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 MVnLbY5ie2ViQYPzZZk> NGPWTlYyKGh? NFq2OmxFVVOR MmHvTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCmZXz0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wNFMh|ryP MXqxPFc2PDZ3NB?=
Sf9 M1XQd2tqdmG|ZTDBd5NigQ>? NGf3VXYyKGh? NEnGZmlFVVOR MknTTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGgyODR5LWKgcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> MlzkNVg4PTR4NUS=
Sf9 NXu4fGFbU2mwYYPlJGF{e2G7 NGLIOpAyKGh? M4jZNWROW09? MkfZTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NGnyb4wyQDd3NE[1OC=>
Sf9 MXvLbY5ie2ViQYPzZZk> MX:xJIg> MmjxSG1UVw>? NYHzdHM{UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= M{D0R|E5PzV2NkW0
Sf9 NGD3OlNMcW6jc3WgRZN{[Xl? NXjhRoZKOSCq NF\aTJJFVVOR M2e4d2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyYXzwbIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIE> MUmxPFc2PDZ3NB?=
MDA-MB-361 NFrSbnRHfW6ldHnvckBCe3OjeR?= MnnJNkBp MUjEUXNQ M2HWOWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvODJ6IN88US=> NIfGZWQyQDd3NE[1OC=>
PC3 MU\GeY5kfGmxbjDBd5NigQ>? MVKyJIg> MlTkSG1UVw>? NEXnSYNKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? M3K3[|E5PzV2NkW0
U87MG NInFV4FHfW6ldHnvckBCe3OjeR?= NVixPIJpOiCq M3zNOmROW09? M{P5bWlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? NX;rVphvOTh5NUS2OVQ>
MDA-MB-361 NXzxdVlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu4PVYhcA>? MWPEUXNQ NIOxZWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjd{IN88US=> MWGxPFc2PDZ3NB?=
A2780 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm5OkBp MX\EUXNQ MmrRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczD3bZRpKFCLS{PDRUBidmRiUGTFUkBufXSjdHnvckB4cXSqIFnDOVAhd2ZiMD6xOEDPxE1? Mo\CNVg4PTR4NUS=
PC3 M4jBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rnV|k3KGh? MoXlSG1UVw>? Ml7VTWM2OD1yLkK4JO69VQ>? NGjUc3gyQDd3NE[1OC=>
U87MG MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYO5OkBp NVKzUGVTTE2VTx?= NHHqXFdKSzVyPUCuPVUh|ryP NHO3b3MyQDd3NE[1OC=>
Sf9 NEHrb5BMcW6jc3WgRZN{[Xl? M1fJO|MxKG2rbh?= NGL6ZXpFVVOR M{nURmlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDhcY92dnRib3[gRXRRKGOxboP1cYVlKHerdHigTWM2OCCxZjCwMlA1OiEQvF2= Mk\4NlI2PDh|NEK=
RAW 264.7 NVHJcoYyU2mwYYPlJGF{e2G7 Mn3xPVAhdWmw M2q4NGROW09? NYTkOFJIUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPL[4FudWFiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQVvUJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUig{txO MYGyNlU1QDN2Mh?=
Sf9 MWrLbY5ie2ViQYPzZZk> MlvnNUBp NITPPWNKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM[mW2YTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU1[5JINmdGy|IIfpeIghUUN3MDDv[kAxNjBzNzFOwG0> MoPGNlM2PDB4NEW=
Sf9 NV\ocmZpU2mwYYPlJGF{e2G7 NWjSOppEOSCq NVvkbpRyUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2SnbIThJIV5eHKnc4Pl[C=> MW[yN|U1ODZ2NR?=
Sf9 Mn3JT4lv[XOnIFHzd4F6 MnLmNUBp M{\ZZmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= NH;KdlgzOzV2ME[0OS=>
Sf9 MmPRT4lv[XOnIFHzd4F6 NF\EcW0yKGh? M3G5O2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXS= MUiyN|U1ODZ2NR?=
SKOV3 NFr1VZhMcW6jc3WgRZN{[Xl? MV6xJO69VQ>? NE\qd5gyKGh? MnW1SG1UVw>? NFvBcJZKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:w NXzC[IhJOjN|NkCzOFg>
MCF7 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3xNUDPxE1? Ml;iPVYhcA>? MV;EUXNQ NFjHUoFIUTVyPUCuNFcxOiEQvF2= NF6wSoMzOzN4MEO0PC=>
SKOV3 NGi5[|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTBXFcyKM7:TR?= MVm5OkBp NYPmR|NTTE2VTx?= NWflSGJMT0l3ME2wMlE1PzZizszN Mkj3NlM{PjB|NEi=
PC3 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW3NkBp NIPHfoJFVVOR NWTidoRQUUN3ME2wMlI5KM7:TR?= Mnu3NlE6QDF5MUS=
MCF7.1 NGnRcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe0eI44OiCq NGCwfJRFVVOR MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkeuNUBk\WyuczDlfJBz\XO|aX7nJGhGWjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD6yPEDPxE1? MnnxNlE6QDF5MUS=
MCF7-neo/Her2 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHyW2k4OiCq NIPrZ3VFVVOR NWrvS3F5UUN3ME2wMlI6KM7:TR?= NXfJNVBOOjN4NkK5NFM>
MCF7-neo/Her2 MYTLbY5ie2ViQYPzZZk> NWPyTVlMUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzD3bZRpKEmFNUCgc4YhOC5yMEeg{txO M1;hUlI{PjZ{OUCz
PC3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXRO|IhcA>? Mn\MSG1UVw>? MVXFR|UxRTBwM{Sg{txO NYrTZ4VvOjF7OEW2N|k>
MCF7.1 NFvLPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorMO|IhcA>? NEXjR4NFVVOR M4r2RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFXDOVAhd2ZiMD6zPUDPxE1? M3\rfFIyQTh3NkO5
PC3 NVnNenhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHhOow4OiCq M1\FXmROW09? NED0cZZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDk[YZq[2mnboSgbY4hWFSHTjD3bZRpKEmFNUCgc4YhOC5|OTFOwG0> MXGyNFA2ODZ4OR?=
MCF7.1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLMR2w4OiCq MUnEUXNQ NXfEV211SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFibYX0ZY51KHerdHigTWM2OCCxZjCwMlM1KM7:TR?= MnnLNlAxPTB4Nkm=
MCF7.1 MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPVO|IhcA>? NFjhXZdGSzVyPUCuO|Ih|ryP MYWyNFM1PjZ3Nh?=
NCI-H1975 NILEN4FEgXSxdH;4bYMhSXO|YYm= NU\4e5o4PzJiaB?= MWLJR|UxRTBwMkeg{txO NXS4Z49MOjNyNUm1OFU>
H460 MY\DfZRwfG:6aXOgRZN{[Xl? NULBWVlWPzJiaB?= NEHIOotKSzVyPUCuPFch|ryP M2\TU|I{ODV7NUS1
HT-29 M2TxSGN6fG:2b4jpZ{BCe3OjeR?= M4LBb|czKGh? M3\YSWlEPTB;MD62OkDPxE1? MkH5NlMxPTl3NEW=
HepG2 M4LHT2N6fG:2b4jpZ{BCe3OjeR?= MnHBO|IhcA>? NHnHPXVKSzVyPUGg{txO MWKyN|A2QTV2NR?=
SGC7901 NIr0OGZEgXSxdH;4bYMhSXO|YYm= MY[3NkBp NH\5dItKSzVyPUGuPEDPxE1? MXSyN|A2QTV2NR?=
NCI-H226 M{HJVGN6fG:2b4jpZ{BCe3OjeR?= MlPSO|IhcA>? NEnNfXNKSzVyPUKuPUDPxE1? NGTUXXQzOzB3OUW0OS=>
A549 NIGzeINEgXSxdH;4bYMhSXO|YYm= NXPXS3Y6PzJiaB?= MWfJR|UxRTZwOTFOwG0> MYiyN|A2QTV2NR?=
U87MG NE\JNpJEgXSxdH;4bYMhSXO|YYm= M4nTVFczKGh? NHfENZRKSzVyPUeuO|ch|ryP MUiyN|A2QTV2NR?=
HBC4 NIrSS5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDRU21td2eJSUWwQU03NjB|IF2= NY[3[|lTOjJ|M{[yOFY>
BSY1 NWHrRmx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDsc4dIUTVyPT22MlkxKE1? M4Phd|IzOzN4MkS2
HBC5 NYrCVlNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljscI9oT0l3ME2tOk43OCCP NWLDS3ZHOjJ|M{[yOFY>
MCF7 M2m0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\sc4dIUTVyPT23MlM{KE1? M33zTlIzOzN4MkS2
MDA-MB-231 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH4VmtzdG:pR1m1NF0uPS52NjDN MUOyNlM{PjJ2Nh?=
U251 M{O3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rreIxw\0eLNUC9MVUvPTBiTR?= Mo\NNlI{OzZ{NE[=
SF268 M1jBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NICx[Yptd2eJSUWwQU02NjN7IF2= NVW1cotsOjJ|M{[yOFY>
SF295 NG\5VVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7sc4dIUTVyPT22MlM4KE1? NXXqPGlkOjJ|M{[yOFY>
SF539 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{WxN4xw\0eLNUC9MVYvPTBiTR?= MVWyNlM{PjJ2Nh?=
SNB75 NWnZVXVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPtSHNtd2eJSUWwQU04NjFyIF2= M4[yOlIzOzN4MkS2
SNB78 NVvSeWdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXVZmptd2eJSUWwQU03NjV{IF2= MXqyNlM{PjJ2Nh?=
HCC2998 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zIcoxw\0eLNUC9MVYvOjliTR?= M2nUSVIzOzN4MkS2
KM12 M1HLU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHwcI9oT0l3ME2tOU44PiCP MlnoNlI{OzZ{NE[=
HT-29 NGm4SVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnCe5Ntd2eJSUWwQU03NjNyIF2= M{TBeVIzOzN4MkS2
HCT15 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\sc4dIUTVyPT22MlEzKE1? NFL2OJUzOjN|NkK0Oi=>
HCT116 M{DkWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3aRYdbdG:pR1m1NF0uPS56NzDN NVy2PFdzOjJ|M{[yOFY>
NCI-H23 NF\qOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:wc4xw\0eLNUC9MVUvPzNiTR?= NYDxOGFbOjJ|M{[yOFY>
NCI-H226 M4HxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XtRoxw\0eLNUC9MVYvOjFiTR?= MYCyNlM{PjJ2Nh?=
NCI-H522 NHvUeXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjUe2Ztd2eJSUWwQU03NjV6IF2= NUTxcoZiOjJ|M{[yOFY>
NCI-H483 NXvNVYxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3wcI9oT0l3ME2tOk42PiCP NGrDSIgzOjN|NkK0Oi=>
A549 MlzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX0O5J4dG:pR1m1NF0uPi5zNTDN MVqyNlM{PjJ2Nh?=
DMS273 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjsc4dIUTVyPT22MlQ{KE1? NWftOpp4OjJ|M{[yOFY>
DMS114 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XPRoxw\0eLNUC9MVUvQTJiTR?= M2TINFIzOzN4MkS2
LOXIMVI NFzyb5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHBcYtzdG:pR1m1NF0uPi5{OTDN MkfMNlI{OzZ{NE[=
OVCAR3 NYfmeYVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3sc4dIUTVyPT22MlcyKE1? MlXUNlI{OzZ{NE[=
OVCAR4 NFTDd49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\6UYxw\0eLNUC9MVUvPzZiTR?= MWSyNlM{PjJ2Nh?=
OVCAR5 NXTTNINQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjOTI5td2eJSUWwQU03NjJ4IF2= MVmyNlM{PjJ2Nh?=
OVCAR8 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HxPYxw\0eLNUC9MVUvPzNiTR?= M2T0NFIzOzN4MkS2
SKOV3 M2O3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDoOZZtd2eJSUWwQU03NjV{IF2= M{LzclIzOzN4MkS2
RXF631L NHfiVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGX4WlNtd2eJSUWwQU03Njh6IF2= NFPhRo4zOjN|NkK0Oi=>
ACHN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYntVFIydG:pR1m1NF0uPi5yNzDN M{HI[|IzOzN4MkS2
St-4 NWTSPYVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:0[W5td2eJSUWwQU02NjV4IF2= NELMVHUzOjN|NkK0Oi=>
MKN1 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LTXIxw\0eLNUC9MVcvODhiTR?= M4TyfFIzOzN4MkS2
MKN7 NXXRcJhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDsc4dIUTVyPT22MlUxKE1? MmHONlI{OzZ{NE[=
MKN28 MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHsc4dIUTVyPT21MlUzKE1? NV;veZVoOjJ|M{[yOFY>
MKN45 NIP0e2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHXcI9oT0l3ME2tOk42PSCP MofMNlI{OzZ{NE[=
MKN74 NYPCVVk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrsc4dIUTVyPT22MlAzKE1? MmTyNlI{OzZ{NE[=
DU145 M1vPW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX0PWltd2eJSUWwQU02Njh3IF2= MV:yNlM{PjJ2Nh?=
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HAL-01 NH\rR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojVTWM2OD1{ME[uO|Mhdk1? M3XkOHNCVkeHUh?=
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OVCAR-5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PQWWlEPTB;OUSwMlE4KG6P M{jvOnNCVkeHUh?=
HDLM-2 NGjFb2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrCd2NKSzVyPUm0PU4zKG6P Mlm3V2FPT0WU
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SK-MEL-28 NH\xbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLnVoVKSzVyPUGuOVYxQDVizszN MWHTRW5ITVJ?
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KARPAS-299 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHKVIdnUUN3ME2yN{4{QDh5IN88US=> MXzTRW5ITVJ?
NCI-H1650 NFTzZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7hOmNQUUN3ME2yN{46OjRzIN88US=> M1L4WnNCVkeHUh?=
ACHN NIW2c5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zjV2lEPTB;MkSuOFY2PiEQvF2= M3KyU3NCVkeHUh?=
M059J M{Dn[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJ2LkW2N|Qh|ryP MmjrV2FPT0WU
AM-38 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJ3LkS4NUDPxE1? MYjTRW5ITVJ?
KG-1 M4nLfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPZN3BwUUN3ME2yOU42PDl2IN88US=> MYPTRW5ITVJ?
COLO-824 M3uz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJ3LkW1PVkh|ryP MnT0V2FPT0WU
NCI-H1155 M{LZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfWTWM2OD1{NT61PFQ4KM7:TR?= MWXTRW5ITVJ?
NCI-H441 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXNTWM2OD1{NT63OFY2KM7:TR?= NYPHb5ZtW0GQR1XS
J-RT3-T3-5 NFzyV3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS3S4RWUUN3ME2yOk4{ODJ5IN88US=> M4jWe3NCVkeHUh?=
JEG-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml32TWM2OD1{Nj62PFA2KM7:TR?= MkPuV2FPT0WU
RKO MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ4Lke2N|Ih|ryP NYXpcmdKW0GQR1XS
CAL-85-1 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ5LkKxNVgh|ryP MlfVV2FPT0WU
CAL-120 NFPJSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJ5Lk[5NVQh|ryP MlLKV2FPT0WU
NCI-H2452 Mom1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfkTWM2OD1{Nz63O|E3KM7:TR?= M{DjTXNCVkeHUh?=
NCI-H1395 NUHjTmxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke5TWM2OD1{Nz63PFM{KM7:TR?= M2LMXXNCVkeHUh?=
KYSE-450 MkTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDuTWM2OD1{Nz65PFYzKM7:TR?= MoXzV2FPT0WU
S-117 NUjFUpFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33TPWlEPTB;MkmuN|g2PyEQvF2= M2fSeXNCVkeHUh?=
SW13 MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvMTGpKSzVyPUK5Mlg2OTlizszN NVL5RWxzW0GQR1XS
ES3 NIHWNmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DwVmlEPTB;M{CuN|c{OyEQvF2= NYLLeml4W0GQR1XS
HCT-116 Mnq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHJTWM2OD1|MD61OVU1KM7:TR?= Ml\EV2FPT0WU
NCI-H1693 NH\o[lZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzR[5FwUUN3ME2zNE42QTR{IN88US=> M1rpWnNCVkeHUh?=
VM-CUB-1 MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTNyLk[0NVMh|ryP NIr1cWpUSU6JRWK=
NCI-H2170 NEPuTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofTTWM2OD1|MT61O|g1KM7:TR?= MWHTRW5ITVJ?
ALL-PO NGjwWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDzTWM2OD1|MT64OFI5KM7:TR?= MXfTRW5ITVJ?
NCI-H661 NU\Ve2J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPnOZFKSzVyPUOyMlA3OjNizszN MXHTRW5ITVJ?
NCI-H2347 NYnNRW13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X5XGlEPTB;M{KuOFg{PyEQvF2= NVjKXno{W0GQR1XS
FTC-133 NUDwS5A2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLV[3cyUUN3ME2zNk44ODZizszN M4TUUXNCVkeHUh?=
COLO-829 Mo\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzmZlZmUUN3ME2zN{4{PDZ5IN88US=> NHLSXHlUSU6JRWK=
GOTO NXPENHRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHLXlJvUUN3ME2zN{42OjV6IN88US=> NVHHXJk1W0GQR1XS
YAPC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fnWGlEPTB;M{OuPFE2QSEQvF2= NHLLSWtUSU6JRWK=
LCLC-103H MnfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF25[HpKSzVyPUO0MlE3OjRizszN NI\UUolUSU6JRWK=
SiHa M3LXd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe0Vo53UUN3ME2zOE4{QDF5IN88US=> MVLTRW5ITVJ?
LK-2 MlfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\lNoVVUUN3ME2zOE42PzB6IN88US=> NFrwUHNUSU6JRWK=
KP-N-YS NFzSfWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrVdVNKSzVyPUO0MlczODJizszN NWDtOnlpW0GQR1XS
NCI-SNU-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrtW5FKSzVyPUO1MlE4QSEQvF2= NV\DfmE1W0GQR1XS
KNS-81-FD NGGyToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Lv[GlEPTB;M{WuOlY{KM7:TR?= MVnTRW5ITVJ?
SCC-9 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\BbnhKSzVyPUO2MlcyPDZizszN MXLTRW5ITVJ?
SH-4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnpfYxKSzVyPUO2Mlc{KM7:TR?= NGnwW5JUSU6JRWK=
HCC-1954 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN5LkK3Nlkh|ryP MVHTRW5ITVJ?
BALL-1 NYWzU|dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3WVmVKSzVyPUO3MlU{OTZizszN MULTRW5ITVJ?
BE-13 M33BV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITkeotKSzVyPUO3MlcxOThizszN NFfqfmhUSU6JRWK=
COLO-678 MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnBPWFXUUN3ME2zO{46PDN5IN88US=> Mn:5V2FPT0WU
SK-MEL-3 M3PF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PWT2lEPTB;M{iuNlM6PyEQvF2= NYKxTYpKW0GQR1XS
OAW-28 NH7FdHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XXOmlEPTB;M{iuOlM6KM7:TR?= MnvqV2FPT0WU
CAMA-1 M4DyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPwTWM2OD1|OD65OlkyKM7:TR?= MmLjV2FPT0WU
C2BBe1 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nPbmlEPTB;M{muPFE5KM7:TR?= NY[0c4FHW0GQR1XS
A3-KAW MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTRyLkO2OlEh|ryP M3jF[3NCVkeHUh?=
SK-MEL-24 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHoTWM2OD12MD61PVMyKM7:TR?= NYjxPJF7W0GQR1XS
KYSE-140 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z0RWlEPTB;NECuO|E3PSEQvF2= MVPTRW5ITVJ?
MOLT-16 M1ztNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXv[JJKSzVyPUSxMlE2OzZizszN M2\IbnNCVkeHUh?=
CFPAC-1 NFe5NJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3O3[2lEPTB;NEKuOVIyOSEQvF2= NUXwd2Y5W0GQR1XS
NB14 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3RTWM2OD12Mj63NFI4KM7:TR?= M{iyT3NCVkeHUh?=
COLO-792 NFHmSZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzndFJKSzVyPUSyMlg6PjFizszN MUDTRW5ITVJ?
RH-1 M1jD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTJTWM2OD12Mz60PFM3KM7:TR?= MXjTRW5ITVJ?
NCI-H522 NF\6bIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\FW2lEPTB;NESuN|U3QCEQvF2= MlLIV2FPT0WU
Ca-Ski NXnkeHBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTR2LkixNVQh|ryP NEj2NIdUSU6JRWK=
KGN MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\WTWM2OD12OD6zNFY{KM7:TR?= NFvJSXNUSU6JRWK=
UACC-62 M1:zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\iXVltUUN3ME20PE41ODd{IN88US=> MmfEV2FPT0WU
NCI-H358 M1y3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{iyT2lEPTB;NEmuN|AyQCEQvF2= MUPTRW5ITVJ?
LS-411N NXjSPJdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELEcnNKSzVyPUS5MlMyOThizszN M1u0eHNCVkeHUh?=
IST-MES1 M4mxcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTR7LkW2NlUh|ryP NIKyVZpUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo試験 Administration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. [1] Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. [2] GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases. [4]
臨床試験 A Phase I study of GDC-0941 in patients with locally advanced or metastatic solid tumors, Non-Hodgkin's lymphoma, or multiple myeloma (MM) (expansion stage only) for which standard therapy either does not exist or has proven ineffective or intolerable is
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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

細胞アッセイ: [2]

細胞株 SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, and MKN-7 cells
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 48 and 72 hours
実験の流れ Cells are exposed to various concentrations of GDC-0941 for 48, and 72 hours. Proliferation/viability of cells is detected by using the CellTiter-Glo Luminescent Cell Viability Assay. The pAkt (Ser473), cleaved caspase-3, and cleaved PARP are analyzed by western blot. The Caspase-Glo 3/7 assay and the Cell Death Detection ELISAplus assay are used to detect caspase 3/7 activity, and apoptosis, respectively.

動物実験: [2]

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

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

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

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

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

参考

化学情報

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

C23H27N7O3S2

CAS No. 957054-30-7
保管 3年-20℃
2年-80℃in solvent
別名 RG7321
溶解度 (25°C) * In vitro DMSO 44 mg/mL (85.66 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidine

文献中の引用 (57)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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