Pictilisib (GDC-0941)

Pictilisib (GDC-0941)は1種の有効なPI3Kα/δ阻害剤です。無細胞試験で、Pictilisib (GDC-0941)はPI3Kα/δに作用する時の IC50値は 3 nM で、p110β (11倍) とp110γ (25倍)に適合な選択性をしています。臨床2期。

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Pictilisib (GDC-0941) 化学構造
分子量: 513.64

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製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Pictilisib (GDC-0941)のメカニズム

製品の説明

生物活性

製品説明 Pictilisib (GDC-0941)は1種の有効なPI3Kα/δ阻害剤です。無細胞試験で、Pictilisib (GDC-0941)はPI3Kα/δに作用する時の IC50値は 3 nM で、p110β (11倍) とp110γ (25倍)に適合な選択性をしています。臨床2期。
ターゲット PI3Kα PI3Kβ PI3Kδ PI3Kγ
IC50 3 nM 33 nM 3 nM 75 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Sf9 MlTkT4lv[XOnIFHzd4F6 MVWxJIg> MoPjSG1UVw>? MUXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGSnbIThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NEnIUYIyQDd3NE[1OC=>
Sf9 M4rpcmtqdmG|ZTDBd5NigQ>? MXuxJIg> M4PyTWROW09? M1PKeWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBJOTB2Nz3SJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO M1\RflE5PzV2NkW0
Sf9 NUfuXXBrU2mwYYPlJGF{e2G7 MmPSNUBp MkPwSG1UVw>? NEDFRnRKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEhTTV2NT3LJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDwPFVidHCqYTD3bZRpKEmFNUCgc4YhOC5yMEOg{txO NXnQOVBsOTh5NUS2OVQ>
Sf9 MmXiT4lv[XOnIFHzd4F6 MUixJIg> NYnV[It[TE2VTx?= Mle3TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCzN{DPxE1? NW[3[GtmOTh5NUS2OVQ>
Sf9 NGHOR4ZMcW6jc3WgRZN{[Xl? NYLh[ohPOSCq MmTGSG1UVw>? MoLTTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> MV6xPFc2PDZ3NB?=
MDA-MB-361 NGO1eYhHfW6ldHnvckBCe3OjeR?= MVWyJIg> Mm\3SG1UVw>? MVXJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlAzQCEQvF2= NIGwWHcyQDd3NE[1OC=>
PC3 M1PNNWZ2dmO2aX;uJGF{e2G7 Ml7ONkBp NIjF[WJFVVOR MoTMTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kAxNjB|NzFOwG0> NEHK[4IyQDd3NE[1OC=>
U87MG M{PmbmZ2dmO2aX;uJGF{e2G7 MYeyJIg> NELVcHFFVVOR MmezTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? M{T5OFE5PzV2NkW0
MDA-MB-361 M1PPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO5OkBp MoLESG1UVw>? Mk\HRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOzZzIHPlcIx{KHerdHigVGlMO0ODIFW1OFUuUyCvdYTheIlwdiC5aYToJGlEPTBib3[gNE44OiEQvF2= MXKxPFc2PDZ3NB?=
A2780 NET3elJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3JcWtPQTZiaB?= MXTEUXNQ NH3Wdm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= NWK2TYZROTh5NUS2OVQ>
PC3 NFi2VZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV25OkBp MVnEUXNQ MVvJR|UxRTBwMkig{txO NHzGS2QyQDd3NE[1OC=>
U87MG NWjSO4hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT3cJZHQTZiaB?= NVHCfXUzTE2VTx?= M3H4eGlEPTB;MD65OUDPxE1? M{X0S|E5PzV2NkW0
Sf9 M1PTTGtqdmG|ZTDBd5NigQ>? NWLROIRMOzBibXnu NIL4TWhFVVOR MlXOTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= MVyyNlU1QDN2Mh?=
RAW 264.7 MYXLbY5ie2ViQYPzZZk> NV;lNZo3QTBibXnu NXvOcWlqTE2VTx?= M1vnXmlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvOjl6IN88US=> Mo\xNlI2PDh|NEK=
Sf9 M1XvSWtqdmG|ZTDBd5NigQ>? MX[xJIg> NGP3SXFKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> M3HlW|I{PTRyNkS1
Sf9 MoGzT4lv[XOnIFHzd4F6 NHjrRYIyKGh? NXrjSIN[UW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> M4\TPFI{PTRyNkS1
Sf9 NFPWfXBMcW6jc3WgRZN{[Xl? MVmxJIg> MYfJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[4FudWFiZYjwdoV{e2Wm NX;0NWtWOjN3NEC2OFU>
Sf9 NYjTXVRRU2mwYYPlJGF{e2G7 MXSxJIg> MV3Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm M133d|I{PTRyNkS1
SKOV3 MXPLbY5ie2ViQYPzZZk> NEjKfIUyKM7:TR?= NXLQemdoOSCq M1rGfGROW09? M3\pdGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25? M{TvTlI{OzZyM{S4
MCF7 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH0NUDPxE1? MVG5OkBp NHvMblFFVVOR NEL3RXpIUTVyPUCuNFcxOiEQvF2= MofjNlM{PjB|NEi=
SKOV3 MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7MNUDPxE1? M{LGSVk3KGh? NELOVXdFVVOR NFr0XllIUTVyPUCuNVQ4PiEQvF2= NYrpXYQ6OjN|NkCzOFg>
PC3 M4j3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp M4GxcGROW09? M3;oc2lEPTB;MD6yPEDPxE1? NFznc5AzOTl6MUexOC=>
MCF7.1 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HLSlczKGh? MkTISG1UVw>? Mo\hRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BJTVJ{IHflcoUhf2m2aDDJR|UxKG:oIECuNlgh|ryP M1:1PFIyQThzN{G0
MCF7-neo/Her2 NFXmTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\1OZhmPzJiaB?= NUXRZWpLTE2VTx?= NWi2b4J[UUN3ME2wMlI6KM7:TR?= NXe2VoxtOjN4NkK5NFM>
MCF7-neo/Her2 M{XJfGtqdmG|ZTDBd5NigQ>? MUfJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDTOFc{KHerdHigTWM2OCCxZjCwMlAxPyEQvF2= NVPZSYI2OjN4NkK5NFM>
PC3 M3SxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TrelczKGh? MUfEUXNQ NVXENmVuTUN3ME2wMlM1KM7:TR?= Mn20NlE6QDV4M{m=
MCF7.1 NWDhRnNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDZTnY4OiCq NGrHc2xFVVOR NVfoVWRLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigSWM2OCCxZjCwMlM6KM7:TR?= MWqyNVk5PTZ|OR?=
PC3 M2rCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp NH3VcYhFVVOR NIT2OWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> NGX1PHMzODB3ME[2PS=>
MCF7.1 NUP3Wng1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDWO|IhcA>? MoPLSG1UVw>? NX\UXYFRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigTWM2OCCxZjCwMlM1KM7:TR?= NVTDUpJsOjByNUC2Olk>
MCF7.1 NWTiPHhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVO3NkBp M1LvN2VEPTB;MD63NkDPxE1? M{P5dVIxOzR4NkW2
NCI-H1975 Mn2zR5l1d3SxeHnjJGF{e2G7 M2LIN|czKGh? MlfqTWM2OD1yLkK3JO69VQ>? MWeyN|A2QTV2NR?=
H460 NEj6OIZEgXSxdH;4bYMhSXO|YYm= NH:5WnY4OiCq NVnKfYxpUUN3ME2wMlg4KM7:TR?= NWr0TIZ{OjNyNUm1OFU>
HT-29 MnX6R5l1d3SxeHnjJGF{e2G7 MUi3NkBp MnHtTWM2OD1yLk[2JO69VQ>? MYSyN|A2QTV2NR?=
HepG2 MXPDfZRwfG:6aXOgRZN{[Xl? MnzjO|IhcA>? NYD3bJlTUUN3ME2xJO69VQ>? MYSyN|A2QTV2NR?=
SGC7901 MnHiR5l1d3SxeHnjJGF{e2G7 NHjiOXQ4OiCq NF3YWmFKSzVyPUGuPEDPxE1? MnfHNlMxPTl3NEW=
NCI-H226 NXPsbJZVS3m2b4TvfIlkKEG|c3H5 Ml;JO|IhcA>? MWnJR|UxRTJwOTFOwG0> MX:yN|A2QTV2NR?=
A549 M3TOXWN6fG:2b4jpZ{BCe3OjeR?= NG\SSXU4OiCq MV3JR|UxRTZwOTFOwG0> NGrCfVMzOzB3OUW0OS=>
U87MG NUX2[GI6S3m2b4TvfIlkKEG|c3H5 NHHQWnM4OiCq MXPJR|UxRTdwN{eg{txO M3jhRVI{ODV7NUS1
HBC4 NHPGS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH2OFhXdG:pR1m1NF0uPi5yMzDN MlnmNlI{OzZ{NE[=
BSY1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fS[Yxw\0eLNUC9MVYvQTBiTR?= NV75NFZ1OjJ|M{[yOFY>
HBC5 NFWyRW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XlbIxw\0eLNUC9MVYvPjBiTR?= NWXNfZJyOjJ|M{[yOFY>
MCF7 NGLoU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn4cI9oT0l3ME2tO{4{OyCP MXyyNlM{PjJ2Nh?=
MDA-MB-231 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPUcI9oT0l3ME2tOU41PiCP M3ewfFIzOzN4MkS2
U251 NXviTo9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPnRWxtd2eJSUWwQU02NjVyIF2= MYmyNlM{PjJ2Nh?=
SF268 NU\rfW02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjIR5E3dG:pR1m1NF0uPS5|OTDN MnH6NlI{OzZ{NE[=
SF295 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\MdIFPdG:pR1m1NF0uPi5|NzDN NYK1SZBqOjJ|M{[yOFY>
SF539 NWrqUIJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmGycI9oT0l3ME2tOk42OCCP MVyyNlM{PjJ2Nh?=
SNB75 Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nYdoxw\0eLNUC9MVcvOTBiTR?= NEXZdVYzOjN|NkK0Oi=>
SNB78 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2mzUYxw\0eLNUC9MVYvPTJiTR?= MnOwNlI{OzZ{NE[=
HCC2998 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPnT21td2eJSUWwQU03NjJ7IF2= NFfmSWwzOjN|NkK0Oi=>
KM12 M3jlbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPwcI9oT0l3ME2tOU44PiCP NGDuN5czOjN|NkK0Oi=>
HT-29 NGflTJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr2Vodtd2eJSUWwQU03NjNyIF2= M1i2e|IzOzN4MkS2
HCT15 NF2zUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\O[ZNQdG:pR1m1NF0uPi5zMjDN MV2yNlM{PjJ2Nh?=
HCT116 M2fhbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\lOoVDdG:pR1m1NF0uPS56NzDN MnTKNlI{OzZ{NE[=
NCI-H23 NGnMZpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yxVoxw\0eLNUC9MVUvPzNiTR?= MmLyNlI{OzZ{NE[=
NCI-H226 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;iVoNtd2eJSUWwQU03NjJzIF2= NEDPW28zOjN|NkK0Oi=>
NCI-H522 NGL6OG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfsc4dIUTVyPT22MlU5KE1? NUHSb4xVOjJ|M{[yOFY>
NCI-H483 NYXi[5l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;5cI9oT0l3ME2tOk42PiCP NVW4dop7OjJ|M{[yOFY>
A549 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\BXmhZdG:pR1m1NF0uPi5zNTDN MmPDNlI{OzZ{NE[=
DMS273 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXwTJJtd2eJSUWwQU03NjR|IF2= MXSyNlM{PjJ2Nh?=
DMS114 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjt[4Ztd2eJSUWwQU02Njl{IF2= MkK1NlI{OzZ{NE[=
LOXIMVI M1LLZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHoV3Btd2eJSUWwQU03NjJ7IF2= NFnrVoQzOjN|NkK0Oi=>
OVCAR3 M37BcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnsc4dIUTVyPT22MlcyKE1? M{jKPFIzOzN4MkS2
OVCAR4 NV3yOVc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfsc4dIUTVyPT21Mlc3KE1? NVewNIx5OjJ|M{[yOFY>
OVCAR5 Ml7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TORoxw\0eLNUC9MVYvOjZiTR?= NYjLTohXOjJ|M{[yOFY>
OVCAR8 NY[0TlZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O0Voxw\0eLNUC9MVUvPzNiTR?= NYOzeHdtOjJ|M{[yOFY>
SKOV3 NX;6NnJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nrfoxw\0eLNUC9MVYvPTJiTR?= MnnNNlI{OzZ{NE[=
RXF631L NXXQS2ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfkNI1td2eJSUWwQU03Njh6IF2= NEn5XJgzOjN|NkK0Oi=>
ACHN MkjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK2TmNtd2eJSUWwQU03NjB5IF2= MVuyNlM{PjJ2Nh?=
St-4 NV7lV4dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfwcI9oT0l3ME2tOU42PiCP MYCyNlM{PjJ2Nh?=
MKN1 NEX4XJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLsc4dIUTVyPT23MlA5KE1? NITwWGwzOjN|NkK0Oi=>
MKN7 NF7J[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvKfI5GdG:pR1m1NF0uPi53MDDN MXqyNlM{PjJ2Nh?=
MKN28 M1fhTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTLNVBtd2eJSUWwQU02NjV{IF2= NEfXRZUzOjN|NkK0Oi=>
MKN45 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfaRlVtd2eJSUWwQU03NjV3IF2= MV2yNlM{PjJ2Nh?=
MKN74 M3XlXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTScI9oT0l3ME2tOk4xOiCP NWLWeYROOjJ|M{[yOFY>
DU145 M17ae2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ezPYxw\0eLNUC9MVUvQDViTR?= MlnTNlI{OzZ{NE[=
PC3 MlnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETWbXdtd2eJSUWwQU03NjZ4IF2= M4fxcVIzOzN4MkS2
ES5 M2Lic2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXNcYpKSzVyPUWwMlIyKG6P MmHaV2FPT0WU
HH MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjPTWM2OD1zMUGuNFghdk1? NWDUXplJW0GQR1XS
MHH-PREB-1 M{PjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XZV2lEPTB;MUG0MlMhdk1? NYj5ZY1EW0GQR1XS
NCI-H1770 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF{Mz64OkBvVQ>? M{T3fnNCVkeHUh?=
HuO9 NHTQdVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDDTWM2OD1{ME[uNFIhdk1? MVLTRW5ITVJ?
HAL-01 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkmxTWM2OD1{ME[uO|Mhdk1? NGKzc5FUSU6JRWK=
NOS-1 NX7FO4F5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PiUGlEPTB;MkGxMlgzKG6P MYDTRW5ITVJ?
HGC-27 NFLNPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXzU29KSzVyPUKxNk42PyCwTR?= MX3TRW5ITVJ?
NB69 M4D4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jIbmlEPTB;MkS1MlI4KG6P NXHWc491W0GQR1XS
RS4-11 Mk\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M161NGlEPTB;Mk[xMlc3KG6P NEPzZXdUSU6JRWK=
DOK MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWniT|BNUUN3ME2zNFEvPyCwTR?= M1WzWnNCVkeHUh?=
LB2241-RCC MmTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITQ[W1KSzVyPUOwN{45PCCwTR?= MW\TRW5ITVJ?
NCI-H1623 M3q0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzDcmxHUUN3ME2zNFQvODhibl2= MlOyV2FPT0WU
YH-13 MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDqO2NUUUN3ME2zNFQvOzJibl2= NWPu[WFpW0GQR1XS
BPH-1 Ml7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTNzNDDuUS=> NW\tbppPW0GQR1XS
AN3-CA MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PaTmlEPTB;M{SwMlM4KG6P M324Z3NCVkeHUh?=
ES7 MmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTsTWM2OD1|NEGuPVkhdk1? MUPTRW5ITVJ?
MDA-MB-175-VII NEfNT|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTN3Mj65NkBvVQ>? NUTISGJnW0GQR1XS
GAMG MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTN5MD64OUBvVQ>? MmrxV2FPT0WU
CHL-1 NFPnUWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPxTWM2OD1|N{iuOlUhdk1? NVm4VpliW0GQR1XS
NB7 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL0dll5UUN3ME2zPFkvQDNibl2= MYDTRW5ITVJ?
MFE-280 M3jKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf2TWM2OD12MUiuNkBvVQ>? MV3TRW5ITVJ?
HL-60 M1H1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoiwTWM2OD12MkWuO|Uhdk1? NEXxeppUSU6JRWK=
GCIY MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LBcWlEPTB;NEOzMlghdk1? M4rQVHNCVkeHUh?=
MDA-MB-361 MmrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHyVFh[UUN3ME20N|kvOTNibl2= MYDTRW5ITVJ?
LXF-289 NYjVSlNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mon2TWM2OD12NEiuNlchdk1? NVjiZ|RbW0GQR1XS
NBsusSR MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HVS2lEPTB;NEi4Mlg2KG6P M2DJeXNCVkeHUh?=
KU-19-19 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnPfoZKSzVyPUWxOk4xPyCwTR?= NFO3RpdUSU6JRWK=
A204 M2TETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjzOIVKSzVyPUWyNk4{OyCwTR?= MW\TRW5ITVJ?
LB1047-RCC NYnvXm5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK3fY5KSzVyPUWyNk46OyCwTR?= NVW0N4hUW0GQR1XS
COLO-684 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTV{Mz6xNUBvVQ>? MWrTRW5ITVJ?
PA-1 NF\YfnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PG[mlEPTB;NUOyMlQyKG6P Mn6wV2FPT0WU
MG-63 NIjvPGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2e1emlEPTB;NUSxMlEyKG6P NYDYTJczW0GQR1XS
BHT-101 NW\vfJF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTMTXdKSzVyPUW0OE46PCCwTR?= MW\TRW5ITVJ?
NKM-1 NHfOe21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXC[3RLUUN3ME21PVMvODlibl2= MYrTRW5ITVJ?
T47D M2PMe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrEdXQ1UUN3ME21PVcvPTZibl2= NX:2W4plW0GQR1XS
MOLT-4 MnnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTZ{Mz62NkBvVQ>? MXzTRW5ITVJ?
IGROV-1 M{L3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH73OWdKSzVyPU[zOE4{OSCwTR?= M2TrW3NCVkeHUh?=
ES4 NXe1fVhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTZ|OT61OEBvVQ>? NHjuOW5USU6JRWK=
HuO-3N1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[z[WlEPTB;NkSyMlM5KG6P NIPvToZUSU6JRWK=
NEC8 MkG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf1OGlOUUN3ME22OVMvPTdibl2= MX3TRW5ITVJ?
HO-1-N-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknYTWM2OD14NUmuNVchdk1? NVfRSVBvW0GQR1XS
EPCL-272H NIDtTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjzToJHUUN3ME22PFcvOjFibl2= Ml7uV2FPT0WU
D-263MG M3LYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[zTWM2OD15MUiuNUBvVQ>? Mli4V2FPT0WU
MV-4-11 NXLyd3piT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTd{ND6zNUBvVQ>? NEW5NY1USU6JRWK=
SK-NEP-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL6TWM2OD15MkWuPVQhdk1? MX;TRW5ITVJ?
SW872 M{S0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\tW3hKSzVyPUeyO{45QSCwTR?= NGPRb4RUSU6JRWK=
P30-OHK MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHrfGJKSzVyPUezNE44OSCwTR?= MUXTRW5ITVJ?
OMC-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HTfWlEPTB;N{WxMlA6KG6P MXfTRW5ITVJ?
LoVo MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLQfZVuUUN3ME23O|cvQSCwTR?= NX3u[pZvW0GQR1XS
LNCaP-Clone-FGC NXnFN453T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojTTWM2OD15OU[uN|Qhdk1? M4XDc3NCVkeHUh?=
L-363 NYLTTGtFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFW5VlBKSzVyPUe5PE41OiCwTR?= MY\TRW5ITVJ?
ES8 NX21TnQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3TTlVKSzVyPUixNE42OiCwTR?= NHGy[|BUSU6JRWK=
697 NYHvbIRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrH[pdoUUN3ME24N|EvPTVibl2= MlzGV2FPT0WU
HSC-3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrZVnJKSzVyPUizPU42PCCwTR?= NVmxdYltW0GQR1XS
H4 M33rbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PBd2lEPTB;OEWwMlg2KG6P MXrTRW5ITVJ?
QIMR-WIL M4DpbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHqSVNKSzVyPUi2OU4zKG6P MmixV2FPT0WU
OAW-42 NU\Gc5RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV71dollUUN3ME24O|IvOTlibl2= M2\H[HNCVkeHUh?=
MCF7 NF2xPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjDTWM2OD16OUiuOVkhdk1? NV7OfIp2W0GQR1XS
SCC-25 NWL5fIlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Hic2lEPTB;OUG0MlE6KG6P M2C0RnNCVkeHUh?=
NCI-H1563 M136S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLBOVBEUUN3ME25NVUvQTlibl2= MY\TRW5ITVJ?
OVCAR-5 NFHlcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jmWWlEPTB;OUSwMlE4KG6P MnrwV2FPT0WU
HDLM-2 NVTi[o9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H4OGlEPTB;OUS5MlIhdk1? MlTYV2FPT0WU
NB5 NXP0NIluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnpdIpNUUN3ME25OVYvPiCwTR?= NImxe4tUSU6JRWK=
NCI-H292 NY\OOYpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTl5ND6zNkBvVQ>? M4XBXXNCVkeHUh?=
A101D NVfYT5RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTqTWM2OD17OUCuNVkhdk1? NV7WOlhUW0GQR1XS
NCI-H1648 NGrucpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\XbIxQUUN3ME25PVgvPTFibl2= NFy1e3VUSU6JRWK=
EKVX NXflPIFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTFwMEGyPUDPxE1? MoG5V2FPT0WU
SW1710 NITuO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTFwMESyN|Mh|ryP MkXBV2FPT0WU
WM-115 M33LNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nDdGlEPTB;MT6wOlY2PiEQvF2= NHLRWWRUSU6JRWK=
CAL-54 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHacGZWUUN3ME2xMlA4ODhzIN88US=> NWPoPI1YW0GQR1XS
TGBC24TKB NYOxPG1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwMEiwOFUh|ryP NUfGN|VtW0GQR1XS
NCI-H520 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXocYVNUUN3ME2xMlA5QTZ5IN88US=> NHXZbG9USU6JRWK=
D-423MG NYfTe2M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYToXW15UUN3ME2xMlA6QTZ{IN88US=> MknUV2FPT0WU
BFTC-905 NUXveXZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;4TWM2OD1zLkGzOFQ6KM7:TR?= NWfrdIx4W0GQR1XS
HT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwMUO0O|gh|ryP MU\TRW5ITVJ?
CTB-1 MkXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwMUSyPVMh|ryP M4S2T3NCVkeHUh?=
Hs-578-T MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGWwNGZKSzVyPUGuNVk2PjVizszN MlfGV2FPT0WU
HuH-7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fqbWlEPTB;MT6yNFk1QSEQvF2= M1rUO3NCVkeHUh?=
LB996-RCC Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfWNXBKSzVyPUGuNlIyPzdizszN MVXTRW5ITVJ?
KYSE-270 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFwMkm3N|Qh|ryP M3HFcXNCVkeHUh?=
A4-Fuk MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz1OYhKSzVyPUGuNlk6QTNizszN NGLPWohUSU6JRWK=
A498 M2TDeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzpbFRKSzVyPUGuN|A1PzRizszN MnSyV2FPT0WU
SK-MEL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwM{C2O|kh|ryP NIPKSVdUSU6JRWK=
AU565 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXyTWM2OD1zLkOxPFY{KM7:TR?= MYXTRW5ITVJ?
Saos-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHvTWM2OD1zLkOzNlA2KM7:TR?= MmrYV2FPT0WU
A549 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW0TWM2OD1zLkO5PVch|ryP NYHQRpdGW0GQR1XS
BFTC-909 MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXKRlVKSzVyPUGuOFM{ODVizszN NVjWb2E3W0GQR1XS
MDA-MB-415 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHqVGxSUUN3ME2xMlQ5Pjl{IN88US=> M135b3NCVkeHUh?=
639-V MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i1PWlEPTB;MT61NFI1PSEQvF2= NWnjSmhOW0GQR1XS
A704 NUfMNlIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXThWXhEUUN3ME2xMlUxPzh3IN88US=> MlW3V2FPT0WU
PANC-03-27 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf2TWM2OD1zLkWxOFA5KM7:TR?= Mlm2V2FPT0WU
SK-MEL-28 NH3UdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\qboxKSzVyPUGuOVYxQDVizszN NEP1XpNUSU6JRWK=
Ramos-2G6-4C10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf3TWM2OD1zLk[wO|Q3KM7:TR?= NWn5TYRmW0GQR1XS
HuP-T4 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHMb|M6UUN3ME2xMlYxPzd6IN88US=> NWLCOnQ1W0GQR1XS
VA-ES-BJ MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnnVplxUUN3ME2xMlYyOjdizszN NFPkN2lUSU6JRWK=
EFM-19 M4i4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnMOZFDUUN3ME2xMlYyQDFizszN NWnGO2dMW0GQR1XS
G-401 NHfzfJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTHTWM2OD1zLk[yNVY1KM7:TR?= NH7QOWdUSU6JRWK=
D-566MG Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwNkK1N{DPxE1? MmTlV2FPT0WU
JVM-3 NIX2dXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrNOI9uUUN3ME2xMlY1QDd3IN88US=> NEnaWG1USU6JRWK=
TK10 NFvudm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XWbWlEPTB;MT62O|A5OyEQvF2= MlLNV2FPT0WU
BT-20 NYnWT45lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwNki5NFIh|ryP NGTtU29USU6JRWK=
EGI-1 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwOES3NFEh|ryP MnfaV2FPT0WU
EW-16 NX3IepRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jDRmlEPTB;MT64OVE5OiEQvF2= M2HCN3NCVkeHUh?=
NCI-H2228 MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XsVmlEPTB;MT64OVIxOyEQvF2= M4\0U3NCVkeHUh?=
BB49-HNC MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorGTWM2OD1zLki4OlkzKM7:TR?= M2LMfHNCVkeHUh?=
G-402 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi2TWM2OD1zLki5O|k4KM7:TR?= M2e5dnNCVkeHUh?=
NCI-H526 M2Xyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFwOUGzPUDPxE1? NV;iW45vW0GQR1XS
ME-180 MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwOUO0O|ch|ryP NETWWmNUSU6JRWK=
PFSK-1 NGDuNVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwOUS0OVgh|ryP MoTKV2FPT0WU
TYK-nu M{foSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGq3eJBKSzVyPUGuPVU5OjNizszN NGn6O25USU6JRWK=
HOS M{W5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnTUpdxUUN3ME2xMlk4QTR6IN88US=> MY\TRW5ITVJ?
T98G MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS1eYVKSzVyPUGuPVkxODZizszN MnH4V2FPT0WU
SK-MES-1 NFW5TI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTtTW1KSzVyPUKuNFE{OzJizszN NHXpfIdUSU6JRWK=
SNB75 MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvBcIpKSzVyPUKuNFE2PDFizszN MV;TRW5ITVJ?
LAMA-84 NHnMWJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\WemlEPTB;Mj6wNlY5QSEQvF2= M3v5VXNCVkeHUh?=
CAL-39 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq2N5ZKSzVyPUKuNFMzQCEQvF2= M1jVcXNCVkeHUh?=
LOXIMVI NG\JTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJwMESwPFQh|ryP M1TTb3NCVkeHUh?=
NH-12 NFfDWVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJwMEW0NlQh|ryP NIO4WWNUSU6JRWK=
NCI-H1048 NIr3N2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXaSZo5UUN3ME2yMlExPTJizszN M4Hme3NCVkeHUh?=
KS-1 NHXqUlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4W5e2lEPTB;Mj6xNVAxOSEQvF2= NFXqPIpUSU6JRWK=
NCI-N87 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTJwMUOzPFQh|ryP NEjJUZlUSU6JRWK=
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EW-11 NHjVRoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPnSIZmUUN3ME2xNU46PDd2IN88US=> MVLTRW5ITVJ?
LB2518-MEL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF{LkC1PUDPxE1? MVXTRW5ITVJ?
KALS-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTF{Lki1OVMh|ryP MV\TRW5ITVJ?
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SNU-C2B MkLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfF[|g5UUN3ME2xO{4xOjN5IN88US=> M4jjZ3NCVkeHUh?=
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OVCAR-3 NVPmUnY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M363dmlEPTB;MkCuOVgzOiEQvF2= NFvORXVUSU6JRWK=
HD-MY-Z Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm5TJJHUUN3ME2yNU4{Pjl4IN88US=> MYLTRW5ITVJ?
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SCH NVfrNm1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVW0OmVbUUN3ME2yNk41QTZizszN Mnr5V2FPT0WU
KARPAS-299 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ|LkO4PFch|ryP MX;TRW5ITVJ?
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CAL-85-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rNVmlEPTB;MkeuNlEyQCEQvF2= Mn\CV2FPT0WU
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NCI-H2170 NFjFd|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL1TmVKSzVyPUOxMlU4QDRizszN M1PJU3NCVkeHUh?=
ALL-PO NG\hVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iyNGlEPTB;M{GuPFQzQCEQvF2= M3HLbHNCVkeHUh?=
NCI-H661 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\xOoNKSzVyPUOyMlA3OjNizszN MVPTRW5ITVJ?
NCI-H2347 NVjwc45jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlX3TWM2OD1|Mj60PFM4KM7:TR?= NH;mNoNUSU6JRWK=
FTC-133 M12xdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWZZdKSzVyPUOyMlcxPiEQvF2= MVjTRW5ITVJ?
COLO-829 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfvfGdOUUN3ME2zN{4{PDZ5IN88US=> MnXhV2FPT0WU
GOTO Mn3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN|LkWyOVgh|ryP Mm\RV2FPT0WU
YAPC M{HsWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrhUZhVUUN3ME2zN{45OTV7IN88US=> Mk\LV2FPT0WU
LCLC-103H MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[wT|hKSzVyPUO0MlE3OjRizszN MYLTRW5ITVJ?
SiHa M1PyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTN2LkO4NVch|ryP NHnxfIlUSU6JRWK=
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NCI-SNU-1 NXPyZ4o2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTN3LkG3PUDPxE1? M3\Wd3NCVkeHUh?=
KNS-81-FD M2\v[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljtTWM2OD1|NT62OlMh|ryP NV3RNllNW0GQR1XS
SCC-9 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnSXotKSzVyPUO2MlcyPDZizszN NVrhXG41W0GQR1XS
SH-4 NHqzZ5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjkbYNKSzVyPUO2Mlc{KM7:TR?= MX;TRW5ITVJ?
HCC-1954 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7CTWM2OD1|Nz6yO|I6KM7:TR?= NI\wR2ZUSU6JRWK=
BALL-1 NGrXcWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLleVZNUUN3ME2zO{42OzF4IN88US=> NFrSNmNUSU6JRWK=
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SK-MEL-3 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\rSIc{UUN3ME2zPE4zOzl5IN88US=> NYi5ZopbW0GQR1XS
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RH-1 NGjsNItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR|LkS4N|Yh|ryP MonkV2FPT0WU
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... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase I study of GDC-0941 in patients with locally advanced or metastatic solid tumors, Non-Hodgkin's lymphoma, or multiple myeloma (MM) (expansion stage only) for which standard therapy either does not exist or has proven ineffective or intolerable is
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [2]

細胞株 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
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 48 and 72 hours
実験の流れ 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.

動物実験: [2]

動物モデル NCR nude mice implanted with MDA-MB-361.1 cells, and SCID, C.B-17/IcrHsd-Prkdcscid mice implanted subcutaneously with BT474-M1 cells
製剤 Dissolved in 10% DMSO, 5% Tween 20, 85% water
投薬量 ~150 mg/kg/day
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Pictilisib (GDC-0941) SDF
分子量 513.64
化学式

C23H27N7O3S2

CAS No. 957054-30-7
保管 3年-20℃
2年-80℃in solvent
別名 RG7321
溶解度 (25°C) * In vitro DMSO 44 mg/mL (85.66 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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.
化学名 2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidine

文献中の引用 (57)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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