Pictilisib (GDC-0941)

Catalog No.S1065 Synonyms: RG7321

Pictilisib (GDC-0941) Chemical Structure

Molecular Weight(MW): 513.64

Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.

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Cited by 59 Publications

9 Customer Reviews

  • Clonogenic assays of TNBC cell lines grown continuously in increasing concentrations of palbociclib, divided by gene expression subtypes: LAR, luminal androgen receptor; MSL, mesenchymal stem-like; MES, mesenchymal and basal-like. All cell lines are RB1 wild-type except RB1 mutant BT549.

    Clin Cancer Res, 2017, 23(18):5561-5572. Pictilisib (GDC-0941) purchased from Selleck.

    Dual PI3K/BRAF inhibition upregulates BIM and enhances apoptosis in PTEN cells. A, left, Western blot of 1205Lu cells treated with PLX4720 (3 μmol/L, 48 hours), the PI3K inhibitor GDC-0941 (3 μmol/L, 48 hours), or both drugs in combination (PtG); right, immunofluorescence staining of BIM (green) and DAPI (blue) in PTEN cells following PLX4720 treatment (3 μmol/L, 48 hours), the PI3K inhibitor LY294002 (10 μmol/L, 48 hours), or both drugs in combination (PLXtLY). B, left, immunofluorescence staining of PTEN 1205Lu following combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48hours) increases nuclear localization of FOXO3a (green). DAPI is shown in blue. Magnification 40. Right, combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48 hours) increases PTEN WM793 BIM mRNA levels to those observed with single BRAF inhibition (3 μmol/L PLX4720, 48 hours) in the PTENt WM35. C, PTEN cells were treated with PLX4720 (3 μmol/L, 48 hours), GDC-0941 (3 μmol/L, 48hours), or a combination of the 2 drugs (3Pt3G) before Annexin-V staining was analyzed by flow cytometry (*, P < 0.05 between the drug combination and each inhibitor alone). D, combined BRAF/PI3K inhibitor treatment blocks the escape of 1205Lu cells (PTEN) from therapy. Spheroids of 1205Lu cells were treated with either PLX4720 alone (3 and 10 μmol/L: data shows 3 mmol/L), LY294002 (10 μmol/L) alone or a combination of the 2 drugs for 72 hours. In other studies, spheroids were treated with drugs for 72 hours and then allowed to recover for 120 hours. Micrograph shows viability staining (green= live cells, red= dead cells). Magnification 10×.

    Cancer Res 2011 71, 2750-2760. Pictilisib (GDC-0941) purchased from Selleck.

  • Combination of rapamycin and PI-103 leads to the suppression of AKT phosphorylation (phospho-specific western blot). Mel-Juso and 518A2 cells were treated with GDC-0941 from 0.05–1 μmol/L alone and in combination with rapamycin (50 nmol/L) for 24 hours. Control treatment was with DMSO.

     

     

    J Inves Der 2010 131, 495-503. Pictilisib (GDC-0941) purchased from Selleck.

    Growth inhibition induced by the FGFR inhibitor BGJ398 and the PI3K inhibitors alone or in combination. AN3CA (A-C), JHUEM2 (D-F) and MFE296 (G-I) cells were treated with the indicated doses of BGJ398, GDC-0941 a n d BYL719 alone or in combination for 96 hours and an Sulforhodamine B (SRB) assay was subsequently performed. Data are presented as a percentage of the control, in which cells were treated with 0.1% (v/v) DMSO. Points represent the mean of three independent experiments (each performed in triplicate). Error bars represent the standard error of the mean (SEM) and lines were fitted using non-linear regression analysis. Interaction of BGJ398 and GDC-0941(redcircles) or BYL719(blacksquares) in AN3CA(C), JHUEM2(F) and MFE296(I). Median effect analysis was used to evaluate the interaction between the inhibitor combinations. Horizontal dotted lines indicate the boundaries for each interaction classification.

    Mol Cancer Ther, 2017, 16(4):637-648. Pictilisib (GDC-0941) purchased from Selleck.

  • TGF-β induces mTORC2 activation. ( A ) NMuMG cells were treated with TGF-β for the indicated times before lysis and immunoblotting. (B ) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to anti-Rictor immunoprecipitation, and the immunoprecipitates were subjected to in vitro kinase assays using kinase-inactive Akt1 as a substrate, before immunoblotting of the kinase reactions, immunoprecipitates and cell lysates. The left panels are from the same gel, without differential exposure. ( C ) NMuMG cells were treated or not with TGF-β or insulin for the indicated times, in the presence or absence of SB431542 or GDC-0941. The kinase activity of mTORC2 was then assessed as in B. The top panels are from the same gel, without differential exposure. (D) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to immunoprecipitation using Rictor antibody, and/or immunoblotted.

    J Cell Sci 2012 125(Pt 5), 1259-73. Pictilisib (GDC-0941) purchased from Selleck.

    Effects of LY294002 and GDC-0941 on the high-glucose-induced plasma membrane translocation of DGK δ1. (A, C) HEK293 cells were transfected with pAcGFP-DGKδ1 or pAcGFP-C1 vector. After being glucose-starved for 2.5 h and the subsequent pretreatment with (A) 10 μM LY294002 (Sigma-Aldrich) or (C) 1 μM GDC-0941 (Selleck Chemicals) for 30 min, the cells were incubated with or without high glucose (25 mM) for 5 min. The cells were fixed with 3.7% formaldehyde and observed using confocal laser-scanning microscopy. Scale bar = 10 μm. (B, D) After treatment with (B) LY294002 or (D) GDC-0941, the percentages of cells exhibiting the translocation of AcGFP-tagged DGK δ 1 to the plasma membrane were scored. More than 20 cells ex-pressing AcGFP-tagged DGK δ1 were counted in each experiment. The results are the means ± S.D. of three independent experiments. The statistical significance was deter-mined using Student's t -test (** P < 0.01, *** P < 0.005)

    Biochim Biophys Acta 2012 1823, 2210-6. Pictilisib (GDC-0941) purchased from Selleck.

  • After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of GDC-0941  for 3h,followed by 15-minute  stimulation of 100ng/ml EGF.

     

     

     

    Dr. Zhang of Tianjin Medical University. Pictilisib (GDC-0941) purchased from Selleck.

    We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

     

     

    Saraswati Sukumar of Johns Hopkins University School of Medicine. Pictilisib (GDC-0941) purchased from Selleck.

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    PI3K pathway signaling in GDC-0941 and MK-2206 treated MCF-7 derivatives with PIK3CA or  AKT1 mutations. Cells were grown in medium containing 5% FBS and treated with vehicle or increasing concentrations of GDC-0941 (0 nM, 50 nM, 100 nM, and 400 nM) or MK-2206 (0 nM, 100 nM, 250 nM, 1000 nM). After 24 hours of drug treatment, lysates were prepared and equal amounts of protein were load ed onto SDS-PAGE gels and blotted with the indicated antibodies.

    Pictilisib (GDC-0941) purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.
Targets
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
3 nM 3 nM 33 nM 75 nM 0.58 μM(Ki app)
In vitro

GDC-0941 is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold), and greater levels of selectivity against members of PI3K class II, III, and IV, including C2β, Vps34, DNA-PK, and mTOR. GDC-0941 potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. GDC-0941 inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 μM, 0.14 μM, 0.28 μM, and 0.72 μM, respectively. [1] GDC-0941 treatment potently inhibits the proliferation of both trastuzumab-sensitive and -insensitive HER2-amplified cells with IC50 of 149-944 nM. GDC-0941 inhibits proliferation of HER2-amplified cells that harbor PIK3CA mutations with IC50 of <500 nM, and effectively inhibits both proliferation and viability of HER2-amplified breast cancer cells that are resistant to trastuzumab due to PTEN loss. [2] GDC-0941 significantly inhibits the growth of HCT116, DLD1 and HT29 cells with GI50 of 1081 nM, 1070 nM and 157 nM, respectively. [3] GDC-0941 inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 M2\hcmtqdmG|ZTDBd5NigQ>? M3HROlEhcA>? MYLEUXNQ NUP4SYZMUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDk[Yx1[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN NGnt[JcyQDd3NE[1OC=>
Sf9 M4TCXGtqdmG|ZTDBd5NigQ>? NF\YRm4yKGh? NH\VcoNFVVOR M1i5eWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBJOTB2Nz3SJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO MmW0NVg4PTR4NUS=
Sf9 NYX5eIZlU2mwYYPlJGF{e2G7 M3[4RlEhcA>? NGfXVGtFVVOR M1vzcmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBGPTR3LVugcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> NHvNdm8yQDd3NE[1OC=>
Sf9 M2jHeWtqdmG|ZTDBd5NigQ>? NWPTTW9mOSCq M{nmfWROW09? M1fD[2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wN|Mh|ryP NWfnTVhZOTh5NUS2OVQ>
Sf9 MlHZT4lv[XOnIFHzd4F6 NFzBWFMyKGh? NVjJOmxpTE2VTx?= NUHZbFdOUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[Q>? MXmxPFc2PDZ3NB?=
MDA-MB-361 MlvDSpVv[3Srb36gRZN{[Xl? Mo\YNkBp MkTWSG1UVw>? M{fOdGlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvODJ6IN88US=> NVHtUlNWOTh5NUS2OVQ>
PC3 NUWzVHlkTnWwY4Tpc44hSXO|YYm= MnHGNkBp M3TNXmROW09? M2\YNWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGDDN{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yM{eg{txO M2ixNlE5PzV2NkW0
U87MG MlGzSpVv[3Srb36gRZN{[Xl? NWftO|FDOiCq MnHpSG1UVw>? M4rUXWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? NXTtVGxUOTh5NUS2OVQ>
MDA-MB-361 NH3kcHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvzPVYhcA>? MlzrSG1UVw>? MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlczKM7:TR?= M1vv[lE5PzV2NkW0
A2780 NXm1[4ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\jU|k3KGh? MmP3SG1UVw>? MlXZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczD3bZRpKFCLS{PDRUBidmRiUGTFUkBufXSjdHnvckB4cXSqIFnDOVAhd2ZiMD6xOEDPxE1? MVixPFc2PDZ3NB?=
PC3 M{HMVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnhWVlQQTZiaB?= NVm2UohkTE2VTx?= NVrhW2R5UUN3ME2wMlI5KM7:TR?= MoHjNVg4PTR4NUS=
U87MG NVjRT45vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXzRoU6PiCq MkXrSG1UVw>? NVriN3RGUUN3ME2wMlk2KM7:TR?= M3\GNVE5PzV2NkW0
Sf9 NVToeJRmU2mwYYPlJGF{e2G7 NGXYd2E{OCCvaX6= M33sVGROW09? Mn3FTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= MknUNlI2PDh|NEK=
RAW 264.7 M{XjUWtqdmG|ZTDBd5NigQ>? M{fFUFkxKG2rbh?= MXvEUXNQ M3vhRmlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvOjl6IN88US=> MXGyNlU1QDN2Mh?=
Sf9 M2\Tc2tqdmG|ZTDBd5NigQ>? NXjRclg1OSCq MmjyTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4JmfGFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOIOTDj[YxteyC5aYToJGlEPTBib3[gNE4xOTdizszN MkTNNlM2PDB4NEW=
Sf9 NF;EdXpMcW6jc3WgRZN{[Xl? NW\NTmtVOSCq NVPkSnFJUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> NX;MXm9WOjN3NEC2OFU>
Sf9 NX;VWpRJU2mwYYPlJGF{e2G7 M2fmSlEhcA>? MlzFTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4didW2jIHX4dJJme3OnZB?= NVrINGFPOjN3NEC2OFU>
Sf9 MXfLbY5ie2ViQYPzZZk> NVjBOZdLOSCq MkK3TY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZB?= M12weFI{PTRyNkS1
SKOV3 NXjIUGtWU2mwYYPlJGF{e2G7 NULwZYNiOSEQvF2= Mon6NUBp NHnabndFVVOR NIP6XWdKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w NIjJd4wzOzN4MEO0PC=>
MCF7 Mm\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuxJO69VQ>? NG\vZYs6PiCq MnfySG1UVw>? NW\I[pFIT0l3ME2wMlA4ODJizszN M2m2d|I{OzZyM{S4
SKOV3 NY\MVZBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfjNUDPxE1? M{jpcVk3KGh? NYr0NHZwTE2VTx?= Mn[zS2k2OD1yLkG0O|Yh|ryP NYfKNpJsOjN|NkCzOFg>
PC3 NU\pNFNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP2TFg4OiCq NVKxVGxFTE2VTx?= NY[5[XhYUUN3ME2wMlI5KM7:TR?= MX[yNVk5OTdzNB?=
MCF7.1 M3[xTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe4WYs4OiCq NHfV[FFFVVOR NV7j[YhOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCKRWKyJIdmdmVid3n0bEBKSzVyIH;mJFAvOjhizszN MmHQNlE6QDF5MUS=
MCF7-neo/Her2 MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7YO|IhcA>? NH;pNGVFVVOR NHe4VZlKSzVyPUCuNlkh|ryP NYixVHVLOjN4NkK5NFM>
MCF7-neo/Her2 NIXJ[4VMcW6jc3WgRZN{[Xl? NXfBd5ZOUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO NIX0VnIzOzZ4MkmwNy=>
PC3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj3fYM4OiCq MnjlSG1UVw>? NFru[|JGSzVyPUCuN|Qh|ryP NVPmdodPOjF7OEW2N|k>
MCF7.1 NVq2XGM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn5O|IhcA>? NIO5b4dFVVOR M1[1OWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFXDOVAhd2ZiMD6zPUDPxE1? NGHufVkzOTl6NU[zPS=>
PC3 NWK4[pQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX23NkBp MnHuSG1UVw>? NG\Xd2VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> MUiyNFA2ODZ4OR?=
MCF7.1 NEjIVXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXW3NkBp NF;4SYpFVVOR M4L0bWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFnDOVAhd2ZiMD6zOEDPxE1? NWXxUoJ6OjByNUC2Olk>
MCF7.1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV63NkBp MYPFR|UxRTBwN{Kg{txO MVuyNFM1PjZ3Nh?=
NCI-H1975 MVTDfZRwfG:6aXOgRZN{[Xl? NVLQbJk3PzJiaB?= MnX4TWM2OD1yLkK3JO69VQ>? Mn;QNlMxPTl3NEW=
H460 MVjDfZRwfG:6aXOgRZN{[Xl? M1jWblczKGh? NUHpdHpIUUN3ME2wMlg4KM7:TR?= NWXMeYFUOjNyNUm1OFU>
HT-29 MV7DfZRwfG:6aXOgRZN{[Xl? Mn3MO|IhcA>? MYjJR|UxRTBwNk[g{txO M1HUVlI{ODV7NUS1
HepG2 NI\TNZBEgXSxdH;4bYMhSXO|YYm= M4e1UlczKGh? MmLBTWM2OD1zIN88US=> Mln5NlMxPTl3NEW=
SGC7901 MUfDfZRwfG:6aXOgRZN{[Xl? NV\sb|h3PzJiaB?= MmHpTWM2OD1zLkig{txO NGXkepQzOzB3OUW0OS=>
NCI-H226 MlfLR5l1d3SxeHnjJGF{e2G7 M1zJTVczKGh? MYLJR|UxRTJwOTFOwG0> NXvZT2JCOjNyNUm1OFU>
A549 MVXDfZRwfG:6aXOgRZN{[Xl? NH:3U5A4OiCq M4LOW2lEPTB;Nj65JO69VQ>? NFK4OYszOzB3OUW0OS=>
U87MG MV7DfZRwfG:6aXOgRZN{[Xl? MlT3O|IhcA>? M3i5N2lEPTB;Nz63O{DPxE1? M2HaPVI{ODV7NUS1
HBC4 NYDFO2E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDsc4dIUTVyPT22MlA{KE1? MljrNlI{OzZ{NE[=
BSY1 M3XpUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jocYxw\0eLNUC9MVYvQTBiTR?= M1LIWlIzOzN4MkS2
HBC5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[zRoxw\0eLNUC9MVYvPjBiTR?= M4KybVIzOzN4MkS2
MCF7 NH\5d5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXJTY1td2eJSUWwQU04NjN|IF2= M17USVIzOzN4MkS2
MDA-MB-231 NFzHSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrTcI9oT0l3ME2tOU41PiCP NFK3XI4zOjN|NkK0Oi=>
U251 Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MniycI9oT0l3ME2tOU42OCCP NVGyZXliOjJ|M{[yOFY>
SF268 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjQ[XZtd2eJSUWwQU02NjN7IF2= MonrNlI{OzZ{NE[=
SF295 NWPwbYJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnIXW4{dG:pR1m1NF0uPi5|NzDN MVuyNlM{PjJ2Nh?=
SF539 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTj[oxtd2eJSUWwQU03NjVyIF2= MVuyNlM{PjJ2Nh?=
SNB75 M121T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\aepNPdG:pR1m1NF0uPy5zMDDN NUjxfXdLOjJ|M{[yOFY>
SNB78 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLpcI9oT0l3ME2tOk42OiCP NHLPVoozOjN|NkK0Oi=>
HCC2998 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnIR3JLdG:pR1m1NF0uPi5{OTDN NF;yXGozOjN|NkK0Oi=>
KM12 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;0cI9oT0l3ME2tOU44PiCP MknCNlI{OzZ{NE[=
HT-29 MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrsc4dIUTVyPT22MlMxKE1? NH3UU2szOjN|NkK0Oi=>
HCT15 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nXVIxw\0eLNUC9MVYvOTJiTR?= MmLCNlI{OzZ{NE[=
HCT116 NYDafGxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\lTGFMdG:pR1m1NF0uPS56NzDN M2PXPFIzOzN4MkS2
NCI-H23 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH2cI9oT0l3ME2tOU44OyCP NYLMbJFqOjJ|M{[yOFY>
NCI-H226 NGPGcGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PKeYxw\0eLNUC9MVYvOjFiTR?= MX:yNlM{PjJ2Nh?=
NCI-H522 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDGcI9oT0l3ME2tOk42QCCP NUHpV3ZnOjJ|M{[yOFY>
NCI-H483 M3mxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXQcI9oT0l3ME2tOk42PiCP NVPaRlI4OjJ|M{[yOFY>
A549 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzZToR6dG:pR1m1NF0uPi5zNTDN NFjUVWozOjN|NkK0Oi=>
DMS273 NX3mcnd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW3cI9oT0l3ME2tOk41OyCP NGfiPVYzOjN|NkK0Oi=>
DMS114 NFjsVnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPmboJmdG:pR1m1NF0uPS57MjDN MWqyNlM{PjJ2Nh?=
LOXIMVI M1TCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LzbIxw\0eLNUC9MVYvOjliTR?= M4H6R|IzOzN4MkS2
OVCAR3 NFrXU3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvsc4dIUTVyPT22MlcyKE1? NFzoTGQzOjN|NkK0Oi=>
OVCAR4 M3jiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfsc4dIUTVyPT21Mlc3KE1? NGG2VVYzOjN|NkK0Oi=>
OVCAR5 Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzsc4dIUTVyPT22MlI3KE1? NXP6bFR7OjJ|M{[yOFY>
OVCAR8 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;McI9oT0l3ME2tOU44OyCP MnvnNlI{OzZ{NE[=
SKOV3 NEPQcJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjod3RrdG:pR1m1NF0uPi53MjDN M33r[|IzOzN4MkS2
RXF631L NGPJZplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDNZo9ldG:pR1m1NF0uPi56ODDN NV24dpV2OjJ|M{[yOFY>
ACHN NYrOPWZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHsc4dIUTVyPT22MlA4KE1? Ml7INlI{OzZ{NE[=
St-4 NHnKS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3sc4dIUTVyPT21MlU3KE1? Mn;sNlI{OzZ{NE[=
MKN1 NIjMNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3Sm9VdG:pR1m1NF0uPy5yODDN M17QSFIzOzN4MkS2
MKN7 NVLTRXRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULsc4dIUTVyPT22MlUxKE1? M3\5dFIzOzN4MkS2
MKN28 NV:3NG0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7sc4dIUTVyPT21MlUzKE1? NYf3OG1WOjJ|M{[yOFY>
MKN45 NYq1WpdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnsc4dIUTVyPT22MlU2KE1? M2Dw[|IzOzN4MkS2
MKN74 MmPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnsXHVVdG:pR1m1NF0uPi5yMjDN NXrkOFI6OjJ|M{[yOFY>
DU145 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPsc4dIUTVyPT21Mlg2KE1? MXKyNlM{PjJ2Nh?=
PC3 NH2yeGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XQXYxw\0eLNUC9MVYvPjZiTR?= M2jT[VIzOzN4MkS2
ES5 NEfLO4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljiTWM2OD13MD6yNUBvVQ>? M4r0dXNCVkeHUh?=
HH M4r0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL5TWM2OD1zMUGuNFghdk1? M1vXfnNCVkeHUh?=
MHH-PREB-1 NF;E[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnXTWM2OD1zMUSuN{BvVQ>? MUfTRW5ITVJ?
NCI-H1770 M1PUWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLTTWM2OD1zMkOuPFYhdk1? NVW5N243W0GQR1XS
HuO9 M3vvPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\1fGdKSzVyPUKwOk4xOiCwTR?= M4fFPXNCVkeHUh?=
HAL-01 NWLhW4pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rwOWlEPTB;MkC2Mlc{KG6P MnrhV2FPT0WU
NOS-1 M{D1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjrTWM2OD1{MUGuPFIhdk1? MXnTRW5ITVJ?
HGC-27 NFjzTpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJzMj61O{BvVQ>? M375fHNCVkeHUh?=
NB69 M3;uZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULGUZljUUN3ME2yOFUvOjdibl2= NVHmbFBwW0GQR1XS
RS4-11 M3vxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3uTWM2OD1{NkGuO|Yhdk1? MXXTRW5ITVJ?
DOK MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzKOpd4UUN3ME2zNFEvPyCwTR?= MXzTRW5ITVJ?
LB2241-RCC NVzUXHhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S4emlEPTB;M{CzMlg1KG6P M1XKTXNCVkeHUh?=
NCI-H1623 M4HiUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3my[2lEPTB;M{C0MlA5KG6P MWDTRW5ITVJ?
YH-13 NXj6N3BoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTNyND6zNkBvVQ>? MVHTRW5ITVJ?
BPH-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLZTWM2OD1|MUSgcm0> MUfTRW5ITVJ?
AN3-CA NWHY[mkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jhcmlEPTB;M{SwMlM4KG6P M1q5cXNCVkeHUh?=
ES7 M1nlNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn5dIxKSzVyPUO0NU46QSCwTR?= Ml3EV2FPT0WU
MDA-MB-175-VII NFvHU|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTOTWM2OD1|NUKuPVIhdk1? NG[xfpRUSU6JRWK=
GAMG NYnNN5lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXnd|VSUUN3ME2zO|AvQDVibl2= NIK4UXBUSU6JRWK=
CHL-1 NXnvb4F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XT[WlEPTB;M{e4MlY2KG6P MknPV2FPT0WU
NB7 MlTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHpW|BMUUN3ME2zPFkvQDNibl2= NVry[pVrW0GQR1XS
MFE-280 Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTRzOD6yJI5O M4j0[nNCVkeHUh?=
HL-60 M1HNPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nPUmlEPTB;NEK1Mlc2KG6P MnT2V2FPT0WU
GCIY M122Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXxZnpKSzVyPUSzN{45KG6P Ml73V2FPT0WU
MDA-MB-361 NH;uSohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M330T2lEPTB;NEO5MlE{KG6P MVzTRW5ITVJ?
LXF-289 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH4TWM2OD12NEiuNlchdk1? NGPqeXJUSU6JRWK=
NBsusSR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\wTGlEPTB;NEi4Mlg2KG6P M3TGb3NCVkeHUh?=
KU-19-19 M3;uOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy0[W9KSzVyPUWxOk4xPyCwTR?= MoXyV2FPT0WU
A204 NEHPfoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jScGlEPTB;NUKyMlM{KG6P NEXxbVFUSU6JRWK=
LB1047-RCC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj6TWM2OD13MkKuPVMhdk1? NUHpbW9NW0GQR1XS
COLO-684 NHfrOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKzTWM2OD13MkOuNVEhdk1? NIXob4VUSU6JRWK=
PA-1 NHjJXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTV|Mj60NUBvVQ>? MlnWV2FPT0WU
MG-63 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3JbXBKSzVyPUW0NU4yOSCwTR?= M2XOWXNCVkeHUh?=
BHT-101 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPucFdKSzVyPUW0OE46PCCwTR?= MmTTV2FPT0WU
NKM-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTNTWM2OD13OUOuNFkhdk1? NXeyXlliW0GQR1XS
T47D NFXkN|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUKzfoVCUUN3ME21PVcvPTZibl2= NIfsZlhUSU6JRWK=
MOLT-4 NXLyc4FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TxNmlEPTB;NkKzMlYzKG6P MV;TRW5ITVJ?
IGROV-1 Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTZ|ND6zNUBvVQ>? MXLTRW5ITVJ?
ES4 NGPDdXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISwTIlKSzVyPU[zPU42PCCwTR?= NHTMe5NUSU6JRWK=
HuO-3N1 MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HvTGlEPTB;NkSyMlM5KG6P MlXXV2FPT0WU
NEC8 NH\VNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPtVW1KSzVyPU[1N{42PyCwTR?= M{nXNXNCVkeHUh?=
HO-1-N-1 NHHjZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Hob2lEPTB;NkW5MlE4KG6P NGrsU|hUSU6JRWK=
EPCL-272H M{iwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXiyflBNUUN3ME22PFcvOjFibl2= NUPYd3hSW0GQR1XS
D-263MG M1HsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D0VWlEPTB;N{G4MlEhdk1? M3jRPXNCVkeHUh?=
MV-4-11 NIO3cVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjzdmlxUUN3ME23NlQvOzFibl2= MWHTRW5ITVJ?
SK-NEP-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;5[2lEPTB;N{K1Mlk1KG6P M2rxeXNCVkeHUh?=
SW872 NHrnWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnFdmpKSzVyPUeyO{45QSCwTR?= NVTPWpU4W0GQR1XS
P30-OHK M3KwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XXbGlEPTB;N{OwMlcyKG6P MmrtV2FPT0WU
OMC-1 M{\YWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r1eWlEPTB;N{WxMlA6KG6P NXruZ4VyW0GQR1XS
LoVo NGDkOnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S1UGlEPTB;N{e3Mlkhdk1? MWHTRW5ITVJ?
LNCaP-Clone-FGC NFXUOHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHBWFZKSzVyPUe5Ok4{PCCwTR?= M2Hl[HNCVkeHUh?=
L-363 NFjUe5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TNXmlEPTB;N{m4MlQzKG6P NWS0V5lvW0GQR1XS
ES8 MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXONZVjUUN3ME24NVAvPTJibl2= M4[1UHNCVkeHUh?=
697 NGK0ZopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf1bnlKSzVyPUizNU42PSCwTR?= MojkV2FPT0WU
HSC-3 NWHLUoE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrsTWM2OD16M{muOVQhdk1? NVW2dY5tW0GQR1XS
H4 NWTNXYZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXqwNVlEUUN3ME24OVAvQDVibl2= NH7jVJFUSU6JRWK=
QIMR-WIL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;GTWM2OD16NkWuNkBvVQ>? NFvIO49USU6JRWK=
OAW-42 NWHJPWxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTh5Mj6xPUBvVQ>? MVXTRW5ITVJ?
MCF7 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfXTWM2OD16OUiuOVkhdk1? NELBNW1USU6JRWK=
SCC-25 M4TM[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\ESZdKSzVyPUmxOE4yQSCwTR?= NH3OVm9USU6JRWK=
NCI-H1563 M1zZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\KV|FKSzVyPUmxOU46QSCwTR?= MYPTRW5ITVJ?
OVCAR-5 NUH5WGtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDrPWozUUN3ME25OFAvOTdibl2= M4HVenNCVkeHUh?=
HDLM-2 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTl2OT6yJI5O MkL1V2FPT0WU
NB5 M4L4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fye2lEPTB;OUW2MlYhdk1? MojzV2FPT0WU
NCI-H292 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTl5ND6zNkBvVQ>? MXzTRW5ITVJ?
A101D MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rxdWlEPTB;OUmwMlE6KG6P MU\TRW5ITVJ?
NCI-H1648 NYThfoE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTZTWM2OD17OUiuOVEhdk1? M1LnZ3NCVkeHUh?=
EKVX NIDQ[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmyPY5HUUN3ME2xMlAyOjlizszN M3riWnNCVkeHUh?=
SW1710 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFwMESyN|Mh|ryP MWPTRW5ITVJ?
WM-115 NIXZ[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfrTWM2OD1zLkC2OlU3KM7:TR?= MVjTRW5ITVJ?
CAL-54 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf0TWM2OD1zLkC3NFgyKM7:TR?= M3vze3NCVkeHUh?=
TGBC24TKB NX;hVHhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTFwMEiwOFUh|ryP MkfVV2FPT0WU
NCI-H520 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFwMEi5Olch|ryP NFzMbGhUSU6JRWK=
D-423MG NYTaNpJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2yV2NiUUN3ME2xMlA6QTZ{IN88US=> MUfTRW5ITVJ?
BFTC-905 NVWwdYNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPBcVFKSzVyPUGuNVM1PDlizszN MnXYV2FPT0WU
HT MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfTTWM2OD1zLkGzOFc5KM7:TR?= M{jO[XNCVkeHUh?=
CTB-1 NIDWc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXtTWM2OD1zLkG0Nlk{KM7:TR?= Mn3aV2FPT0WU
Hs-578-T M4DzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFwMUm1OlUh|ryP NX7vOY1HW0GQR1XS
HuH-7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrzcWtKSzVyPUGuNlA6PDlizszN MVrTRW5ITVJ?
LB996-RCC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjMXpFbUUN3ME2xMlIzOTd5IN88US=> MoGwV2FPT0WU
KYSE-270 MkDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PlNWlEPTB;MT6yPVc{PCEQvF2= M4[1WXNCVkeHUh?=
A4-Fuk NEjKR5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTh[ZpGUUN3ME2xMlI6QTl|IN88US=> M3rmVnNCVkeHUh?=
A498 NYXFUJVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwM{C0O|Qh|ryP NVn1SYF[W0GQR1XS
SK-MEL-1 NF;4S|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjnWIM4UUN3ME2xMlMxPjd7IN88US=> MofsV2FPT0WU
AU565 MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfjTWM2OD1zLkOxPFY{KM7:TR?= M3jxTnNCVkeHUh?=
Saos-2 M1rJVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwM{OyNFUh|ryP NFz4cI1USU6JRWK=
A549 M3\RUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPnTWM2OD1zLkO5PVch|ryP NFnC[Y9USU6JRWK=
BFTC-909 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGKwO5pKSzVyPUGuOFM{ODVizszN M3jYSnNCVkeHUh?=
MDA-MB-415 NX3aVZc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17rV2lEPTB;MT60PFY6OiEQvF2= M2PnTnNCVkeHUh?=
639-V MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIO4ZoNKSzVyPUGuOVAzPDVizszN NWPSemdJW0GQR1XS
A704 NHfPZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mni1TWM2OD1zLkWwO|g2KM7:TR?= MYjTRW5ITVJ?
PANC-03-27 NHvBOJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjZb5pKSzVyPUGuOVE1ODhizszN NVvt[mpPW0GQR1XS
SK-MEL-28 NUfZNZVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHTd5pPUUN3ME2xMlU3ODh3IN88US=> NX7XZpdYW0GQR1XS
Ramos-2G6-4C10 NWPXPVQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDNWGhCUUN3ME2xMlYxPzR4IN88US=> MUjTRW5ITVJ?
HuP-T4 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnETpZTUUN3ME2xMlYxPzd6IN88US=> NVTvZ5R4W0GQR1XS
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NCI-H358 M3[4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTR7LkOwNVgh|ryP MXXTRW5ITVJ?
LS-411N MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTvTWM2OD12OT6zNVE5KM7:TR?= NVLkXZdbW0GQR1XS
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... Click to View More Cell Line Experimental Data

In vivo GDC-0941 shows limited microsomal metabolism, resulting in 78% oral bioavailability [5]. Administration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. [1] Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. [2] GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases. [4]

Protocol

Kinase Assay:

[1]

+ Expand

Scintillation proximity assay:

Recombinant human PI3Kα, PI3Kβ, and PI3Kδ are coexpressed in a Sf9 baculovirus system with the p85α regulatory subunit and purified as GST-fusion proteins using affinity chromatography on glutathione-sepharose. Recombinant human PI3Kγ is expressed as monomeric GST-fusions and purified similarly. GDC-0941 is dissolved in DMSO and added to 20 mM Tris-HCl (pH 7.5) containing 200 μg yttrium silicate (Ysi) polylysine SPA beads, 4 mM MgCl2, 1 mM dithiothreitol (DTT), 1 μM ATP, 0.125 μCi [γ-33P]-ATP, and 4% (v/v) DMSO in a total volume of 50 μL. The recombinant GST-fusion of PI3Kα (5 ng), PI3Kβ (5 ng), PI3Kδ (5 ng), or PI3Kγ (5 ng) is added to the assay mixture to initiate the kinase reaction. After incubation for 1 hour at room temperature, the kinase reaction is terminated with 150 μL PBS. The mixture is then centrifuged for 2 minutes at 2000 rpm and read using a Wallac Microbeta counter. The reported IC50 values are calculated using a sigmoidal, dose-response curve fit in MDL Assay Explorer.
Cell Research:

[2]

+ Expand
  • Cell lines: SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, and MKN-7 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 48 and 72 hours
  • Method:

    Cells are exposed to various concentrations of GDC-0941 for 48, and 72 hours. Proliferation/viability of cells is detected by using the CellTiter-Glo Luminescent Cell Viability Assay. The pAkt (Ser473), cleaved caspase-3, and cleaved PARP are analyzed by western blot. The Caspase-Glo 3/7 assay and the Cell Death Detection ELISAplus assay are used to detect caspase 3/7 activity, and apoptosis, respectively.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: NCR nude mice implanted with MDA-MB-361.1 cells, and SCID, C.B-17/IcrHsd-Prkdcscid mice implanted subcutaneously with BT474-M1 cells
  • Formulation: Dissolved in 10% DMSO, 5% Tween 20, 85% water
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 44 mg/mL (85.66 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.64
Formula

C23H27N7O3S2

CAS No. 957054-30-7
Storage powder
in solvent
Synonyms RG7321

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

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Dilution Calculator

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02092831 Completed Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT01740336 Completed Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01474668 Completed Healthy Volunteer Genentech Inc. October 2011 Phase 1
NCT01437566 Completed Breast Cancer Genentech Inc. October 2011 Phase 2
NCT01240226 Completed Healthy Volunteer Genentech Inc. November 2010 Phase 1
NCT00999128 Completed Healthy Volunteers Genentech Inc. October 26 2009 Phase 1

Tech Support

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

Handling Instructions

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

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

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID