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 M2rSSGtqdmG|ZTDBd5NigQ>? MVmxJIg> NYHIbZdNTE2VTx?= M37FeWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= Ml\VNVg4PTR4NUS=
Sf9 MX3LbY5ie2ViQYPzZZk> NYP1blZmOSCq MYnEUXNQ NXn3UnF7UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NWDsW3JrOTh5NUS2OVQ>
Sf9 NHjpTmhMcW6jc3WgRZN{[Xl? MnjvNUBp NVWwZpg1TE2VTx?= MmD2TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NITETWgyQDd3NE[1OC=>
Sf9 M3jJWWtqdmG|ZTDBd5NigQ>? NH:3V4syKGh? NXr3Ro52TE2VTx?= NYPqO3M3UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= M164UlE5PzV2NkW0
Sf9 NVTqNGc2U2mwYYPlJGF{e2G7 NHPUdFMyKGh? NFrhb|RFVVOR NWq1OGJSUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[Q>? MoP3NVg4PTR4NUS=
MDA-MB-361 Ml\ZSpVv[3Srb36gRZN{[Xl? M2[yUFIhcA>? NUOyZ281TE2VTx?= NV7VSYJtUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO MVOxPFc2PDZ3NB?=
PC3 M2SxTGZ2dmO2aX;uJGF{e2G7 M{Xy[FIhcA>? M4LQSWROW09? MWrJcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4udnWubDDoeY1idiCSQ{OgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODN5IN88US=> NF;KOJkyQDd3NE[1OC=>
U87MG NHrybWJHfW6ldHnvckBCe3OjeR?= MW[yJIg> NEnVVolFVVOR NW[4cWRzUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDJR|UxKG:oIECuNFQ3KM7:TR?= MX6xPFc2PDZ3NB?=
MDA-MB-361 MmHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\ocoo6PiCq NGr5NVhFVVOR NGrVdIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> MXOxPFc2PDZ3NB?=
A2780 NYXTZo9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1y4eVk3KGh? MlG4SG1UVw>? MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IIfpeIghWEmNM1PBJIFv\CCSVFXOJI12fGG2aX;uJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? NIPqW3UyQDd3NE[1OC=>
PC3 NHL2XFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrrPVYhcA>? NGG2UYtFVVOR M3jEeWlEPTB;MD6yPEDPxE1? NV3IWodDOTh5NUS2OVQ>
U87MG MnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnnPVYhcA>? Mln1SG1UVw>? NIj4PG5KSzVyPUCuPVUh|ryP NU\ZVnRCOTh5NUS2OVQ>
Sf9 MnjpT4lv[XOnIFHzd4F6 NInzOIc{OCCvaX6= MUfEUXNQ MXPJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiYX3veY51KG:oIFHUVEBkd26|dX3l[EB4cXSqIFnDOVAhd2ZiMD6wOFIh|ryP MlzUNlI2PDh|NEK=
RAW 264.7 NGXnd|BMcW6jc3WgRZN{[Xl? MlnWPVAhdWmw NX3KOmxkTE2VTx?= NEC0N3FKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjJ7ODFOwG0> NYjZOph1OjJ3NEizOFI>
Sf9 M1i1UGtqdmG|ZTDBd5NigQ>? NY\3ZlZ2OSCq NFrl[IxKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> MXWyN|U1ODZ2NR?=
Sf9 M4jSb2tqdmG|ZTDBd5NigQ>? MUixJIg> M1;OZmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tl\Wy2YTDlfJBz\XO|ZXS= NXfLSpFUOjN3NEC2OFU>
Sf9 MoPST4lv[XOnIFHzd4F6 MlnQNUBp NXq4fZlJUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2ejbX3hJIV5eHKnc4Pl[C=> M1jWd|I{PTRyNkS1
Sf9 M37He2tqdmG|ZTDBd5NigQ>? MWqxJIg> NYjqXI1iUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2GucHjhJIV5eHKnc4Pl[C=> NWPNTYJLOjN3NEC2OFU>
SKOV3 NEewWIRMcW6jc3WgRZN{[Xl? MkmxNUDPxE1? Mn7aNUBp MmXjSG1UVw>? NYXuVVZCUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbh?= MnzaNlM{PjB|NEi=
MCF7 M{nWXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rpUVEh|ryP M1X2OVk3KGh? NV;RdYNtTE2VTx?= NUO3PXljT0l3ME2wMlA4ODJizszN NWXDRmp4OjN|NkCzOFg>
SKOV3 M2n0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDCe|ViOSEQvF2= MlPrPVYhcA>? M2HJdmROW09? MlL5S2k2OD1yLkG0O|Yh|ryP NILVe4gzOzN4MEO0PC=>
PC3 NF63fFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37FNVczKGh? MkfESG1UVw>? NVvUdmp1UUN3ME2wMlI5KM7:TR?= MoDiNlE6QDF5MUS=
MCF7.1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj6O|IhcA>? NIjHdG1FVVOR NH;2W4JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKEiHUkKg[4Vv\SC5aYToJGlEPTBib3[gNE4zQCEQvF2= NH3Ic4szOTl6MUexOC=>
MCF7-neo/Her2 NWHleI5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPuNYRyPzJiaB?= NFPnWpBFVVOR MoK3TWM2OD1yLkK5JO69VQ>? NX\IPJdLOjN4NkK5NFM>
MCF7-neo/Her2 M{SxR2tqdmG|ZTDBd5NigQ>? MnjqTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC5aYToJGlEPTBib3[gNE4xODdizszN NITaUpAzOzZ4MkmwNy=>
PC3 M2H1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3YboU4OiCq Mn7KSG1UVw>? Mmj6SWM2OD1yLkO0JO69VQ>? M2jMeVIyQTh3NkO5
MCF7.1 MoLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPtO|IhcA>? NUHHb5M3TE2VTx?= NH7ZPG9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDFR|UxKG:oIECuN|kh|ryP NV3nWpo{OjF7OEW2N|k>
PC3 MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq3NkBp M2Dre2ROW09? M3zKS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHTl[olkcWWwdDDpckBRXEWQIIfpeIghUUN3MDDv[kAxNjN7IN88US=> MYGyNFA2ODZ4OR?=
MCF7.1 NFPwfo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHm[ZdlPzJiaB?= NFjjXHBFVVOR MlX4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? MYSyNFA2ODZ4OR?=
MCF7.1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS2[pc4OiCq NWHjfIRZTUN3ME2wMlczKM7:TR?= NXHzW4xMOjB|NE[2OVY>
NCI-H1975 M{POWGN6fG:2b4jpZ{BCe3OjeR?= NGexV3E4OiCq NGfndmVKSzVyPUCuNlch|ryP MoS3NlMxPTl3NEW=
H460 M1;3dGN6fG:2b4jpZ{BCe3OjeR?= MUC3NkBp M{T6[mlEPTB;MD64O{DPxE1? MVSyN|A2QTV2NR?=
HT-29 NHyyO3hEgXSxdH;4bYMhSXO|YYm= MXW3NkBp MoToTWM2OD1yLk[2JO69VQ>? NGLLXm4zOzB3OUW0OS=>
HepG2 M{PTZ2N6fG:2b4jpZ{BCe3OjeR?= MV63NkBp M4HhZWlEPTB;MTFOwG0> NFrINWozOzB3OUW0OS=>
SGC7901 MmjCR5l1d3SxeHnjJGF{e2G7 Mm[0O|IhcA>? M4jW[GlEPTB;MT64JO69VQ>? NGrNWJMzOzB3OUW0OS=>
NCI-H226 M1[zb2N6fG:2b4jpZ{BCe3OjeR?= NHHWW3A4OiCq MnHGTWM2OD1{Lkmg{txO M1rZNFI{ODV7NUS1
A549 M3rWc2N6fG:2b4jpZ{BCe3OjeR?= NEjm[lE4OiCq M{P0[mlEPTB;Nj65JO69VQ>? NInlUWgzOzB3OUW0OS=>
U87MG M1v2Z2N6fG:2b4jpZ{BCe3OjeR?= MUW3NkBp NFjteYxKSzVyPUeuO|ch|ryP NVXFfIFkOjNyNUm1OFU>
HBC4 NGPQdplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmzWlQ{dG:pR1m1NF0uPi5yMzDN M2PjNFIzOzN4MkS2
BSY1 Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPlPIJtd2eJSUWwQU03NjlyIF2= NU\qS5M6OjJ|M{[yOFY>
HBC5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm0RWZXdG:pR1m1NF0uPi54MDDN MY[yNlM{PjJ2Nh?=
MCF7 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDacI9oT0l3ME2tO{4{OyCP NHf6d5czOjN|NkK0Oi=>
MDA-MB-231 M3vUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TGOYxw\0eLNUC9MVUvPDZiTR?= NHTDW2QzOjN|NkK0Oi=>
U251 NVjTO3FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLzcI9oT0l3ME2tOU42OCCP M2KyS|IzOzN4MkS2
SF268 NVnNfFdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS5c5pidG:pR1m1NF0uPS5|OTDN MYGyNlM{PjJ2Nh?=
SF295 NFTSWnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;qelVodG:pR1m1NF0uPi5|NzDN MY[yNlM{PjJ2Nh?=
SF539 MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXCfJk3dG:pR1m1NF0uPi53MDDN M2WzW|IzOzN4MkS2
SNB75 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\sc4dIUTVyPT23MlExKE1? MmnRNlI{OzZ{NE[=
SNB78 M1fWfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XGTIxw\0eLNUC9MVYvPTJiTR?= M{DPfVIzOzN4MkS2
HCC2998 NF3OSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jJWIxw\0eLNUC9MVYvOjliTR?= NXrhOlhPOjJ|M{[yOFY>
KM12 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWSy[mxOdG:pR1m1NF0uPS55NjDN MmLBNlI{OzZ{NE[=
HT-29 NHTQb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXsc4dIUTVyPT22MlMxKE1? MnnoNlI{OzZ{NE[=
HCT15 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq5bWJPdG:pR1m1NF0uPi5zMjDN NXvTXWlXOjJ|M{[yOFY>
HCT116 NG\DNmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;tWXZIdG:pR1m1NF0uPS56NzDN MoDoNlI{OzZ{NE[=
NCI-H23 NWPKcHJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzHcI9oT0l3ME2tOU44OyCP NYXpeYhwOjJ|M{[yOFY>
NCI-H226 NYrJ[nNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjtcI9oT0l3ME2tOk4zOSCP M1HOZ|IzOzN4MkS2
NCI-H522 NH3DcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjsc4dIUTVyPT22MlU5KE1? MWGyNlM{PjJ2Nh?=
NCI-H483 NEXBcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jYeoxw\0eLNUC9MVYvPTZiTR?= NIXJ[oIzOjN|NkK0Oi=>
A549 M4rQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfHVGNtd2eJSUWwQU03NjF3IF2= NXTHenNqOjJ|M{[yOFY>
DMS273 MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnlcoFGdG:pR1m1NF0uPi52MzDN M4D4bVIzOzN4MkS2
DMS114 NFzYNINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDkcI9oT0l3ME2tOU46OiCP NFrhd5AzOjN|NkK0Oi=>
LOXIMVI MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDtdGxtd2eJSUWwQU03NjJ7IF2= MXGyNlM{PjJ2Nh?=
OVCAR3 NXviS|A6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrEZXAxdG:pR1m1NF0uPi55MTDN M2H6[|IzOzN4MkS2
OVCAR4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrwboptd2eJSUWwQU02Njd4IF2= M4Ly[|IzOzN4MkS2
OVCAR5 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz3cI9oT0l3ME2tOk4zPiCP NYPZRWtmOjJ|M{[yOFY>
OVCAR8 NX;3UXE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXncI9oT0l3ME2tOU44OyCP NWjqO4g3OjJ|M{[yOFY>
SKOV3 M1TlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HTcIxw\0eLNUC9MVYvPTJiTR?= MUSyNlM{PjJ2Nh?=
RXF631L NG[wNnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLucI9oT0l3ME2tOk45QCCP NH3yRXczOjN|NkK0Oi=>
ACHN NH3IW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXYZoptd2eJSUWwQU03NjB5IF2= NFLleGIzOjN|NkK0Oi=>
St-4 NXr2[XcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP3cI9oT0l3ME2tOU42PiCP NYS1b3pQOjJ|M{[yOFY>
MKN1 NGDL[nBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HrRoxw\0eLNUC9MVcvODhiTR?= M37TNFIzOzN4MkS2
MKN7 M3z4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XRWIxw\0eLNUC9MVYvPTBiTR?= MnfiNlI{OzZ{NE[=
MKN28 MnvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILxRXJtd2eJSUWwQU02NjV{IF2= MU[yNlM{PjJ2Nh?=
MKN45 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rye4xw\0eLNUC9MVYvPTViTR?= NUPNPZB7OjJ|M{[yOFY>
MKN74 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrsc4dIUTVyPT22MlAzKE1? NWPsN3VwOjJ|M{[yOFY>
DU145 NIf2XFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjKcI9oT0l3ME2tOU45PSCP M3zIN|IzOzN4MkS2
PC3 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;qNHBtd2eJSUWwQU03NjZ4IF2= NWDVUmh7OjJ|M{[yOFY>
ES5 MoXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjyWIdKSzVyPUWwMlIyKG6P Ml72V2FPT0WU
HH MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS0THlKSzVyPUGxNU4xQCCwTR?= MULTRW5ITVJ?
MHH-PREB-1 NEnmfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjBTWM2OD1zMUSuN{BvVQ>? M4TDcnNCVkeHUh?=
NCI-H1770 NYHGOpoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TW[GlEPTB;MUKzMlg3KG6P MkfKV2FPT0WU
HuO9 M3;QNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJyNj6wNkBvVQ>? MW\TRW5ITVJ?
HAL-01 M3XiW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zDWWlEPTB;MkC2Mlc{KG6P NFHSW3BUSU6JRWK=
NOS-1 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJzMT64NkBvVQ>? MmTDV2FPT0WU
HGC-27 MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjQfplKSzVyPUKxNk42PyCwTR?= NFrYPZZUSU6JRWK=
NB69 M3jDWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvUUlNIUUN3ME2yOFUvOjdibl2= MoS1V2FPT0WU
RS4-11 M2rtbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWwcYdKSzVyPUK2NU44PiCwTR?= M{DQdHNCVkeHUh?=
DOK NXrP[mo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjLWY9KSzVyPUOwNU44KG6P NF3LWHlUSU6JRWK=
LB2241-RCC MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nyemlEPTB;M{CzMlg1KG6P MnK5V2FPT0WU
NCI-H1623 MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfJNlBKSzVyPUOwOE4xQCCwTR?= MnjMV2FPT0WU
YH-13 MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrVVI1KSzVyPUOwOE4{OiCwTR?= NGrjRndUSU6JRWK=
BPH-1 M1HRNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnO1TWM2OD1|MUSgcm0> M2DvN3NCVkeHUh?=
AN3-CA NYi3R29MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN2MD6zO{BvVQ>? MVzTRW5ITVJ?
ES7 NFXKTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fr[GlEPTB;M{SxMlk6KG6P MXfTRW5ITVJ?
MDA-MB-175-VII NUfUVXBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjGN2xnUUN3ME2zOVIvQTJibl2= NFvqUGxUSU6JRWK=
GAMG NYDXOFg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTN5MD64OUBvVQ>? Ml\qV2FPT0WU
CHL-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6zZW5KSzVyPUO3PE43PSCwTR?= NILVcWVUSU6JRWK=
NB7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDXTWM2OD1|OEmuPFMhdk1? NWO4UopGW0GQR1XS
MFE-280 NI\tSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTRzOD6yJI5O MV\TRW5ITVJ?
HL-60 M4XlbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPJUIFKSzVyPUSyOU44PSCwTR?= NVPOPZFyW0GQR1XS
GCIY M2C4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTR|Mz64JI5O NVPzdXZXW0GQR1XS
MDA-MB-361 NHjDdmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTR|OT6xN{BvVQ>? MVXTRW5ITVJ?
LXF-289 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTR2OD6yO{BvVQ>? MV3TRW5ITVJ?
NBsusSR MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPSTGtKSzVyPUS4PE45PSCwTR?= MVfTRW5ITVJ?
KU-19-19 NUn6PJE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjJcGhrUUN3ME21NVYvODdibl2= MmHRV2FPT0WU
A204 NFz1RZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jhRmlEPTB;NUKyMlM{KG6P NIPndXpUSU6JRWK=
LB1047-RCC M4WzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rteGlEPTB;NUKyMlk{KG6P NFTofWJUSU6JRWK=
COLO-684 MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX4RopKSzVyPUWyN{4yOSCwTR?= M3zRVnNCVkeHUh?=
PA-1 M{Pkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLjTWM2OD13M{KuOFEhdk1? M1TBW3NCVkeHUh?=
MG-63 NHjjO|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTV2MT6xNUBvVQ>? MmPPV2FPT0WU
BHT-101 Mke1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvDVlNKSzVyPUW0OE46PCCwTR?= NF3KWpVUSU6JRWK=
NKM-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjpRlN4UUN3ME21PVMvODlibl2= M1LuSnNCVkeHUh?=
T47D M3\kUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXDUppKSzVyPUW5O{42PiCwTR?= NELFPWRUSU6JRWK=
MOLT-4 NHjsSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTZ{Mz62NkBvVQ>? NUDjZYMyW0GQR1XS
IGROV-1 NED6fZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT5OZUzUUN3ME22N|QvOzFibl2= M1;WPXNCVkeHUh?=
ES4 NXG0eWNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjD[YtHUUN3ME22N|kvPTRibl2= M1T6eXNCVkeHUh?=
HuO-3N1 M17ncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonvTWM2OD14NEKuN|ghdk1? NULBPFN7W0GQR1XS
NEC8 NGDURmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HocGlEPTB;NkWzMlU4KG6P MoHSV2FPT0WU
HO-1-N-1 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonLTWM2OD14NUmuNVchdk1? NXLmXVVnW0GQR1XS
EPCL-272H NXWxOXRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vvRWlEPTB;Nki3MlIyKG6P M1LudHNCVkeHUh?=
D-263MG M4TxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHBWZdKSzVyPUexPE4yKG6P MXPTRW5ITVJ?
MV-4-11 M4HHOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7acVloUUN3ME23NlQvOzFibl2= Mm\TV2FPT0WU
SK-NEP-1 M1\UZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T3WmlEPTB;N{K1Mlk1KG6P NYn4[YNDW0GQR1XS
SW872 NFTaZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLZTWM2OD15MkeuPFkhdk1? NGT0boxUSU6JRWK=
P30-OHK NUfE[ndkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTd|MD63NUBvVQ>? NIK4eZNUSU6JRWK=
OMC-1 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTd3MT6wPUBvVQ>? M2\zUHNCVkeHUh?=
LoVo MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX2PXpKSzVyPUe3O{46KG6P MV7TRW5ITVJ?
LNCaP-Clone-FGC NF21ZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7BN|JKSzVyPUe5Ok4{PCCwTR?= MW\TRW5ITVJ?
L-363 NW\MfIJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKyTWM2OD15OUiuOFIhdk1? MlLsV2FPT0WU
ES8 M2S3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfWO4tKSzVyPUixNE42OiCwTR?= MlTkV2FPT0WU
697 M2D4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi5eodnUUN3ME24N|EvPTVibl2= MXHTRW5ITVJ?
HSC-3 NYD3O5dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTh|OT61OEBvVQ>? NGHO[ZlUSU6JRWK=
H4 M3HzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rxbmlEPTB;OEWwMlg2KG6P M2jHZXNCVkeHUh?=
QIMR-WIL MorIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7BNZpXUUN3ME24OlUvOiCwTR?= MlvkV2FPT0WU
OAW-42 NWnGc|dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjZ[ldKSzVyPUi3Nk4yQSCwTR?= MXzTRW5ITVJ?
MCF7 NYO4cVdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXY[nNLUUN3ME24PVgvPTlibl2= NHi2folUSU6JRWK=
SCC-25 M3:yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUKwWpRxUUN3ME25NVQvOTlibl2= M{nVNnNCVkeHUh?=
NCI-H1563 NEnocodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\wTWM2OD17MUWuPVkhdk1? MUTTRW5ITVJ?
OVCAR-5 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvKXYRKSzVyPUm0NE4yPyCwTR?= M3\DOHNCVkeHUh?=
HDLM-2 MofPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vsUmlEPTB;OUS5MlIhdk1? MXzTRW5ITVJ?
NB5 M1r5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPxTWM2OD17NU[uOkBvVQ>? NYfj[YdCW0GQR1XS
NCI-H292 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfaTWM2OD17N{SuN|Ihdk1? MknpV2FPT0WU
A101D MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LOcGlEPTB;OUmwMlE6KG6P MVPTRW5ITVJ?
NCI-H1648 M{LzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4Z2FvUUN3ME25PVgvPTFibl2= M{XrNHNCVkeHUh?=
EKVX NHTsdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7FeXhZUUN3ME2xMlAyOjlizszN MnvSV2FPT0WU
SW1710 NX3ySJQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nVTmlEPTB;MT6wOFI{OyEQvF2= NELid2NUSU6JRWK=
WM-115 NEKyUHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTFwME[2OVYh|ryP MWrTRW5ITVJ?
CAL-54 NI\YfYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDBVnBKSzVyPUGuNFcxQDFizszN MVLTRW5ITVJ?
TGBC24TKB NYfrUGltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLzTWM2OD1zLkC4NFQ2KM7:TR?= NVntW481W0GQR1XS
NCI-H520 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XHNWlEPTB;MT6wPFk3PyEQvF2= M3\venNCVkeHUh?=
D-423MG NH;kblVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jpW2lEPTB;MT6wPVk3OiEQvF2= NEHCbJVUSU6JRWK=
BFTC-905 NUjGeZV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFwMUO0OFkh|ryP MV\TRW5ITVJ?
HT M3vsbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;STmVKSzVyPUGuNVM1PzhizszN MULTRW5ITVJ?
CTB-1 MoPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7nUWw{UUN3ME2xMlE1Ojl|IN88US=> NEm1d4lUSU6JRWK=
Hs-578-T MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjXN2JKSzVyPUGuNVk2PjVizszN MXjTRW5ITVJ?
HuH-7 M17tcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjTd|dKSzVyPUGuNlA6PDlizszN NELFflZUSU6JRWK=
LB996-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrlTWM2OD1zLkKyNVc4KM7:TR?= NXvET5dpW0GQR1XS
KYSE-270 Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXQXXZXUUN3ME2xMlI6PzN2IN88US=> M4fLWXNCVkeHUh?=
A4-Fuk NEXQU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOwTWM2OD1zLkK5PVk{KM7:TR?= NVHneGdGW0GQR1XS
A498 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;RPYVKSzVyPUGuN|A1PzRizszN MWHTRW5ITVJ?
SK-MEL-1 M2DRN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLXbmZKSzVyPUGuN|A3PzlizszN MmfhV2FPT0WU
AU565 M36zfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFwM{G4OlMh|ryP MXfTRW5ITVJ?
Saos-2 M{nXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTTTWM2OD1zLkOzNlA2KM7:TR?= NYD4R3pPW0GQR1XS
A549 NXiwVo9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvk[lNvUUN3ME2xMlM6QTdizszN MUPTRW5ITVJ?
BFTC-909 NHLob45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHRV3cxUUN3ME2xMlQ{OzB3IN88US=> NVLYS|lSW0GQR1XS
MDA-MB-415 MnG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7sd5hKUUN3ME2xMlQ5Pjl{IN88US=> MlrsV2FPT0WU
639-V MmDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvOVHg4UUN3ME2xMlUxOjR3IN88US=> MlvOV2FPT0WU
A704 NUj3emNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwNUC3PFUh|ryP MUPTRW5ITVJ?
PANC-03-27 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zPdmlEPTB;MT61NVQxQCEQvF2= MYXTRW5ITVJ?
SK-MEL-28 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPwTWM2OD1zLkW2NFg2KM7:TR?= MU\TRW5ITVJ?
Ramos-2G6-4C10 NWDxXGgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjTem9sUUN3ME2xMlYxPzR4IN88US=> NHHwZotUSU6JRWK=
HuP-T4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwNkC3O|gh|ryP MnrxV2FPT0WU
VA-ES-BJ MmTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS5dVhKSzVyPUGuOlEzPyEQvF2= NEi5d3pUSU6JRWK=
EFM-19 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzhVodKSzVyPUGuOlE5OSEQvF2= MWTTRW5ITVJ?
G-401 NULhVZd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe1[ZJKSzVyPUGuOlIyPjRizszN MoTTV2FPT0WU
D-566MG MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP2SYZKSzVyPUGuOlI2OyEQvF2= MoPqV2FPT0WU
JVM-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS5UJNmUUN3ME2xMlY1QDd3IN88US=> MnjzV2FPT0WU
TK10 NGDtTnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LBTmlEPTB;MT62O|A5OyEQvF2= NEm3OpBUSU6JRWK=
BT-20 NYPz[nFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfDVI5KSzVyPUGuOlg6ODJizszN NYCyZXI4W0GQR1XS
EGI-1 NWjEOmpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGyeoFuUUN3ME2xMlg1PzBzIN88US=> M4CzO3NCVkeHUh?=
EW-16 NELKfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS5TWM2OD1zLki1NVgzKM7:TR?= NWjYWXZpW0GQR1XS
NCI-H2228 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTxSphJUUN3ME2xMlg2OjB|IN88US=> NHP3[ZBUSU6JRWK=
BB49-HNC NHTtTIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\mWHJKSzVyPUGuPFg3QTJizszN MWHTRW5ITVJ?
G-402 M1jCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTFwOEm3PVch|ryP MU\TRW5ITVJ?
NCI-H526 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\0emlEPTB;MT65NVM6KM7:TR?= MXvTRW5ITVJ?
ME-180 NVzDNHdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;ETWM2OD1zLkmzOFc4KM7:TR?= MVrTRW5ITVJ?
PFSK-1 M{D2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX4WoJJUUN3ME2xMlk1PDV6IN88US=> M1y5UnNCVkeHUh?=
TYK-nu NGCyfZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwOUW4NlMh|ryP NFy4dJVUSU6JRWK=
HOS MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HQd2lEPTB;MT65O|k1QCEQvF2= MXvTRW5ITVJ?
T98G MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnmWHlKUUN3ME2xMlk6ODB4IN88US=> NGq1Z2pUSU6JRWK=
SK-MES-1 NIX5S|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zBXWlEPTB;Mj6wNVM{OiEQvF2= NYLUTJBIW0GQR1XS
SNB75 NF7ZVVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXITWM2OD1{LkCxOVQyKM7:TR?= NFPIZWJUSU6JRWK=
LAMA-84 NHPSSGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJwMEK2PFkh|ryP NXHz[4VpW0GQR1XS
CAL-39 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJwMEOyPEDPxE1? Mmj1V2FPT0WU
LOXIMVI MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rYfWlEPTB;Mj6wOFA5PCEQvF2= MnLVV2FPT0WU
NH-12 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7OenRKSzVyPUKuNFU1OjRizszN NXrPOIg{W0GQR1XS
NCI-H1048 M4mzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7lRXZKSzVyPUKuNVA2OiEQvF2= MVHTRW5ITVJ?
KS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXwXXBKSzVyPUKuNVExODFizszN NF;JXlNUSU6JRWK=
NCI-N87 M4Dzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j1c2lEPTB;Mj6xN|M5PCEQvF2= MoS2V2FPT0WU
CHP-212 NYn0N4hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJwMUi0OFIh|ryP M2\S[XNCVkeHUh?=
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NCI-H441 NV7rb3F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXpfHg3UUN3ME2yOU44PDZ3IN88US=> NFPFfYZUSU6JRWK=
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RKO NX;u[VRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDpTWM2OD1{Nj63OlMzKM7:TR?= NGXPVXZUSU6JRWK=
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CAL-120 NVzUcXZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\sTWM2OD1{Nz62PVE1KM7:TR?= MVLTRW5ITVJ?
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S-117 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfs[o5KSzVyPUK5MlM5PTdizszN M3XIbnNCVkeHUh?=
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HCT-116 NH3QdIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTNyLkW1OVQh|ryP NIPJ[|dUSU6JRWK=
NCI-H1693 NWjKcXVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PsPGlEPTB;M{CuOVk1OiEQvF2= MlfmV2FPT0WU
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NCI-H2170 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTNzLkW3PFQh|ryP NFLnNI5USU6JRWK=
ALL-PO M4ntdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjl[2tKSzVyPUOxMlg1OjhizszN NYCyXFljW0GQR1XS
NCI-H661 NHy4ZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzWNXZKSzVyPUOyMlA3OjNizszN NFrFNVJUSU6JRWK=
NCI-H2347 NYfZS2g{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTN{LkS4N|ch|ryP M37ubHNCVkeHUh?=
FTC-133 M{SzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPSSGtMUUN3ME2zNk44ODZizszN MUjTRW5ITVJ?
COLO-829 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Psd2lEPTB;M{OuN|Q3PyEQvF2= NGrNeFZUSU6JRWK=
GOTO M{TaN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPWVXY3UUN3ME2zN{42OjV6IN88US=> Ml7JV2FPT0WU
YAPC M{XRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTN|LkixOVkh|ryP NXe0NohPW0GQR1XS
LCLC-103H NX\yTYxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M124SmlEPTB;M{SuNVYzPCEQvF2= NGruSplUSU6JRWK=
SiHa MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzrTWM2OD1|ND6zPFE4KM7:TR?= M1LmWnNCVkeHUh?=
LK-2 MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml36TWM2OD1|ND61O|A5KM7:TR?= MojpV2FPT0WU
KP-N-YS M3judGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHEeYNkUUN3ME2zOE44OjB{IN88US=> MoXLV2FPT0WU
NCI-SNU-1 NX\QTZcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN3LkG3PUDPxE1? NFnnXVdUSU6JRWK=
KNS-81-FD M1\vPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTN3Lk[2N{DPxE1? MXfTRW5ITVJ?
SCC-9 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTGUFVzUUN3ME2zOk44OTR4IN88US=> MVPTRW5ITVJ?
SH-4 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[w[GlEPTB;M{[uO|Mh|ryP MYrTRW5ITVJ?
HCC-1954 NVrtV5VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInsSY5KSzVyPUO3MlI4OjlizszN NGO1bodUSU6JRWK=
BALL-1 NVPGTZhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW3TWM2OD1|Nz61N|E3KM7:TR?= NYLvWFUyW0GQR1XS
BE-13 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;aPGJKSzVyPUO3MlcxOThizszN MUPTRW5ITVJ?
COLO-678 MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVK2XItmUUN3ME2zO{46PDN5IN88US=> NEPuR2hUSU6JRWK=
SK-MEL-3 NYTlcIxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXDTWM2OD1|OD6yN|k4KM7:TR?= M1vBO3NCVkeHUh?=
OAW-28 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIixOXVKSzVyPUO4MlY{QSEQvF2= NY\MVYNiW0GQR1XS
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C2BBe1 MlTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfKTWM2OD1|OT64NVgh|ryP M2nYOHNCVkeHUh?=
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KYSE-140 NFjYT|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTkb2J7UUN3ME20NE44OTZ3IN88US=> NUXZTXVQW0GQR1XS
MOLT-16 NIjBSVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPNV4VUUUN3ME20NU4yPTN4IN88US=> NVT0dVU1W0GQR1XS
CFPAC-1 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTR{LkWyNVEh|ryP Mn\rV2FPT0WU
NB14 MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR{LkewNlch|ryP MX\TRW5ITVJ?
COLO-792 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTR{Lki5OlEh|ryP NXfMbYVzW0GQR1XS
RH-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7Xc|BuUUN3ME20N{41QDN4IN88US=> MkjvV2FPT0WU
NCI-H522 M4m4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXGT2xKSzVyPUS0MlM2PjhizszN M{W1c3NCVkeHUh?=
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KGN MofNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTR6LkOwOlMh|ryP MXXTRW5ITVJ?
UACC-62 NYOwOG1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTR6LkSwO|Ih|ryP MVTTRW5ITVJ?
NCI-H358 MontS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTR7LkOwNVgh|ryP Mmn3V2FPT0WU
LS-411N MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\YTWM2OD12OT6zNVE5KM7:TR?= MnXzV2FPT0WU
IST-MES1 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[4TWM2OD12OT61OlI2KM7:TR?= Mlz5V2FPT0WU

... 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 (58)

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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