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

高品質保証

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Quality Control & MSDS

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、PI3Kα、PI3Kβ、PI3KδとPI3Kγの強力な阻害剤で、IC50 がそれぞれ 3 nM、 33 nM、 3 nM、75 nMです。
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 MXTLbY5ie2ViQYPzZZk> M{jGRlEhcA>? M1n1[GROW09? M2n1PWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= MYCxPFc2PDZ3NB?=
Sf9 MXTLbY5ie2ViQYPzZZk> NV3QOWpHOSCq M1vpVGROW09? NVWzbJExUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NVLEN5dROTh5NUS2OVQ>
Sf9 MYfLbY5ie2ViQYPzZZk> NGXaVIEyKGh? MVrEUXNQ MXvJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN NYfaWZlLOTh5NUS2OVQ>
Sf9 MVLLbY5ie2ViQYPzZZk> NX65V2ZWOSCq MXnEUXNQ M3rMRmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYnX0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wN|Mh|ryP NYfZOIlGOTh5NUS2OVQ>
Sf9 NEX2cm5McW6jc3WgRZN{[Xl? MkjYNUBp NIjPb2RFVVOR MnXzTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> MoHuNVg4PTR4NUS=
MDA-MB-361 MkTWSpVv[3Srb36gRZN{[Xl? MWGyJIg> MoPqSG1UVw>? M{fC[GlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvODJ6IN88US=> MU[xPFc2PDZ3NB?=
PC3 MonxSpVv[3Srb36gRZN{[Xl? NYTCbWR2OiCq M3T2RmROW09? NH;ibIVKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? NYTTclduOTh5NUS2OVQ>
U87MG NXP4RWd{TnWwY4Tpc44hSXO|YYm= NUTnfIoxOiCq MV3EUXNQ MmTQTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? NHPB[GkyQDd3NE[1OC=>
MDA-MB-361 NG[2dJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPTe2w6PiCq NVq2RndjTE2VTx?= M4D1dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvPzJizszN MYmxPFc2PDZ3NB?=
A2780 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLVbWE6PiCq M1S2VmROW09? MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IIfpeIghWEmNM1PBJIFv\CCSVFXOJI12fGG2aX;uJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? MX:xPFc2PDZ3NB?=
PC3 NYrBRXNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnLPVYhcA>? MVnEUXNQ NXK1PIxNUUN3ME2wMlI5KM7:TR?= NHXGXlAyQDd3NE[1OC=>
U87MG NX\SVlBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;RPVYhcA>? MmHwSG1UVw>? MVPJR|UxRTBwOUWg{txO NGnSRnoyQDd3NE[1OC=>
Sf9 M1z2RmtqdmG|ZTDBd5NigQ>? NVvGSlNxOzBibXnu MnG4SG1UVw>? Mn7UTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= NEnsd4UzOjV2OEO0Ni=>
RAW 264.7 NV7DPHluU2mwYYPlJGF{e2G7 NWrLOZZVQTBibXnu MnvHSG1UVw>? M3z6S2lvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvOjl6IN88US=> M1;iSVIzPTR6M{Sy
Sf9 NXLqOJZ2U2mwYYPlJGF{e2G7 NU\iW2pNOSCq M2m2NmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tj\XSjIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVRkmgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODF5IN88US=> M{G0OVI{PTRyNkS1
Sf9 M4CxN2tqdmG|ZTDBd5NigQ>? M172blEhcA>? Mk\CTY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= MlKwNlM2PDB4NEW=
Sf9 MmTZT4lv[XOnIFHzd4F6 NEe1XZMyKGh? MX3Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[4FudWFiZYjwdoV{e2Wm NEnTeZUzOzV2ME[0OS=>
Sf9 NU[5R2JbU2mwYYPlJGF{e2G7 NXj2NWZTOSCq MWrJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm NITMTmQzOzV2ME[0OS=>
SKOV3 NYjBd5hCU2mwYYPlJGF{e2G7 MX2xJO69VQ>? M4frZlEhcA>? NFvNeG9FVVOR MnXMTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? M4\nWFI{OzZyM{S4
MCF7 NYrPNnF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxJO69VQ>? Ml\NPVYhcA>? M1P5[2ROW09? M3nmfWdKPTB;MD6wO|AzKM7:TR?= NHjvb2wzOzN4MEO0PC=>
SKOV3 NYrvdpZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOxJO69VQ>? M3\mSVk3KGh? NF;pdnVFVVOR NVTtfHRjT0l3ME2wMlE1PzZizszN MVqyN|M3ODN2OB?=
PC3 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVq3NkBp M{OzPWROW09? NHXtNHdKSzVyPUCuNlgh|ryP Mk[xNlE6QDF5MUS=
MCF7.1 NH;YbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17QR|czKGh? MUnEUXNQ NHP2XldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKEiHUkKg[4Vv\SC5aYToJGlEPTBib3[gNE4zQCEQvF2= M4DqNFIyQThzN{G0
MCF7-neo/Her2 NY[5e5RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG4XlU4OiCq MmXaSG1UVw>? NWrM[nhuUUN3ME2wMlI6KM7:TR?= MoPkNlM3PjJ7MEO=
MCF7-neo/Her2 NI\MbpVMcW6jc3WgRZN{[Xl? NX7mSJNpUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO NF3Jd20zOzZ4MkmwNy=>
PC3 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX63NkBp NUHTPWdsTE2VTx?= M13URmVEPTB;MD6zOEDPxE1? MnW4NlE6QDV4M{m=
MCF7.1 NHu2e3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:3NkBp MULEUXNQ NGS1O25CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDFR|UxKG:oIECuN|kh|ryP M2C4W|IyQTh3NkO5
PC3 M4X2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPhdFRNPzJiaB?= MXrEUXNQ MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCmZX\pZ4lmdnRiaX6gVHRGViC5aYToJGlEPTBib3[gNE4{QSEQvF2= NX70ZoNUOjByNUC2Olk>
MCF7.1 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLjR4w4OiCq NVfsbG5tTE2VTx?= MkHsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? MUWyNFA2ODZ4OR?=
MCF7.1 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjwWZhDPzJiaB?= M2\Rd2VEPTB;MD63NkDPxE1? NXqxdm1TOjB|NE[2OVY>
NCI-H1975 MXTDfZRwfG:6aXOgRZN{[Xl? MWi3NkBp M2CxR2lEPTB;MD6yO{DPxE1? MVKyN|A2QTV2NR?=
H460 MXfDfZRwfG:6aXOgRZN{[Xl? M{PmWlczKGh? MlHNTWM2OD1yLki3JO69VQ>? MX6yN|A2QTV2NR?=
HT-29 MmPtR5l1d3SxeHnjJGF{e2G7 Ml;aO|IhcA>? M4PsXmlEPTB;MD62OkDPxE1? M1XQb|I{ODV7NUS1
HepG2 NELkOlVEgXSxdH;4bYMhSXO|YYm= MkT3O|IhcA>? NGLRO45KSzVyPUGg{txO NEP0NGEzOzB3OUW0OS=>
SGC7901 Mn7GR5l1d3SxeHnjJGF{e2G7 M{nrUlczKGh? NGLwUZZKSzVyPUGuPEDPxE1? MkD6NlMxPTl3NEW=
NCI-H226 MUPDfZRwfG:6aXOgRZN{[Xl? NHvaPHk4OiCq MVzJR|UxRTJwOTFOwG0> MWiyN|A2QTV2NR?=
A549 NX3WWnZ4S3m2b4TvfIlkKEG|c3H5 MUW3NkBp MnTqTWM2OD14Lkmg{txO MUmyN|A2QTV2NR?=
U87MG MVzDfZRwfG:6aXOgRZN{[Xl? MXS3NkBp NEjNW2pKSzVyPUeuO|ch|ryP MlnVNlMxPTl3NEW=
HBC4 M{XiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnSZo9HdG:pR1m1NF0uPi5yMzDN NED5PGozOjN|NkK0Oi=>
BSY1 M37iOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\ZPYhHdG:pR1m1NF0uPi57MDDN NFnq[HgzOjN|NkK0Oi=>
HBC5 NH;xXmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnsc4dIUTVyPT22MlYxKE1? MlO3NlI{OzZ{NE[=
MCF7 NI\CdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTsc4dIUTVyPT23MlM{KE1? NVHVXZVbOjJ|M{[yOFY>
MDA-MB-231 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7NPHJtd2eJSUWwQU02NjR4IF2= MVuyNlM{PjJ2Nh?=
U251 MnzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13iOoxw\0eLNUC9MVUvPTBiTR?= NUPjcIw5OjJ|M{[yOFY>
SF268 M3vkb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXXUW97dG:pR1m1NF0uPS5|OTDN NHvC[m8zOjN|NkK0Oi=>
SF295 NXnW[41YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfsc4dIUTVyPT22MlM4KE1? NVvZXFFvOjJ|M{[yOFY>
SF539 NHGyNotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfsc4dIUTVyPT22MlUxKE1? M{juOlIzOzN4MkS2
SNB75 M{PscWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojUcI9oT0l3ME2tO{4yOCCP NGLEVJkzOjN|NkK0Oi=>
SNB78 NVTmeGQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfVN2Ftd2eJSUWwQU03NjV{IF2= MlfjNlI{OzZ{NE[=
HCC2998 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDsc4dIUTVyPT22MlI6KE1? MUeyNlM{PjJ2Nh?=
KM12 NXHGSlRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\VTnp1dG:pR1m1NF0uPS55NjDN M3fGV|IzOzN4MkS2
HT-29 M1TBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe5S5htd2eJSUWwQU03NjNyIF2= NYfobpJuOjJ|M{[yOFY>
HCT15 NVrK[HlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTsc4dIUTVyPT22MlEzKE1? NF;ZS5IzOjN|NkK0Oi=>
HCT116 NHri[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnsc4dIUTVyPT21Mlg4KE1? NVTuc4FCOjJ|M{[yOFY>
NCI-H23 M4TzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXsc4dIUTVyPT21Mlc{KE1? MnLoNlI{OzZ{NE[=
NCI-H226 M{DlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3DcI9oT0l3ME2tOk4zOSCP Ml;0NlI{OzZ{NE[=
NCI-H522 Mny5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDuU|FWdG:pR1m1NF0uPi53ODDN M13IeFIzOzN4MkS2
NCI-H483 NEG5TXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPJN|VVdG:pR1m1NF0uPi53NjDN M{fp[FIzOzN4MkS2
A549 M4HqSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnxfFRGdG:pR1m1NF0uPi5zNTDN MX[yNlM{PjJ2Nh?=
DMS273 NVPHXYtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHNcI9oT0l3ME2tOk41OyCP NVn0dGs1OjJ|M{[yOFY>
DMS114 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnsc4dIUTVyPT21MlkzKE1? NHrNflQzOjN|NkK0Oi=>
LOXIMVI NWPMW|FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[zcYxtd2eJSUWwQU03NjJ7IF2= M4Lu[|IzOzN4MkS2
OVCAR3 NGW2fmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXDcI9oT0l3ME2tOk44OSCP NIXPcFEzOjN|NkK0Oi=>
OVCAR4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XSNYxw\0eLNUC9MVUvPzZiTR?= NHfQNGkzOjN|NkK0Oi=>
OVCAR5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrCT5Jtd2eJSUWwQU03NjJ4IF2= M1jTSlIzOzN4MkS2
OVCAR8 NF;rNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkO2cI9oT0l3ME2tOU44OyCP MmP0NlI{OzZ{NE[=
SKOV3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PWbYxw\0eLNUC9MVYvPTJiTR?= NGnYbZEzOjN|NkK0Oi=>
RXF631L M3[xUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvy[Ixtd2eJSUWwQU03Njh6IF2= M3v1UlIzOzN4MkS2
ACHN NYjsdnVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfWVIptd2eJSUWwQU03NjB5IF2= M4fwOFIzOzN4MkS2
St-4 M4n4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PSZoxw\0eLNUC9MVUvPTZiTR?= Ml3nNlI{OzZ{NE[=
MKN1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTsc4dIUTVyPT23MlA5KE1? M4XGNFIzOzN4MkS2
MKN7 M1fsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC0V45td2eJSUWwQU03NjVyIF2= M1rhZVIzOzN4MkS2
MKN28 NF\zXpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrsc4dIUTVyPT21MlUzKE1? M4HueVIzOzN4MkS2
MKN45 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W3S4xw\0eLNUC9MVYvPTViTR?= NFvBeYszOjN|NkK0Oi=>
MKN74 NXf6cow{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DVW4xw\0eLNUC9MVYvODJiTR?= M1TEOVIzOzN4MkS2
DU145 M{PUTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLscI9oT0l3ME2tOU45PSCP NXv0bZZrOjJ|M{[yOFY>
PC3 MlTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jQfIxw\0eLNUC9MVYvPjZiTR?= M1f1R|IzOzN4MkS2
ES5 M3zRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGwfYVKSzVyPUWwMlIyKG6P MV\TRW5ITVJ?
HH MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFzMT6wPEBvVQ>? NG[xS5FUSU6JRWK=
MHH-PREB-1 NXjqTIlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[yTHFKSzVyPUGxOE4{KG6P MXjTRW5ITVJ?
NCI-H1770 NVrTd2N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\ySWlEPTB;MUKzMlg3KG6P M1nrTnNCVkeHUh?=
HuO9 M4HGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXj[HFFUUN3ME2yNFYvODJibl2= NFrRenVUSU6JRWK=
HAL-01 NVm5fVN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV35V4c3UUN3ME2yNFYvPzNibl2= MYHTRW5ITVJ?
NOS-1 NYDmOYVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJzMT64NkBvVQ>? MUDTRW5ITVJ?
HGC-27 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\pZXBZUUN3ME2yNVIvPTdibl2= NG\HUYNUSU6JRWK=
NB69 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7IcXFlUUN3ME2yOFUvOjdibl2= MUPTRW5ITVJ?
RS4-11 NHXNd4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jEbGlEPTB;Mk[xMlc3KG6P NVfKe4dbW0GQR1XS
DOK M1PVe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTNyMT63JI5O NYDvdo9rW0GQR1XS
LB2241-RCC NV;MPHRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2e2dWlEPTB;M{CzMlg1KG6P NIC1SW5USU6JRWK=
NCI-H1623 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHqTWM2OD1|MESuNFghdk1? NWLrc4hLW0GQR1XS
YH-13 NWDU[oRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\nc2VKSzVyPUOwOE4{OiCwTR?= MlqzV2FPT0WU
BPH-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rXbWlEPTB;M{G0JI5O NU\VNIt4W0GQR1XS
AN3-CA NXW0Xmx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\r[49bUUN3ME2zOFAvOzdibl2= M3zi[3NCVkeHUh?=
ES7 M2jiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPrU4ZKSzVyPUO0NU46QSCwTR?= MoC3V2FPT0WU
MDA-MB-175-VII NVj3U4RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\pTWM2OD1|NUKuPVIhdk1? MVXTRW5ITVJ?
GAMG NX7FN3JyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXqTWM2OD1|N{CuPFUhdk1? NGPRcoRUSU6JRWK=
CHL-1 Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K1S2lEPTB;M{e4MlY2KG6P MoW1V2FPT0WU
NB7 NIHLS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\KTWM2OD1|OEmuPFMhdk1? NXrZcnRFW0GQR1XS
MFE-280 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXyTWM2OD12MUiuNkBvVQ>? M2LMb3NCVkeHUh?=
HL-60 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PXbGlEPTB;NEK1Mlc2KG6P NVfHPYRzW0GQR1XS
GCIY NFn3TmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR|Mz64JI5O NG\GTItUSU6JRWK=
MDA-MB-361 NXHJT5ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr4XnF1UUN3ME20N|kvOTNibl2= MYfTRW5ITVJ?
LXF-289 NH25VFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LMRmlEPTB;NES4MlI4KG6P NYXHS446W0GQR1XS
NBsusSR MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD4NWZpUUN3ME20PFgvQDVibl2= NXfCdWVGW0GQR1XS
KU-19-19 Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XVSGlEPTB;NUG2MlA4KG6P MnfWV2FPT0WU
A204 NFm4dlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrlRWZvUUN3ME21NlIvOzNibl2= MnXhV2FPT0WU
LB1047-RCC MlTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HzSGlEPTB;NUKyMlk{KG6P M2\sfnNCVkeHUh?=
COLO-684 M4S0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXKTWM2OD13MkOuNVEhdk1? NHrFPGhUSU6JRWK=
PA-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO0TZNKSzVyPUWzNk41OSCwTR?= MVnTRW5ITVJ?
MG-63 NUX1VW1mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTV2MT6xNUBvVQ>? Mn7lV2FPT0WU
BHT-101 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXMepc4UUN3ME21OFQvQTRibl2= NIfZR4RUSU6JRWK=
NKM-1 M{nZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\GTWM2OD13OUOuNFkhdk1? MmG5V2FPT0WU
T47D Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XHdmlEPTB;NUm3MlU3KG6P NISwXW1USU6JRWK=
MOLT-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTZ{Mz62NkBvVQ>? MYnTRW5ITVJ?
IGROV-1 NUHMdnRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXSxTGpwUUN3ME22N|QvOzFibl2= NXjsbGlxW0GQR1XS
ES4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTZ|OT61OEBvVQ>? MmTZV2FPT0WU
HuO-3N1 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6zTo9KSzVyPU[0Nk4{QCCwTR?= M2\yVnNCVkeHUh?=
NEC8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT6S3FLUUN3ME22OVMvPTdibl2= MmWwV2FPT0WU
HO-1-N-1 NGPJVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTZ3OT6xO{BvVQ>? NYnrcoxKW0GQR1XS
EPCL-272H NGThN|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPoUZcxUUN3ME22PFcvOjFibl2= Ml;DV2FPT0WU
D-263MG NG\3UYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLjTWM2OD15MUiuNUBvVQ>? M1H3fHNCVkeHUh?=
MV-4-11 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XlbmlEPTB;N{K0MlMyKG6P MX\TRW5ITVJ?
SK-NEP-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTd{NT65OEBvVQ>? MXvTRW5ITVJ?
SW872 NXjR[mZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXNeGNKSzVyPUeyO{45QSCwTR?= MX7TRW5ITVJ?
P30-OHK M2\rTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrpTWM2OD15M{CuO|Ehdk1? NFXOc49USU6JRWK=
OMC-1 NEDYVpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXFXYtYUUN3ME23OVEvODlibl2= NWLZeldQW0GQR1XS
LoVo NYXXRnZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfwbHpwUUN3ME23O|cvQSCwTR?= MoXlV2FPT0WU
LNCaP-Clone-FGC NEG2[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK3dnVKSzVyPUe5Ok4{PCCwTR?= NW\DXpRxW0GQR1XS
L-363 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXLdVMzUUN3ME23PVgvPDJibl2= NIT4[25USU6JRWK=
ES8 NYHVUlBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC3TWM2OD16MUCuOVIhdk1? MWPTRW5ITVJ?
697 M4TJcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fKOmlEPTB;OEOxMlU2KG6P NFXlephUSU6JRWK=
HSC-3 MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTh|OT61OEBvVQ>? M1njeXNCVkeHUh?=
H4 NVzMVXJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTh3MD64OUBvVQ>? MUfTRW5ITVJ?
QIMR-WIL NHjxU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;2TWM2OD16NkWuNkBvVQ>? M4DHRnNCVkeHUh?=
OAW-42 M3HMV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELse2lKSzVyPUi3Nk4yQSCwTR?= NV61U3MzW0GQR1XS
MCF7 NF;zcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTwbGtjUUN3ME24PVgvPTlibl2= MVfTRW5ITVJ?
SCC-25 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG2UmhKSzVyPUmxOE4yQSCwTR?= MVrTRW5ITVJ?
NCI-H1563 M{i2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTlzNT65PUBvVQ>? NIrEWWFUSU6JRWK=
OVCAR-5 MkDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\BNGlEPTB;OUSwMlE4KG6P Mn3VV2FPT0WU
HDLM-2 NYjGPGFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfxTWM2OD17NEmuNkBvVQ>? NGTwPItUSU6JRWK=
NB5 M1vofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTl3Nj62JI5O NX3zTZhUW0GQR1XS
NCI-H292 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7ITWM2OD17N{SuN|Ihdk1? MoW4V2FPT0WU
A101D NESxVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rw[2lEPTB;OUmwMlE6KG6P NIe2WXJUSU6JRWK=
NCI-H1648 Ml[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHFUoVKSzVyPUm5PE42OSCwTR?= NYDmU4hWW0GQR1XS
EKVX NHi2VGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjnOnkxUUN3ME2xMlAyOjlizszN NHP3OWhUSU6JRWK=
SW1710 NXzIS5J[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ywO2lEPTB;MT6wOFI{OyEQvF2= MVPTRW5ITVJ?
WM-115 NFz0WGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTETWM2OD1zLkC2OlU3KM7:TR?= MkjTV2FPT0WU
CAL-54 NH\XdXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHmXml{UUN3ME2xMlA4ODhzIN88US=> NXHkWmc{W0GQR1XS
TGBC24TKB M1nMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwMEiwOFUh|ryP NVL2OIhLW0GQR1XS
NCI-H520 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHDTWM2OD1zLkC4PVY4KM7:TR?= NILXSlhUSU6JRWK=
D-423MG Ml;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTMc3RSUUN3ME2xMlA6QTZ{IN88US=> MofhV2FPT0WU
BFTC-905 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HJcGlEPTB;MT6xN|Q1QSEQvF2= MVvTRW5ITVJ?
HT MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluzTWM2OD1zLkGzOFc5KM7:TR?= NXy2PWdTW0GQR1XS
CTB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLBPW5KSzVyPUGuNVQzQTNizszN MVjTRW5ITVJ?
Hs-578-T NYjnPG1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nuNWlEPTB;MT6xPVU3PSEQvF2= MV\TRW5ITVJ?
HuH-7 M1TxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn0XW1KSzVyPUGuNlA6PDlizszN MkeyV2FPT0WU
LB996-RCC NVvLO5Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\DTWM2OD1zLkKyNVc4KM7:TR?= M3G2PHNCVkeHUh?=
KYSE-270 M1rnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T5VmlEPTB;MT6yPVc{PCEQvF2= NEPnRpdUSU6JRWK=
A4-Fuk NFzF[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\lTWM2OD1zLkK5PVk{KM7:TR?= M3PKbnNCVkeHUh?=
A498 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwM{C0O|Qh|ryP NFS1S5NUSU6JRWK=
SK-MEL-1 Mm\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvpRZJEUUN3ME2xMlMxPjd7IN88US=> M1f6[HNCVkeHUh?=
AU565 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzjW5BKUUN3ME2xMlMyQDZ|IN88US=> MYHTRW5ITVJ?
Saos-2 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\sdYRKSzVyPUGuN|MzODVizszN MlrEV2FPT0WU
A549 M4D4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3THXmlEPTB;MT6zPVk4KM7:TR?= NHyzNnRUSU6JRWK=
BFTC-909 NELRNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn60TWM2OD1zLkSzN|A2KM7:TR?= MnHFV2FPT0WU
MDA-MB-415 MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPYVVNMUUN3ME2xMlQ5Pjl{IN88US=> NVOyZXZjW0GQR1XS
639-V Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFwNUCyOFUh|ryP NW\iOVVFW0GQR1XS
A704 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFwNUC3PFUh|ryP Mn22V2FPT0WU
PANC-03-27 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\tdIpsUUN3ME2xMlUyPDB6IN88US=> M{\F[XNCVkeHUh?=
SK-MEL-28 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjpPXBNUUN3ME2xMlU3ODh3IN88US=> MkPOV2FPT0WU
Ramos-2G6-4C10 MkC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfi[IlKSzVyPUGuOlA4PDZizszN MnTLV2FPT0WU
HuP-T4 M4HzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFwNkC3O|gh|ryP MWDTRW5ITVJ?
VA-ES-BJ NX6yZ5hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwNkGyO{DPxE1? MYrTRW5ITVJ?
EFM-19 NWPmOW5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW1TWM2OD1zLk[xPFEh|ryP MXjTRW5ITVJ?
G-401 M{fV[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn4coNyUUN3ME2xMlYzOTZ2IN88US=> NIj3NGNUSU6JRWK=
D-566MG M13Dcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK0b3RKSzVyPUGuOlI2OyEQvF2= NX\ScZN7W0GQR1XS
JVM-3 NF7BTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjBOJZGUUN3ME2xMlY1QDd3IN88US=> MoPRV2FPT0WU
TK10 NVr3UJhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf4TWM2OD1zLk[3NFg{KM7:TR?= NE\aT29USU6JRWK=
BT-20 MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PMbmlEPTB;MT62PFkxOiEQvF2= NWHrSoI3W0GQR1XS
EGI-1 NXzQR|VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXKwXHpvUUN3ME2xMlg1PzBzIN88US=> MV7TRW5ITVJ?
EW-16 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\jT2lEPTB;MT64OVE5OiEQvF2= MoC5V2FPT0WU
NCI-H2228 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjINWI2UUN3ME2xMlg2OjB|IN88US=> M136PHNCVkeHUh?=
BB49-HNC NGjOb5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwOEi2PVIh|ryP M1P5TnNCVkeHUh?=
G-402 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwOEm3PVch|ryP NXP0S2ZyW0GQR1XS
NCI-H526 NV7IcJVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn0TWM2OD1zLkmxN|kh|ryP NGmxfoFUSU6JRWK=
ME-180 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPsPVM{UUN3ME2xMlk{PDd5IN88US=> NI\OPYNUSU6JRWK=
PFSK-1 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\QTWM2OD1zLkm0OFU5KM7:TR?= NH\sWmVUSU6JRWK=
TYK-nu MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG4TWM2OD1zLkm1PFI{KM7:TR?= NHu5XndUSU6JRWK=
HOS MkXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUS1bY46UUN3ME2xMlk4QTR6IN88US=> Ml;oV2FPT0WU
T98G NW\O[FdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\obJNbUUN3ME2xMlk6ODB4IN88US=> NFnkO|hUSU6JRWK=
SK-MES-1 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJwMEGzN|Ih|ryP NYe1UGJ{W0GQR1XS
SNB75 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJwMEG1OFEh|ryP NVrJZ2JRW0GQR1XS
LAMA-84 NEnvdpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwMEK2PFkh|ryP M1PuTXNCVkeHUh?=
CAL-39 NFv5fZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXCTWM2OD1{LkCzNlgh|ryP MoTlV2FPT0WU
LOXIMVI NIjNT4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;OTWM2OD1{LkC0NFg1KM7:TR?= MWHTRW5ITVJ?
NH-12 M2n3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHiTWM2OD1{LkC1OFI1KM7:TR?= NFXCNYVUSU6JRWK=
NCI-H1048 NV33dIRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:5N2lEPTB;Mj6xNFUzKM7:TR?= NHjNbWtUSU6JRWK=
KS-1 NHXIVlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Lpe2lEPTB;Mj6xNVAxOSEQvF2= M3zaW3NCVkeHUh?=
NCI-N87 NVfjNoRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInxPGlKSzVyPUKuNVM{QDRizszN MoW3V2FPT0WU
CHP-212 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr5TWM2OD1{LkG4OFQzKM7:TR?= MX7TRW5ITVJ?
HCC1419 NUnDNYx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLyTWM2OD1{LkKxNVE2KM7:TR?= MVfTRW5ITVJ?
ES1 NILyN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlraTWM2OD1{LkKxN|I3KM7:TR?= MYHTRW5ITVJ?
NCI-H2030 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e5dGlEPTB;Mj6yOFEzOyEQvF2= NHPLPHlUSU6JRWK=
EW-22 NHr5clNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;xTWM2OD1{LkK1NFY4KM7:TR?= M2i4O3NCVkeHUh?=
A431 NVPTW41vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTJwMkezOVQh|ryP M13WXHNCVkeHUh?=
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AM-38 NGiyWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\JcmlEPTB;MkWuOFgyKM7:TR?= MXzTRW5ITVJ?
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COLO-824 M3\6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fZT2lEPTB;MkWuOVU6QSEQvF2= NGHRbnpUSU6JRWK=
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NCI-H441 M12w[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPQTWM2OD1{NT63OFY2KM7:TR?= NHf6bWVUSU6JRWK=
J-RT3-T3-5 M{DkTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL3TWM2OD1{Nj6zNFI4KM7:TR?= MlLIV2FPT0WU
JEG-3 M2TFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIOydVdKSzVyPUK2MlY5ODVizszN MkDFV2FPT0WU
RKO M1vadGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HtbmlEPTB;Mk[uO|Y{OiEQvF2= M1jwZ3NCVkeHUh?=
CAL-85-1 NW\EWVN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TEdmlEPTB;MkeuNlEyQCEQvF2= Mo[wV2FPT0WU
CAL-120 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjHSlNKSzVyPUK3MlY6OTRizszN M4\DVHNCVkeHUh?=
NCI-H2452 M{\Ubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnldZB3UUN3ME2yO{44PzF4IN88US=> M1fMbXNCVkeHUh?=
NCI-H1395 NIj4eolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfaTWM2OD1{Nz63PFM{KM7:TR?= MVLTRW5ITVJ?
KYSE-450 Ml7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJ5Lkm4OlIh|ryP MonsV2FPT0WU
S-117 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\GU|FKSzVyPUK5MlM5PTdizszN NFjYN3RUSU6JRWK=
SW13 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXseIZKSzVyPUK5Mlg2OTlizszN MlT5V2FPT0WU
ES3 NGnGdXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLpUmkxUUN3ME2zNE4{PzN|IN88US=> NIn4cWFUSU6JRWK=
HCT-116 M2DITGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\pTWM2OD1|MD61OVU1KM7:TR?= NF;pdodUSU6JRWK=
NCI-H1693 NHrGTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrUfFhKSzVyPUOwMlU6PDJizszN MnPoV2FPT0WU
VM-CUB-1 M1vKb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\QTGlEPTB;M{CuOlQyOyEQvF2= NH7ibGVUSU6JRWK=
NCI-H2170 NWOwb|VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTWdHBKSzVyPUOxMlU4QDRizszN MUHTRW5ITVJ?
ALL-PO M{nHZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTNzLki0Nlgh|ryP NVfQWXp2W0GQR1XS
NCI-H661 M2frb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vpRmlEPTB;M{KuNFYzOyEQvF2= Mlf3V2FPT0WU
NCI-H2347 M2nLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN{LkS4N|ch|ryP Mk[5V2FPT0WU
FTC-133 MoG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[5NoJKSzVyPUOyMlcxPiEQvF2= NVTGPZptW0GQR1XS
COLO-829 NV;RW5BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLLV29{UUN3ME2zN{4{PDZ5IN88US=> MVXTRW5ITVJ?
GOTO MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ezb2lEPTB;M{OuOVI2QCEQvF2= NGrtWXRUSU6JRWK=
YAPC MnPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXnPFNKSzVyPUOzMlgyPTlizszN MlyxV2FPT0WU
LCLC-103H NILwUFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrPTWM2OD1|ND6xOlI1KM7:TR?= M4Kyd3NCVkeHUh?=
SiHa MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\KXJlKSzVyPUO0MlM5OTdizszN M13pfHNCVkeHUh?=
LK-2 MlnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfkPYJVUUN3ME2zOE42PzB6IN88US=> NH;VS5hUSU6JRWK=
KP-N-YS M4e5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILnc5dKSzVyPUO0MlczODJizszN MojEV2FPT0WU
NCI-SNU-1 MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[0TWM2OD1|NT6xO|kh|ryP Mkn3V2FPT0WU
KNS-81-FD M3vMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\jNmlEPTB;M{WuOlY{KM7:TR?= M2jPbHNCVkeHUh?=
SCC-9 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXkTWM2OD1|Nj63NVQ3KM7:TR?= MlTwV2FPT0WU
SH-4 M3HDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPuTWM2OD1|Nj63N{DPxE1? MmnKV2FPT0WU
HCC-1954 NUn2cFFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u4fWlEPTB;M{euNlczQSEQvF2= M335ZnNCVkeHUh?=
BALL-1 Ml33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN5LkWzNVYh|ryP NGnlRYFUSU6JRWK=
BE-13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN5LkewNVgh|ryP NXryXJJ5W0GQR1XS
COLO-678 NYLM[2hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfUTWM2OD1|Nz65OFM4KM7:TR?= MYTTRW5ITVJ?
SK-MEL-3 M{XWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH2yNmpKSzVyPUO4MlI{QTdizszN MoS0V2FPT0WU
OAW-28 MmXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4S5NmlEPTB;M{iuOlM6KM7:TR?= MUnTRW5ITVJ?
CAMA-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf1eFVKSzVyPUO4Mlk3QTFizszN NEXuUodUSU6JRWK=
C2BBe1 NXfmTWc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTrcVFMUUN3ME2zPU45OThizszN NXP5T5dnW0GQR1XS
A3-KAW M4GwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjjfolKSzVyPUSwMlM3PjFizszN MXHTRW5ITVJ?
SK-MEL-24 NYHtNndGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrJVpNKSzVyPUSwMlU6OzFizszN MXvTRW5ITVJ?
KYSE-140 NX31eGg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zXbWlEPTB;NECuO|E3PSEQvF2= NHXJeIdUSU6JRWK=
MOLT-16 NHfNbHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jCW2lEPTB;NEGuNVU{PiEQvF2= MYnTRW5ITVJ?
CFPAC-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnXTI0xUUN3ME20Nk42OjFzIN88US=> MmrIV2FPT0WU
NB14 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjD[pBKSzVyPUSyMlcxOjdizszN NGTNe5dUSU6JRWK=
COLO-792 MmrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuyd4xKSzVyPUSyMlg6PjFizszN MVzTRW5ITVJ?
RH-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLvbFRyUUN3ME20N{41QDN4IN88US=> MVPTRW5ITVJ?
NCI-H522 M2jie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnhfmloUUN3ME20OE4{PTZ6IN88US=> MVzTRW5ITVJ?
Ca-Ski MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTzNnU6UUN3ME20OE45OTF2IN88US=> Mnu3V2FPT0WU
KGN NVTaO|MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\YTWM2OD12OD6zNFY{KM7:TR?= NHnLT49USU6JRWK=
UACC-62 NIKxWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTR6LkSwO|Ih|ryP M{TLRnNCVkeHUh?=
NCI-H358 M3\xNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfwTWM2OD12OT6zNFE5KM7:TR?= M1;3d3NCVkeHUh?=
LS-411N NYjTboJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q3UmlEPTB;NEmuN|EyQCEQvF2= M{jtcXNCVkeHUh?=
IST-MES1 M3;S[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7FZ3hEUUN3ME20PU42PjJ3IN88US=> NEfPc2xUSU6JRWK=

... 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 2年-20℃
6月-80℃in solvent
別名 RG7321
溶解度 (25°C) * In vitro DMSO 44 mg/mL (85.66 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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

カスタマーフィードバック (7)


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Rating
Source Cancer Res, 2011, 71, 2750-2760. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot, Immunofluorescence staining, flow cytometry
Cell Lines 1205Lu cells
Concentrations 3 µmol/L
Incubation Time 48 h
Results Combined PI3K and BRAF inhibition increased the level of BIM expression in both Western blot and immunofluorescence studies (Fig. A). Consistent with a role for increased AKT signaling suppressing BIM expression in PTEN- cells, dual BRAF and PI3K inhibition increased nuclear FOXO3a localization in the PTEN- cell lines (Fig. B) and enhanced the level of BIM mRNA (Fig. B). the combination of PLX4720 with the PI3K inhibitor GDC-0941 significantly enhanced the levels of apoptosis observed in PTEN melanoma cell lines compared to either the BRAF or PI3K inhibitor alone (Fig. C). Similar results were also observed in a 3D spheroid assay, where combined PLX4720 (3 µmol/L) and LY294002 (10 µmol/L) treatment prevented the recovery of cell growth observed when melanoma spheroids were treated with either drug alone (Fig. D).

Click to enlarge
Rating
Source J Inves Der, 2010, 131, 495-503. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines Mel-Juso cells, 518A2 cells
Concentrations 0.05–1 µmol/L
Incubation Time 24 h
Results In addition, GDC-0941 treatment blocked the phosphorylation of AKT protein (S473 and T308) at even lower concentrations than PI-103, and S6 protein phosphorylation was blocked at similar concentrations.

Click to enlarge
Rating
Source J Cell Sci, 2012, 125(Pt 5), 1259-73. Pictilisib (GDC-0941) purchased from Selleck
Method Western Blot
Cell Lines NMuMG cells
Concentrations 1 μM
Incubation Time 1 h
Results GDC-0941, a specific inhibitor of the class IA PI3K, similarly blocked the TGF-b-induced Akt(S473) phosphorylation, confirming the role of PI3K in the induction of mTORC2 kinase activity by TGF-β (Fig. C).

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Rating
Source Dr. Zhang of Tianjin Medical University. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-10 nM
Incubation Time 3 h
Results

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Rating
Source Saraswati Sukumar of Johns Hopkins University School of Medicine. Pictilisib (GDC-0941) purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results

Click to enlarge
Rating
Source Biochim Biophys Acta, 2012, 1823, 2210-6. Pictilisib (GDC-0941) purchased from Selleck
Method confocal laser-scanning microscopy
Cell Lines HEK293 cells
Concentrations 1 μM
Incubation Time 30 min
Results Both LY294002 and GDC-0941 markedly attenuated the high-glucose-dependent plasma membrane translocation of DGKδ1, indicating that the event is positively regulated by phosphatidylinositol 3-kinase.

Click to enlarge
Rating
Source Pictilisib (GDC-0941) purchased from Selleck
Method Western blot analysis
Cell Lines MCF-7 cells
Concentrations 0 nM/50 nM/100 nM/400 nM
Incubation Time 24 h
Results GDC-0941 caused a surprising increase in phosphorylation of ERK proteins as well as AKT2 S474. GDC-0941 showed differences in its ability to suppr ess PI3K-dependent signaling across the genotypes. AKT1 mutant cells demonstrated greater residual AKT1 S473 phosphorylation and greater phosphorylation of downstream proteins FOXO 1/3, PRAS40, GSK3β , and p70S6K at equivalent doses of GDC-0941, compared to PIK3CA mutant cells.

文献中の引用 (56)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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