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 MYDLbY5ie2ViQYPzZZk> MojzNUBp MX7EUXNQ MlTUTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCmZXz0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wNFMh|ryP MkG5NVg4PTR4NUS=
Sf9 MYHLbY5ie2ViQYPzZZk> NWf1cFdnOSCq MmS3SG1UVw>? NWexVm1sUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? MUSxPFc2PDZ3NB?=
Sf9 NWfhW3NLU2mwYYPlJGF{e2G7 NIHxW5YyKGh? M13qd2ROW09? MWPJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgSVU1PS2NIH31eIFvfCCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[SC5aYToJGlEPTBib3[gNE4xODNizszN MofMNVg4PTR4NUS=
Sf9 NXztUZJDU2mwYYPlJGF{e2G7 MXyxJIg> MXHEUXNQ NVq4PZAyUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= MYixPFc2PDZ3NB?=
Sf9 NIfwVIhMcW6jc3WgRZN{[Xl? MkGyNUBp MmXsSG1UVw>? MlnGTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> M2LidFE5PzV2NkW0
MDA-MB-361 M{DRb2Z2dmO2aX;uJGF{e2G7 NYrERpJMOiCq MYDEUXNQ NVGycoJXUW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNSGEuVUJvM{[xJINmdGy|IIfpeIghWEmNM1PBJGU2PDVvSzDteZRifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkig{txO NW\FeIg3OTh5NUS2OVQ>
PC3 M1PmVGZ2dmO2aX;uJGF{e2G7 M3XRS|IhcA>? NGf6PJRFVVOR MnXBTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kAxNjB|NzFOwG0> NHnsVpYyQDd3NE[1OC=>
U87MG M2j0bGZ2dmO2aX;uJGF{e2G7 MmjrNkBp M3XxUWROW09? NX6zSm56UW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDpckBRXEWQLX71cIwhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDJR|UxKG:oIECuNFQ3KM7:TR?= NV\RWo01OTh5NUS2OVQ>
MDA-MB-361 NXPVdFZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknBPVYhcA>? NHL5UGxFVVOR MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlczKM7:TR?= NFPueIEyQDd3NE[1OC=>
A2780 NXrQS2h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3JSGw6PiCq M2L3OmROW09? M1TxfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCSSVuzR2Eh[W6mIGDUSW4hdXW2YYTpc44hf2m2aDDJR|UxKG:oIECuNVQh|ryP M{LPZ|E5PzV2NkW0
PC3 NHv6XJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n5[Vk3KGh? NVH5XWtPTE2VTx?= NIPq[WhKSzVyPUCuNlgh|ryP NIPqOZgyQDd3NE[1OC=>
U87MG NIe4XWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\hPVYhcA>? MUTEUXNQ NEfPZpJKSzVyPUCuPVUh|ryP NUTOOG5mOTh5NUS2OVQ>
Sf9 NYL2d4NDU2mwYYPlJGF{e2G7 MWqzNEBucW5? NGnueZlFVVOR M{nxb2lvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDhcY92dnRib3[gRXRRKGOxboP1cYVlKHerdHigTWM2OCCxZjCwMlA1OiEQvF2= NXPFeYdzOjJ3NEizOFI>
RAW 264.7 MULLbY5ie2ViQYPzZZk> M{\tNVkxKG2rbh?= NX\McYx6TE2VTx?= NVr1NJNQUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPL[4FudWFiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQVvUJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUig{txO MmPENlI2PDh|NEK=
Sf9 NFv4e2NMcW6jc3WgRZN{[Xl? NX7Wb|JjOSCq NUXNTYdSUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2KndHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPGPUBk\WyuczD3bZRpKEmFNUCgc4YhOC5yMUeg{txO M13uUFI{PTRyNkS1
Sf9 M2PqWmtqdmG|ZTDBd5NigQ>? NXS5clVxOSCq NUm4RVFCUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> NGHYZY0zOzV2ME[0OS=>
Sf9 MlvmT4lv[XOnIFHzd4F6 Mn;3NUBp NIHZ[ZJKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM\2GvbXGg[ZhxemW|c3Xk MV6yN|U1ODZ2NR?=
Sf9 Ml\qT4lv[XOnIFHzd4F6 MYSxJIg> M33SVmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXS= NXvENYZNOjN3NEC2OFU>
SKOV3 M2DENGtqdmG|ZTDBd5NigQ>? MVSxJO69VQ>? NGH2SGcyKGh? MkftSG1UVw>? MmSyTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? MVWyN|M3ODN2OB?=
MCF7 MkLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7lWIdCOSEQvF2= M{TvZ|k3KGh? NXzTRWhnTE2VTx?= NYjTS5BUT0l3ME2wMlA4ODJizszN MmLmNlM{PjB|NEi=
SKOV3 NFvnRYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TNXlEh|ryP MYK5OkBp MVvEUXNQ M4LnOGdKPTB;MD6xOFc3KM7:TR?= Mm\QNlM{PjB|NEi=
PC3 NYTHW4ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvGO|IhcA>? M2nRbWROW09? NUDSenF3UUN3ME2wMlI5KM7:TR?= NF\EbJMzOTl6MUexOC=>
MCF7.1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnuO|IhcA>? M3HxXGROW09? MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? MXeyNVk5OTdzNB?=
MCF7-neo/Her2 MmDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LmVVczKGh? MUDEUXNQ NUXKOHI1UUN3ME2wMlI6KM7:TR?= MnHLNlM3PjJ7MEO=
MCF7-neo/Her2 NEGzN|FMcW6jc3WgRZN{[Xl? M4DYc2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> MonqNlM3PjJ7MEO=
PC3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:3NkBp MmC5SG1UVw>? MlLKSWM2OD1yLkO0JO69VQ>? NF;LO4szOTl6NU[zPS=>
MCF7.1 NUnrV|I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS3NkBp M4rZSmROW09? M2PVc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFXDOVAhd2ZiMD6zPUDPxE1? M{myW|IyQTh3NkO5
PC3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrrcWRoPzJiaB?= MkizSG1UVw>? NGn0O|JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> M1;NNlIxODVyNk[5
MCF7.1 NF33VYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;OO|IhcA>? NICzO25FVVOR Mn25RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkO0JO69VQ>? MleyNlAxPTB4Nkm=
MCF7.1 M4nP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWq3NkBp NIKyUHFGSzVyPUCuO|Ih|ryP MV6yNFM1PjZ3Nh?=
NCI-H1975 MXzDfZRwfG:6aXOgRZN{[Xl? MXi3NkBp NIK3UXpKSzVyPUCuNlch|ryP MXqyN|A2QTV2NR?=
H460 NVPOZZRtS3m2b4TvfIlkKEG|c3H5 NX;FbZZWPzJiaB?= MYrJR|UxRTBwOEeg{txO M{XSNVI{ODV7NUS1
HT-29 NF7SW21EgXSxdH;4bYMhSXO|YYm= M1TyNlczKGh? MkW3TWM2OD1yLk[2JO69VQ>? Mk[2NlMxPTl3NEW=
HepG2 MXvDfZRwfG:6aXOgRZN{[Xl? MonmO|IhcA>? MUXJR|UxRTFizszN M4HLdFI{ODV7NUS1
SGC7901 Mn\PR5l1d3SxeHnjJGF{e2G7 NGO0dlM4OiCq NFSy[pNKSzVyPUGuPEDPxE1? MUmyN|A2QTV2NR?=
NCI-H226 M2K2VmN6fG:2b4jpZ{BCe3OjeR?= MXu3NkBp MWDJR|UxRTJwOTFOwG0> MlzyNlMxPTl3NEW=
A549 MUfDfZRwfG:6aXOgRZN{[Xl? NVP1[lV6PzJiaB?= MmiyTWM2OD14Lkmg{txO MoHWNlMxPTl3NEW=
U87MG Mor4R5l1d3SxeHnjJGF{e2G7 MlTPO|IhcA>? NFPmdW9KSzVyPUeuO|ch|ryP NWeyV3hNOjNyNUm1OFU>
HBC4 MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljwcI9oT0l3ME2tOk4xOyCP M2CwRVIzOzN4MkS2
BSY1 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnV[pJtdG:pR1m1NF0uPi57MDDN M33ub|IzOzN4MkS2
HBC5 NYfhVZNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\0XFZtd2eJSUWwQU03NjZyIF2= MojlNlI{OzZ{NE[=
MCF7 NXq2XItmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7hS3p6dG:pR1m1NF0uPy5|MzDN MlqyNlI{OzZ{NE[=
MDA-MB-231 M2PTTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXsc4dIUTVyPT21MlQ3KE1? Mni2NlI{OzZ{NE[=
U251 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrsc4dIUTVyPT21MlUxKE1? NGPReZIzOjN|NkK0Oi=>
SF268 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfFVIN2dG:pR1m1NF0uPS5|OTDN NVn4S3dzOjJ|M{[yOFY>
SF295 NXmxTpU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\BS4xw\0eLNUC9MVYvOzdiTR?= MUiyNlM{PjJ2Nh?=
SF539 NYTqNnRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqxb3B2dG:pR1m1NF0uPi53MDDN MUSyNlM{PjJ2Nh?=
SNB75 NHTaWHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37jNoxw\0eLNUC9MVcvOTBiTR?= NHWyepAzOjN|NkK0Oi=>
SNB78 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoWycI9oT0l3ME2tOk42OiCP MYOyNlM{PjJ2Nh?=
HCC2998 NXTQeotPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHsc4dIUTVyPT22MlI6KE1? NUWxdZZsOjJ|M{[yOFY>
KM12 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3sc4dIUTVyPT21Mlc3KE1? NWjQblJIOjJ|M{[yOFY>
HT-29 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO2cI9oT0l3ME2tOk4{OCCP MYCyNlM{PjJ2Nh?=
HCT15 NF3IRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DXXIxw\0eLNUC9MVYvOTJiTR?= NYfWPYJUOjJ|M{[yOFY>
HCT116 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHuOlFtd2eJSUWwQU02Njh5IF2= M1LvSlIzOzN4MkS2
NCI-H23 NU\rdI1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXhdZptd2eJSUWwQU02Njd|IF2= M3TGWlIzOzN4MkS2
NCI-H226 MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGqzcJhtd2eJSUWwQU03NjJzIF2= MknxNlI{OzZ{NE[=
NCI-H522 NUXzUYp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml20cI9oT0l3ME2tOk42QCCP NFvGSo8zOjN|NkK0Oi=>
NCI-H483 MkTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3NcI9oT0l3ME2tOk42PiCP MYWyNlM{PjJ2Nh?=
A549 NX\pXI4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHDRmttd2eJSUWwQU03NjF3IF2= NEDJXZIzOjN|NkK0Oi=>
DMS273 NF7Ed3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnsc4dIUTVyPT22MlQ{KE1? MmrHNlI{OzZ{NE[=
DMS114 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDhN2ttd2eJSUWwQU02Njl{IF2= MlnmNlI{OzZ{NE[=
LOXIMVI Mn7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjsc4dIUTVyPT22MlI6KE1? NYDzNIVUOjJ|M{[yOFY>
OVCAR3 Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfMclhtd2eJSUWwQU03NjdzIF2= NV\3VnBmOjJ|M{[yOFY>
OVCAR4 NVL5VVUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTsc4dIUTVyPT21Mlc3KE1? M37EcVIzOzN4MkS2
OVCAR5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXsc4dIUTVyPT22MlI3KE1? M1vhelIzOzN4MkS2
OVCAR8 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfrcI9oT0l3ME2tOU44OyCP MXmyNlM{PjJ2Nh?=
SKOV3 NX7hcIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPtS41IdG:pR1m1NF0uPi53MjDN NIDmTIQzOjN|NkK0Oi=>
RXF631L Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTScI9oT0l3ME2tOk45QCCP NVr2dpE3OjJ|M{[yOFY>
ACHN MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHNcI9oT0l3ME2tOk4xPyCP MoXuNlI{OzZ{NE[=
St-4 Mn32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;mNYxw\0eLNUC9MVUvPTZiTR?= NWLyempEOjJ|M{[yOFY>
MKN1 NX;MdJlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H0eoxw\0eLNUC9MVcvODhiTR?= MYKyNlM{PjJ2Nh?=
MKN7 NF74T4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDsc4dIUTVyPT22MlUxKE1? NF7aWVYzOjN|NkK0Oi=>
MKN28 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[5eWVtd2eJSUWwQU02NjV{IF2= M17WPVIzOzN4MkS2
MKN45 NEOzb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jHOoxw\0eLNUC9MVYvPTViTR?= MXiyNlM{PjJ2Nh?=
MKN74 NXy3V|NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXybJltd2eJSUWwQU03NjB{IF2= M{ftXlIzOzN4MkS2
DU145 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLsc4dIUTVyPT21Mlg2KE1? NVryNHVoOjJ|M{[yOFY>
PC3 M1[5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rOcoxw\0eLNUC9MVYvPjZiTR?= NVzjdZEyOjJ|M{[yOFY>
ES5 NGrVVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfjNJZQUUN3ME21NE4zOSCwTR?= NWLrXYtCW0GQR1XS
HH NX[wbmZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e3dmlEPTB;MUGxMlA5KG6P M37HN3NCVkeHUh?=
MHH-PREB-1 M4P1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH5TWM2OD1zMUSuN{BvVQ>? M4O4c3NCVkeHUh?=
NCI-H1770 NEXYcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK3TWM2OD1zMkOuPFYhdk1? M{XEOXNCVkeHUh?=
HuO9 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXJVnJKSzVyPUKwOk4xOiCwTR?= MX3TRW5ITVJ?
HAL-01 NITKXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJyNj63N{BvVQ>? Ml:1V2FPT0WU
NOS-1 M4nOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK1TWM2OD1{MUGuPFIhdk1? NWrDcXlEW0GQR1XS
HGC-27 NFv2[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn6bXBKSzVyPUKxNk42PyCwTR?= MVLTRW5ITVJ?
NB69 NFfBWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XqbWlEPTB;MkS1MlI4KG6P NGDNdWtUSU6JRWK=
RS4-11 NEf5dVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r2N2lEPTB;Mk[xMlc3KG6P MXrTRW5ITVJ?
DOK NWLGfZVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLhTWM2OD1|MEGuO{BvVQ>? NE\5fmZUSU6JRWK=
LB2241-RCC NVn2UpdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\EZmlEPTB;M{CzMlg1KG6P M2\MbXNCVkeHUh?=
NCI-H1623 NHO4Z4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTNyND6wPEBvVQ>? M2rKWHNCVkeHUh?=
YH-13 NEjXSYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jEO2lEPTB;M{C0MlMzKG6P NFvFZ|lUSU6JRWK=
BPH-1 MoLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPiVJdKSzVyPUOxOEBvVQ>? M1nJU3NCVkeHUh?=
AN3-CA MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIftNZJKSzVyPUO0NE4{PyCwTR?= NEnvSHZUSU6JRWK=
ES7 NY[2XlMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTN2MT65PUBvVQ>? MYPTRW5ITVJ?
MDA-MB-175-VII MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HBRWlEPTB;M{WyMlkzKG6P MoTXV2FPT0WU
GAMG M12yZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTN5MD64OUBvVQ>? NX[0WWhsW0GQR1XS
CHL-1 NE\BbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\UeZhqUUN3ME2zO|gvPjVibl2= MVjTRW5ITVJ?
NB7 NV\4TWc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DINGlEPTB;M{i5Mlg{KG6P MnmyV2FPT0WU
MFE-280 MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTRzOD6yJI5O M4rZdXNCVkeHUh?=
HL-60 NUXBe3pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjRb3FRUUN3ME20NlUvPzVibl2= MlPhV2FPT0WU
GCIY MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\VTWM2OD12M{OuPEBvVQ>? NUTZdG12W0GQR1XS
MDA-MB-361 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkO2TWM2OD12M{muNVMhdk1? M33DVXNCVkeHUh?=
LXF-289 NFzBU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;zN2lEPTB;NES4MlI4KG6P MULTRW5ITVJ?
NBsusSR NWn2d4RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIraPJVKSzVyPUS4PE45PSCwTR?= MofaV2FPT0WU
KU-19-19 NXK4OHRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rJeWlEPTB;NUG2MlA4KG6P M4S4[HNCVkeHUh?=
A204 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrsSndKSzVyPUWyNk4{OyCwTR?= NHz1UJhUSU6JRWK=
LB1047-RCC M4LmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7SWFRbUUN3ME21NlIvQTNibl2= NIH6RlNUSU6JRWK=
COLO-684 M{jpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXXcoY5UUN3ME21NlMvOTFibl2= M{O5NXNCVkeHUh?=
PA-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXLTWM2OD13M{KuOFEhdk1? M3rPbHNCVkeHUh?=
MG-63 M2HGUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTV2MT6xNUBvVQ>? M1rNPHNCVkeHUh?=
BHT-101 NUXDbpR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XoeGlEPTB;NUS0Mlk1KG6P M4LwNHNCVkeHUh?=
NKM-1 NIHXV3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLsTWM2OD13OUOuNFkhdk1? M1K1NHNCVkeHUh?=
T47D NYLmWplxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\uTWM2OD13OUeuOVYhdk1? MmjyV2FPT0WU
MOLT-4 NH\MO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[yb|hKSzVyPU[yN{43OiCwTR?= MUfTRW5ITVJ?
IGROV-1 NUHGOWJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XNPGlEPTB;NkO0MlMyKG6P MmDJV2FPT0WU
ES4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLXTWM2OD14M{muOVQhdk1? M2nXfXNCVkeHUh?=
HuO-3N1 Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L1XmlEPTB;NkSyMlM5KG6P M2[4ZnNCVkeHUh?=
NEC8 M3jaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXZclRKSzVyPU[1N{42PyCwTR?= M3PwZ3NCVkeHUh?=
HO-1-N-1 M2\VVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoKxTWM2OD14NUmuNVchdk1? M{iwS3NCVkeHUh?=
EPCL-272H MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkWwTWM2OD14OEeuNlEhdk1? NWDXWHVTW0GQR1XS
D-263MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDsPWFDUUN3ME23NVgvOSCwTR?= Mn7mV2FPT0WU
MV-4-11 M4K3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPiTWM2OD15MkSuN|Ehdk1? NX3kNplkW0GQR1XS
SK-NEP-1 NEHIeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XM[GlEPTB;N{K1Mlk1KG6P MlPhV2FPT0WU
SW872 NVHGRopTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorJTWM2OD15MkeuPFkhdk1? M4XGdnNCVkeHUh?=
P30-OHK Mn3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP2WppKSzVyPUezNE44OSCwTR?= NG\ZW5NUSU6JRWK=
OMC-1 NG\6dmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETlUllKSzVyPUe1NU4xQSCwTR?= M4j4VnNCVkeHUh?=
LoVo NFjNZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjWTWM2OD15N{euPUBvVQ>? NH3jVVhUSU6JRWK=
LNCaP-Clone-FGC NFv4XHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPZXHlKSzVyPUe5Ok4{PCCwTR?= NFLhdmlUSU6JRWK=
L-363 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmOxTWM2OD15OUiuOFIhdk1? MoWxV2FPT0WU
ES8 NITHXpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy1OGVNUUN3ME24NVAvPTJibl2= MlPQV2FPT0WU
697 NEPNR|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPXWod7UUN3ME24N|EvPTVibl2= MUjTRW5ITVJ?
HSC-3 Mmn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnRUnFpUUN3ME24N|kvPTRibl2= MnjPV2FPT0WU
H4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3jOlRKSzVyPUi1NE45PSCwTR?= NUPVd|Q2W0GQR1XS
QIMR-WIL M1u2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rVbGlEPTB;OE[1MlIhdk1? NVjnRWNpW0GQR1XS
OAW-42 M4\oXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XHemlEPTB;OEeyMlE6KG6P NYK3U2Z1W0GQR1XS
MCF7 M{HOcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjLdGU3UUN3ME24PVgvPTlibl2= NWHYUIp3W0GQR1XS
SCC-25 NInGVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf1O5VuUUN3ME25NVQvOTlibl2= NE\uNJZUSU6JRWK=
NCI-H1563 M1XBXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHTW|VrUUN3ME25NVUvQTlibl2= MkPPV2FPT0WU
OVCAR-5 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn25TWM2OD17NECuNVchdk1? Moj4V2FPT0WU
HDLM-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe0dXh2UUN3ME25OFkvOiCwTR?= NUi2SlI1W0GQR1XS
NB5 MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTl3Nj62JI5O MXfTRW5ITVJ?
NCI-H292 MoHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHqUnpDUUN3ME25O|QvOzJibl2= NF7K[|dUSU6JRWK=
A101D NEDLSZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTl7MD6xPUBvVQ>? MmjqV2FPT0WU
NCI-H1648 NWLFc|RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCyeYd3UUN3ME25PVgvPTFibl2= NF7yXYRUSU6JRWK=
EKVX M2HqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFwMEGyPUDPxE1? Mn75V2FPT0WU
SW1710 M3raU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljvTWM2OD1zLkC0NlM{KM7:TR?= NHf0R5JUSU6JRWK=
WM-115 Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSxTWM2OD1zLkC2OlU3KM7:TR?= M3XxbHNCVkeHUh?=
CAL-54 MmjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFwMEewPFEh|ryP NULJVYQyW0GQR1XS
TGBC24TKB M3TtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFwMEiwOFUh|ryP NHGyeItUSU6JRWK=
NCI-H520 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrZZmFkUUN3ME2xMlA5QTZ5IN88US=> MXjTRW5ITVJ?
D-423MG NXrYfWVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT1TWM2OD1zLkC5PVYzKM7:TR?= MnuzV2FPT0WU
BFTC-905 M4XvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTIboI4UUN3ME2xMlE{PDR7IN88US=> M2rOTHNCVkeHUh?=
HT NYLqUnhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjIOZZ3UUN3ME2xMlE{PDd6IN88US=> NWLMVIlqW0GQR1XS
CTB-1 NWDtU5p[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMUSyPVMh|ryP M2nrd3NCVkeHUh?=
Hs-578-T Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zwcmlEPTB;MT6xPVU3PSEQvF2= NUD6RYZ2W0GQR1XS
HuH-7 NFTNUVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1T1UmlEPTB;MT6yNFk1QSEQvF2= M3XVPHNCVkeHUh?=
LB996-RCC NX;hVppiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\tVoFKSzVyPUGuNlIyPzdizszN NWPF[ZVYW0GQR1XS
KYSE-270 NWXVVnpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTyTWM2OD1zLkK5O|M1KM7:TR?= MXzTRW5ITVJ?
A4-Fuk NW\DWZJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFwMkm5PVMh|ryP M2L1NHNCVkeHUh?=
A498 M4rQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojBTWM2OD1zLkOwOFc1KM7:TR?= Ml74V2FPT0WU
SK-MEL-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXCVoQ{UUN3ME2xMlMxPjd7IN88US=> MX3TRW5ITVJ?
AU565 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFwM{G4OlMh|ryP Mn:1V2FPT0WU
Saos-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO3W3NHUUN3ME2xMlM{OjB3IN88US=> M{PLOXNCVkeHUh?=
A549 NH3acFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7SRW1KSzVyPUGuN|k6PyEQvF2= NXryNopoW0GQR1XS
BFTC-909 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT3TWM2OD1zLkSzN|A2KM7:TR?= NHz6XHBUSU6JRWK=
MDA-MB-415 NHjZfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PuZ2lEPTB;MT60PFY6OiEQvF2= M3TpVnNCVkeHUh?=
639-V MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljPTWM2OD1zLkWwNlQ2KM7:TR?= NG\zZ2pUSU6JRWK=
A704 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjmcGtKSzVyPUGuOVA4QDVizszN NVTIVmcxW0GQR1XS
PANC-03-27 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfvcVJbUUN3ME2xMlUyPDB6IN88US=> NU\5XVNwW0GQR1XS
SK-MEL-28 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFwNU[wPFUh|ryP NXu1UY16W0GQR1XS
Ramos-2G6-4C10 MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwNkC3OFYh|ryP MmDPV2FPT0WU
HuP-T4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLDTWM2OD1zLk[wO|c5KM7:TR?= NWXNTmZkW0GQR1XS
VA-ES-BJ NECzT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvOXoRKSzVyPUGuOlEzPyEQvF2= NH25dXZUSU6JRWK=
EFM-19 NX3EWVRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zz[mlEPTB;MT62NVgyKM7:TR?= NYmwWnViW0GQR1XS
G-401 NFK3XpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH70OZZKSzVyPUGuOlIyPjRizszN MV;TRW5ITVJ?
D-566MG MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDneXhKSzVyPUGuOlI2OyEQvF2= NUX2NZpEW0GQR1XS
JVM-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nieGlEPTB;MT62OFg4PSEQvF2= NVjZdGd4W0GQR1XS
TK10 M{G3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDUSXBPUUN3ME2xMlY4ODh|IN88US=> Mm\CV2FPT0WU
BT-20 M4W1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwNki5NFIh|ryP M2m0bHNCVkeHUh?=
EGI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjGcFVFUUN3ME2xMlg1PzBzIN88US=> MnHqV2FPT0WU
EW-16 M4nFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmCxTWM2OD1zLki1NVgzKM7:TR?= MmW0V2FPT0WU
NCI-H2228 M2f3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnje5psUUN3ME2xMlg2OjB|IN88US=> M2TJPHNCVkeHUh?=
BB49-HNC M1j3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7rTWM2OD1zLki4OlkzKM7:TR?= NIHuTYdUSU6JRWK=
G-402 NU\CWGVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXHd5MzUUN3ME2xMlg6Pzl5IN88US=> MXXTRW5ITVJ?
NCI-H526 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTsPGZKSzVyPUGuPVE{QSEQvF2= M3XOW3NCVkeHUh?=
ME-180 NVnRPGRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknvTWM2OD1zLkmzOFc4KM7:TR?= MkK1V2FPT0WU
PFSK-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwOUS0OVgh|ryP MUnTRW5ITVJ?
TYK-nu MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFdm5QUUN3ME2xMlk2QDJ|IN88US=> MYjTRW5ITVJ?
HOS MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;6TWM2OD1zLkm3PVQ5KM7:TR?= NETK[o5USU6JRWK=
T98G NIizS4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXTe45KSzVyPUGuPVkxODZizszN NU[3TIpOW0GQR1XS
SK-MES-1 M2XqNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJwMEGzN|Ih|ryP NUfh[oZsW0GQR1XS
SNB75 Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[wZ2lEPTB;Mj6wNVU1OSEQvF2= NUPKVGJZW0GQR1XS
LAMA-84 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJwMEK2PFkh|ryP NUPGUFVCW0GQR1XS
CAL-39 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJwMEOyPEDPxE1? NG\aVYpUSU6JRWK=
LOXIMVI MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7rTWM2OD1{LkC0NFg1KM7:TR?= M4rvPXNCVkeHUh?=
NH-12 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jFc2lEPTB;Mj6wOVQzPCEQvF2= Mk\MV2FPT0WU
NCI-H1048 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJwMUC1NkDPxE1? NFrUOnZUSU6JRWK=
KS-1 NXTSXVE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PSZ2lEPTB;Mj6xNVAxOSEQvF2= M3TTW3NCVkeHUh?=
NCI-N87 NFXzbZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLjTWM2OD1{LkGzN|g1KM7:TR?= MUHTRW5ITVJ?
CHP-212 M4DBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJwMUi0OFIh|ryP NE\qb2dUSU6JRWK=
HCC1419 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fTb2lEPTB;Mj6yNVEyPSEQvF2= NYDZcHE1W0GQR1XS
ES1 NGHyZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rMbmlEPTB;Mj6yNVMzPiEQvF2= Ml;3V2FPT0WU
NCI-H2030 NF;lZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33X[WlEPTB;Mj6yOFEzOyEQvF2= MV;TRW5ITVJ?
EW-22 NYqxN5NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS2XFhqUUN3ME2yMlI2ODZ5IN88US=> MmDFV2FPT0WU
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M059J MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmyTWM2OD1{ND61OlM1KM7:TR?= MVPTRW5ITVJ?
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KG-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLjTWM2OD1{NT61OFk1KM7:TR?= NIn3TYRUSU6JRWK=
COLO-824 MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLnTWM2OD1{NT61OVk6KM7:TR?= NF;rXXhUSU6JRWK=
NCI-H1155 M4\qWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljZTWM2OD1{NT61PFQ4KM7:TR?= MXjTRW5ITVJ?
NCI-H441 NGrQNG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmC1TWM2OD1{NT63OFY2KM7:TR?= MYHTRW5ITVJ?
J-RT3-T3-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rD[2lEPTB;Mk[uN|AzPyEQvF2= NUH1fWFNW0GQR1XS
JEG-3 MkPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL4bm9nUUN3ME2yOk43QDB3IN88US=> MlK5V2FPT0WU
RKO MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJ4Lke2N|Ih|ryP NEXCTZhUSU6JRWK=
CAL-85-1 NIW4V4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXMTWM2OD1{Nz6yNVE5KM7:TR?= NUX4e5BtW0GQR1XS
CAL-120 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMRWlEPTB;MkeuOlkyPCEQvF2= NUHBSoFFW0GQR1XS
NCI-H2452 NHPUN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLJbXh6UUN3ME2yO{44PzF4IN88US=> MX3TRW5ITVJ?
NCI-H1395 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJ5Lke4N|Mh|ryP M1X3Z3NCVkeHUh?=
KYSE-450 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HOeGlEPTB;MkeuPVg3OiEQvF2= Mmq0V2FPT0WU
S-117 NGH1U2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULoTVA3UUN3ME2yPU4{QDV5IN88US=> M1v1VHNCVkeHUh?=
SW13 NWrmS3N{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnGTWM2OD1{OT64OVE6KM7:TR?= NUDYbHlbW0GQR1XS
ES3 MnPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfkd21mUUN3ME2zNE4{PzN|IN88US=> NHvxV|FUSU6JRWK=
HCT-116 M{XzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnxfpNKSzVyPUOwMlU2PTRizszN MnvvV2FPT0WU
NCI-H1693 NHnONFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTNyLkW5OFIh|ryP NYG3S|N5W0GQR1XS
VM-CUB-1 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;aVJh5UUN3ME2zNE43PDF|IN88US=> MVnTRW5ITVJ?
NCI-H2170 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELBWHFKSzVyPUOxMlU4QDRizszN MnroV2FPT0WU
ALL-PO NXe2[21XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfUWFAzUUN3ME2zNU45PDJ6IN88US=> NX\ySnR6W0GQR1XS
NCI-H661 NHr3cIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPRcGhDUUN3ME2zNk4xPjJ|IN88US=> NXfRXllQW0GQR1XS
NCI-H2347 MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTN{LkS4N|ch|ryP MmPTV2FPT0WU
FTC-133 NYra[2w5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLpXGZHUUN3ME2zNk44ODZizszN NIfXe5VUSU6JRWK=
COLO-829 NGryS4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\Oe2lEPTB;M{OuN|Q3PyEQvF2= MnXyV2FPT0WU
GOTO MnHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfkPWV5UUN3ME2zN{42OjV6IN88US=> MWDTRW5ITVJ?
YAPC NX7FemdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoW2TWM2OD1|Mz64NVU6KM7:TR?= NYH2WVVPW0GQR1XS
LCLC-103H NFLtWpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnL6TWM2OD1|ND6xOlI1KM7:TR?= M2TT[XNCVkeHUh?=
SiHa M1vpe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LzVWlEPTB;M{SuN|gyPyEQvF2= NFW2cFNUSU6JRWK=
LK-2 NHjsPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTN2LkW3NFgh|ryP MVPTRW5ITVJ?
KP-N-YS NUPQWHB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTN2LkeyNFIh|ryP MnSwV2FPT0WU
NCI-SNU-1 NFj0TG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7CeWloUUN3ME2zOU4yPzlizszN MXjTRW5ITVJ?
KNS-81-FD NIr1Zo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzGTW9KSzVyPUO1MlY3OyEQvF2= NFfTUIxUSU6JRWK=
SCC-9 M2q5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLvVIZlUUN3ME2zOk44OTR4IN88US=> M4XYZXNCVkeHUh?=
SH-4 NF7ETJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTlZnh6UUN3ME2zOk44OyEQvF2= MX;TRW5ITVJ?
HCC-1954 NF\kcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7wOpNKSzVyPUO3MlI4OjlizszN NGLJW|JUSU6JRWK=
BALL-1 NVLsZ|JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q5XmlEPTB;M{euOVMyPiEQvF2= M3e5OHNCVkeHUh?=
BE-13 M4Li[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq4TWM2OD1|Nz63NFE5KM7:TR?= Mnv0V2FPT0WU
COLO-678 Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm5UlB5UUN3ME2zO{46PDN5IN88US=> NETmT|NUSU6JRWK=
SK-MEL-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj5VndKSzVyPUO4MlI{QTdizszN NGLJN|ZUSU6JRWK=
OAW-28 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rFT2lEPTB;M{iuOlM6KM7:TR?= MnPIV2FPT0WU
CAMA-1 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP3fmRKSzVyPUO4Mlk3QTFizszN MmXwV2FPT0WU
C2BBe1 NEe5bo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK2VpJJUUN3ME2zPU45OThizszN MU\TRW5ITVJ?
A3-KAW M4fZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPReFVKSzVyPUSwMlM3PjFizszN MVHTRW5ITVJ?
SK-MEL-24 M{j4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTRyLkW5N|Eh|ryP MYXTRW5ITVJ?
KYSE-140 MnHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrzTWM2OD12MD63NVY2KM7:TR?= M1PjdnNCVkeHUh?=
MOLT-16 MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;JTWM2OD12MT6xOVM3KM7:TR?= NUGzSIc{W0GQR1XS
CFPAC-1 NIHIXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK5N2dKSzVyPUSyMlUzOTFizszN NVHrdGFjW0GQR1XS
NB14 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPVTWM2OD12Mj63NFI4KM7:TR?= MmPUV2FPT0WU
COLO-792 NF;jepZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfGWJVCUUN3ME20Nk45QTZzIN88US=> NHTNeJhUSU6JRWK=
RH-1 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHVWJpKSzVyPUSzMlQ5OzZizszN M{XHeXNCVkeHUh?=
NCI-H522 Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjURYdnUUN3ME20OE4{PTZ6IN88US=> NVr0N5ROW0GQR1XS
Ca-Ski MlTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDUdGJKSzVyPUS0MlgyOTRizszN NFTJfmJUSU6JRWK=
KGN Ml25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTR6LkOwOlMh|ryP M4XINXNCVkeHUh?=
UACC-62 NFPOdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPETWM2OD12OD60NFczKM7:TR?= MV\TRW5ITVJ?
NCI-H358 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTR7LkOwNVgh|ryP NXnuZ|ZwW0GQR1XS
LS-411N Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULZSHdxUUN3ME20PU4{OTF6IN88US=> MXPTRW5ITVJ?
IST-MES1 NEXBd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\3TWM2OD12OT61OlI2KM7:TR?= M3SwS3NCVkeHUh?=

... 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 (57)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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