTB;N{OwMlcyKG6P Mn3jV2FPT0WU
OMC-1 NViyclZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYOxdXlPUUN3ME23OVEvODlibl2= MkPIV2FPT0WU
LoVo MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7XOVJKSzVyPUe3O{46KG6P M4L0WnNCVkeHUh?=
LNCaP-Clone-FGC NEHaXGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTd7Nj6zOEBvVQ>? M2n6fHNCVkeHUh?=
L-363 MnnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmwN48xUUN3ME23PVgvPDJibl2= MmqwV2FPT0WU
ES8 NVfYTJRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrOTWM2OD16MUCuOVIhdk1? M320T3NCVkeHUh?=
697 NUK4eFFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTh|MT61OUBvVQ>? NVzreXk4W0GQR1XS
HSC-3 MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nMfGlEPTB;OEO5MlU1KG6P MnXiV2FPT0WU
H4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q4UWlEPTB;OEWwMlg2KG6P M{H5THNCVkeHUh?=
QIMR-WIL MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X3[GlEPTB;OE[1MlIhdk1? MmfxV2FPT0WU
OAW-42 NYrvPXU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\SbmlEPTB;OEeyMlE6KG6P NG\WNXNUSU6JRWK=
MCF7 MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHvNIVUUUN3ME24PVgvPTlibl2= NVvZNodXW0GQR1XS
SCC-25 NGm2V2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;hNmlEPTB;OUG0MlE6KG6P Mle2V2FPT0WU
NCI-H1563 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;4TWM2OD17MUWuPVkhdk1? MYnTRW5ITVJ?
OVCAR-5 M2\vZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\zTWM2OD17NECuNVchdk1? MUDTRW5ITVJ?
HDLM-2 NX\yRXZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXhe4M5UUN3ME25OFkvOiCwTR?= M1PVfnNCVkeHUh?=
NB5 NGDnTWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13XfWlEPTB;OUW2MlYhdk1? MlTHV2FPT0WU
NCI-H292 NG\PbGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7GbFVUUUN3ME25O|QvOzJibl2= NFrGSnBUSU6JRWK=
A101D NXXyfZRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTl7MD6xPUBvVQ>? NFXmV2dUSU6JRWK=
NCI-H1648 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTl7OD61NUBvVQ>? NXPOPZpQW0GQR1XS
EKVX M3PqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfJSFJPUUN3ME2xMlAyOjlizszN NUTmfJpmW0GQR1XS
SW1710 MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr6[Y1uUUN3ME2xMlA1OjN|IN88US=> NIPyfnBUSU6JRWK=
WM-115 NUXicVNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;Nd2lEPTB;MT6wOlY2PiEQvF2= MX;TRW5ITVJ?
CAL-54 NHzXZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXVTWM2OD1zLkC3NFgyKM7:TR?= M3jmRnNCVkeHUh?=
TGBC24TKB NHXzXWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPNRphKSzVyPUGuNFgxPDVizszN MY\TRW5ITVJ?
NCI-H520 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7BOmhsUUN3ME2xMlA5QTZ5IN88US=> NYT4ToJFW0GQR1XS
D-423MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P0[2lEPTB;MT6wPVk3OiEQvF2= MoGxV2FPT0WU
BFTC-905 NIHOTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHRO5VKSzVyPUGuNVM1PDlizszN NH;4TnlUSU6JRWK=
HT MnP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwMUO0O|gh|ryP MX\TRW5ITVJ?
CTB-1 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwMUSyPVMh|ryP MYDTRW5ITVJ?
Hs-578-T M4LLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwMUm1OlUh|ryP MonGV2FPT0WU
HuH-7 NE\CNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfYTWM2OD1zLkKwPVQ6KM7:TR?= NGSyPYNUSU6JRWK=
LB996-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKzWY1GUUN3ME2xMlIzOTd5IN88US=> NInTXIhUSU6JRWK=
KYSE-270 NH3lRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrlTWM2OD1zLkK5O|M1KM7:TR?= NI\rOFVUSU6JRWK=
A4-Fuk M4myOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP0TWM2OD1zLkK5PVk{KM7:TR?= MV;TRW5ITVJ?
A498 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;XWGNKSzVyPUGuN|A1PzRizszN MnvVV2FPT0WU
SK-MEL-1 NVnlc5lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPLVHZ7UUN3ME2xMlMxPjd7IN88US=> NYfHV3FyW0GQR1XS
AU565 MnfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFwM{G4OlMh|ryP MUTTRW5ITVJ?
Saos-2 NED6RWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjr[W5KSzVyPUGuN|MzODVizszN MljwV2FPT0WU
A549 NGLCd2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnHboVKSzVyPUGuN|k6PyEQvF2= MnH1V2FPT0WU
BFTC-909 M2PlT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXjTWM2OD1zLkSzN|A2KM7:TR?= M2r6cXNCVkeHUh?=
MDA-MB-415 NWnpU28{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHGTWM2OD1zLkS4OlkzKM7:TR?= Ml63V2FPT0WU
639-V NWLsVGJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLiSVVKSzVyPUGuOVAzPDVizszN MWPTRW5ITVJ?
A704 M4DVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXaW241UUN3ME2xMlUxPzh3IN88US=> MXnTRW5ITVJ?
PANC-03-27 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf6TWM2OD1zLkWxOFA5KM7:TR?= NH7YZVNUSU6JRWK=
SK-MEL-28 M1fTc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvUVoxLUUN3ME2xMlU3ODh3IN88US=> NVvlfoZyW0GQR1XS
Ramos-2G6-4C10 M2ewNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvoWIdiUUN3ME2xMlYxPzR4IN88US=> NYrndnEzW0GQR1XS
HuP-T4 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7aWYdbUUN3ME2xMlYxPzd6IN88US=> M{TOfHNCVkeHUh?=
VA-ES-BJ MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwNkGyO{DPxE1? MoTkV2FPT0WU
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RKO NHzXeWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\sTWM2OD1{Nj63OlMzKM7:TR?= Mke1V2FPT0WU
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CAL-120 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL4TWM2OD1{Nz62PVE1KM7:TR?= NYTIPGJJW0GQR1XS
NCI-H2452 MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP0SFJKSzVyPUK3Mlc4OTZizszN NWLxT2Y5W0GQR1XS
NCI-H1395 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJ5Lke4N|Mh|ryP NXf1Z3ZUW0GQR1XS
KYSE-450 MnjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXONGtNUUN3ME2yO{46QDZ{IN88US=> NWPKfJJGW0GQR1XS
S-117 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjzTWM2OD1{OT6zPFU4KM7:TR?= MVLTRW5ITVJ?
SW13 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJ7Lki1NVkh|ryP NWHNSIhwW0GQR1XS
ES3 NUXWNmhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTNyLkO3N|Mh|ryP NY\pWW4yW0GQR1XS
HCT-116 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHhR5dWUUN3ME2zNE42PTV2IN88US=> NXjlW4ZlW0GQR1XS
NCI-H1693 MmnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW0TWM2OD1|MD61PVQzKM7:TR?= NWnjSIg6W0GQR1XS
VM-CUB-1 NYfkUYhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTNyLk[0NVMh|ryP NIfVPVdUSU6JRWK=
NCI-H2170 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjnTWM2OD1|MT61O|g1KM7:TR?= NIXSRmJUSU6JRWK=
ALL-PO M4XyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrYTWM2OD1|MT64OFI5KM7:TR?= NGjLc|JUSU6JRWK=
NCI-H661 NXLMRpF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjY[JBxUUN3ME2zNk4xPjJ|IN88US=> MYjTRW5ITVJ?
NCI-H2347 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmzNXBKSzVyPUOyMlQ5OzdizszN M1yyRnNCVkeHUh?=
FTC-133 NXPXUmEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LFbGlEPTB;M{KuO|A3KM7:TR?= NYftVmVrW0GQR1XS
COLO-829 M{XnRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjvelNKSzVyPUOzMlM1PjdizszN NYnMO2ZJW0GQR1XS
GOTO M4XsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFyw[3pKSzVyPUOzMlUzPThizszN MWnTRW5ITVJ?
YAPC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\WTWM2OD1|Mz64NVU6KM7:TR?= NUTHV49uW0GQR1XS
LCLC-103H M1HX[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Hac2lEPTB;M{SuNVYzPCEQvF2= MX;TRW5ITVJ?
SiHa NYrK[HpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Lsc2lEPTB;M{SuN|gyPyEQvF2= NFXBb5ZUSU6JRWK=
LK-2 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vY[mlEPTB;M{SuOVcxQCEQvF2= NWPnSGFnW0GQR1XS
KP-N-YS Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTN2LkeyNFIh|ryP MWXTRW5ITVJ?
NCI-SNU-1 NX:xfVNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnVeVRKSzVyPUO1MlE4QSEQvF2= M{iw[3NCVkeHUh?=
KNS-81-FD NUn5fXA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jwU2lEPTB;M{WuOlY{KM7:TR?= NVPiXolIW0GQR1XS
SCC-9 NG\Yb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTN4LkexOFYh|ryP NV3jVGM{W0GQR1XS
SH-4 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Wwc2lEPTB;M{[uO|Mh|ryP NUHScY5lW0GQR1XS
HCC-1954 MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN5LkK3Nlkh|ryP MmfLV2FPT0WU
BALL-1 NX3HdXlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTN5LkWzNVYh|ryP M4C4cHNCVkeHUh?=
BE-13 MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\SfIVOUUN3ME2zO{44ODF6IN88US=> M2nrTnNCVkeHUh?=
COLO-678 NX25[Fh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTN5Lkm0N|ch|ryP M4SxSXNCVkeHUh?=
SK-MEL-3 M1PITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUP3O4l4UUN3ME2zPE4zOzl5IN88US=> M{jDOHNCVkeHUh?=
OAW-28 M1vmN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXFV2FKSzVyPUO4MlY{QSEQvF2= M4PONHNCVkeHUh?=
CAMA-1 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTPTWM2OD1|OD65OlkyKM7:TR?= MYXTRW5ITVJ?
C2BBe1 M3PEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN7LkixPEDPxE1? MVXTRW5ITVJ?
A3-KAW NEGycGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[yNoVDUUN3ME20NE4{PjZzIN88US=> MYPTRW5ITVJ?
SK-MEL-24 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT5TWM2OD12MD61PVMyKM7:TR?= MlzSV2FPT0WU
KYSE-140 NFzieJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHmdJZKSzVyPUSwMlcyPjVizszN NITvdWVUSU6JRWK=
MOLT-16 NWDoUW8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TU[GlEPTB;NEGuNVU{PiEQvF2= M{O3XHNCVkeHUh?=
CFPAC-1 NHHTNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTR{LkWyNVEh|ryP NIHHPWpUSU6JRWK=
NB14 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3aPYpKSzVyPUSyMlcxOjdizszN MWXTRW5ITVJ?
COLO-792 MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf5bWJoUUN3ME20Nk45QTZzIN88US=> MVPTRW5ITVJ?
RH-1 NVO0cGFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTHTWM2OD12Mz60PFM3KM7:TR?= NID4enFUSU6JRWK=
NCI-H522 NETHRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jRe2lEPTB;NESuN|U3QCEQvF2= M4T6OHNCVkeHUh?=
Ca-Ski M{DmbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW4W4NKSzVyPUS0MlgyOTRizszN NFr1UmRUSU6JRWK=
KGN Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXJTWM2OD12OD6zNFY{KM7:TR?= Ml;qV2FPT0WU
UACC-62 M3qzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7w[nBKSzVyPUS4MlQxPzJizszN NHv2OpZUSU6JRWK=
NCI-H358 M4rVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vIZ2lEPTB;NEmuN|AyQCEQvF2= M4K1V3NCVkeHUh?=
LS-411N NVf3WVdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXtTWM2OD12OT6zNVE5KM7:TR?= MVHTRW5ITVJ?
IST-MES1 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR7LkW2NlUh|ryP MkLIV2FPT0WU

... 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 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

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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Clinical Trial Information

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

Tech Support

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

Handling Instructions

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID