Pictilisib (GDC-0941)

For research use only. Not for use in humans.

目录号：S1065 别名： RG7321

Pictilisib (GDC-0941) Chemical Structure

CAS No. 957054-30-7

Pictilisib (GDC-0941, RG7321) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Pictilisib (GDC-0941) 可诱导自噬和凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1972.48 现货
RMB 986.88 现货
RMB 1390.74 现货
RMB 3026.17 现货
RMB 7926.11 现货
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客户使用Selleck生产的Pictilisib (GDC-0941)发表文献327篇：

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Pictilisib (GDC-0941, RG7321) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Pictilisib (GDC-0941) 可诱导自噬和凋亡。Phase 2。
靶点
p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)		 p110γ [1]
(Cell-free assay)		 mTOR [1]
(Cell-free assay)
3 nM 3 nM 33 nM 75 nM 0.58 μM(Ki app)
体外研究

GDC-0941也等效作用于PI3Kα和 PI3Kδ和PI3Kα突变型E545-K和H1047-R,也选择性作用于PI3Kβ(10倍)和 PI3Kγ(25倍), 选择性更高地作用于PI3K II, III, 和IV类成员，包括, C2β, Vps34, DNA-PK和mTOR。GDC-0941 作用于U87MG, PC3, 和 MDA-MB-361 细胞，有效抑制Akt磷酸化，IC50分别为46 nM, 37 nM,和 28 nM。GDC-0941抑制U87MG, A2780, PC3, 和MDA-MB-361细胞增殖，IC50分别为 0.95 μM, 0.14 μM, 0.28 μM, 和0.72 μM。[1]GDC-0941处理，有效抑制对Trastuzumab敏感和不敏感的HER2扩增细胞增殖，IC50为149-944 nM,与 Trastuzumab敏感性无关。GDC-0941抑制含PIK3CA突变的HER2扩增的细胞增殖，IC50<500 nM, 且有效抑制抗trastuzumab 的HER2 扩增乳腺癌细胞增殖和活力。[2]GDC-0941 显著抑制HCT116, DLD1和 HT29细胞生长，GI50分别为1081 nM, 1070 nM 和157 nM。[4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 NWHtZ5J[U2mwYYPlJGF{e2G7 MYexJIg> NGK0NJBFVVOR M4G5SWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUFmzT{BxOTFyZHXseIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFA{KM7:TR?= MX:xPFc2PDZ3NB?=
Sf9 MmLDT4lv[XOnIFHzd4F6 MVyxJIg> MYjEUXNQ MlfYTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGgyODR5LWKgcZV1[W62IHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIIC4OYFteGijIIfpeIghUUN3MDDv[kAxNjByMzFOwG0> MX2xPFc2PDZ3NB?=
Sf9 NEXqd|hMcW6jc3WgRZN{[Xl? MVWxJIg> MVnEUXNQ NYnZRZRwUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEV3NEWtT{BufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMECzJO69VQ>? MkHyNVg4PTR4NUS=
Sf9 M2HDOGtqdmG|ZTDBd5NigQ>? MYWxJIg> M1HoWmROW09? NUHEWo9TUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZ49mgHC{ZYPzbY5oKHB6NXHsdIhiKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= NV;XSGE5OTh5NUS2OVQ>
Sf9 MkjiT4lv[XOnIFHzd4F6 M{XyOlEhcA>? MVXEUXNQ MkfUTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> MnXrNVg4PTR4NUS=
MDA-MB-361 MoG2SpVv[3Srb36gRZN{[Xl? M1vROlIhcA>? MYnEUXNQ NHTHVpFKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3ERU1OSi1|NkGgZ4VtdHNid3n0bEBRUUt|Q1GgSVU1PS2NIH31eIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{ODFOwG0> NEjuWVQyQDd3NE[1OC=>
PC3 NGn1S2xHfW6ldHnvckBCe3OjeR?= NEjhRmUzKGh? NGLyeoRFVVOR M4jMR2lvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGDDN{Bk\WyuczD3bZRpKEmFNUCgc4YhOC5yM{eg{txO MnLTNVg4PTR4NUS=
U87MG NY\Ieox7TnWwY4Tpc44hSXO|YYm= NI\p[YQzKGh? MWXEUXNQ NFXrbopKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFnDOVAhd2ZiMD6wOFYh|ryP MlrsNVg4PTR4NUS=
MDA-MB-361 NX3SW3B6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17WPFk3KGh? NHHlXYRFVVOR MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlczKM7:TR?= NVfQWpRKOTh5NUS2OVQ>
A2780 NXnoOo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPQPVYhcA>? NV3RRZBPTE2VTx?= NEPaXpBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiUFnLN2NCKGGwZDDQWGVPKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlE1KM7:TR?= MVexPFc2PDZ3NB?=
PC3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT4V5BpQTZiaB?= M1ToRWROW09? M3HaNGlEPTB;MD6yPEDPxE1? NEPLUpEyQDd3NE[1OC=>
U87MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC1XFV[QTZiaB?= NUj6O5JmTE2VTx?= MXrJR|UxRTBwOUWg{txO NIW1[lIyQDd3NE[1OC=>
Sf9 M3z3[WtqdmG|ZTDBd5NigQ>? NVjKZ4R{OzBibXnu Mm\DSG1UVw>? MULJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiYX3veY51KG:oIFHUVEBkd26|dX3l[EB4cXSqIFnDOVAhd2ZiMD6wOFIh|ryP NIHubpIzOjV2OEO0Ni=>
RAW 264.7 NYixN4hXU2mwYYPlJGF{e2G7 NYq5e3A6QTBibXnu MmjJSG1UVw>? MXPJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlI6QCEQvF2= NGXveW0zOjV2OEO0Ni=>
Sf9 MUHLbY5ie2ViQYPzZZk> MVKxJIg> M4HSc2lvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2tj\XSjIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVRkmgZ4VtdHNid3n0bEBKSzVyIH;mJFAvODF5IN88US=> MkX1NlM2PDB4NEW=
Sf9 MXzLbY5ie2ViQYPzZZk> MXWxJIg> NFnyWFFKdmirYnn0bY9vKG:oIFfTWE1nfXOnZDDoeY1idiC{ZXPvcYJqdmGwdDDQTVNM\GWudHGg[ZhxemW|c3Xk NXPQU|ZUOjN3NEC2OFU>
Sf9 NG\tT|FMcW6jc3WgRZN{[Xl? MljzNUBp Mn[1TY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4didW2jIHX4dJJme3OnZB?= M3TnfVI{PTRyNkS1
Sf9 MkDBT4lv[XOnIFHzd4F6 MVKxJIg> MV7Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm NEHScXUzOzV2ME[0OS=>
SKOV3 M37DOGtqdmG|ZTDBd5NigQ>? NHrHNIQyKM7:TR?= MUSxJIg> MoS2SG1UVw>? Mlv4TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? NXHzbZZ[OjN|NkCzOFg>
MCF7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIX1ZnYyKM7:TR?= M3j0[lk3KGh? M{m3[GROW09? MoWyS2k2OD1yLkC3NFIh|ryP M{C4UlI{OzZyM{S4
SKOV3 MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHrWFQyKM7:TR?= NI\OeHA6PiCq MYHEUXNQ NVraNG91T0l3ME2wMlE1PzZizszN M322blI{OzZyM{S4
PC3 M{HjZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp MWjEUXNQ M3v6fmlEPTB;MD6yPEDPxE1? NXLvU|htOjF7OEG3NVQ>
MCF7.1 MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXK3NkBp NV;UVWxQTE2VTx?= NV;aXYwySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NjFiY3XscJMh\XiycnXzd4lv\yCKRWKyJIdmdmVid3n0bEBKSzVyIH;mJFAvOjhizszN NFy4SIkzOTl6MUexOC=>
MCF7-neo/Her2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfo[2dxPzJiaB?= MYnEUXNQ MVnJR|UxRTBwMkmg{txO MV:yN|Y3OjlyMx?=
MCF7-neo/Her2 NXjRboJOU2mwYYPlJGF{e2G7 MnjYTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC5aYToJGlEPTBib3[gNE4xODdizszN NGntSWYzOzZ4MkmwNy=>
PC3 MlmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHFfJQ4OiCq NGL1NHNFVVOR MnWwSWM2OD1yLkO0JO69VQ>? MkjwNlE6QDV4M{m=
MCF7.1 M3zrb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV63NkBp MmP5SG1UVw>? MkCwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? NFX2fpQzOTl6NU[zPS=>
PC3 Mn23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP5Z4E4OiCq MV;EUXNQ MnK1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiZHXmbYNq\W62IHnuJHBVTU5id3n0bEBKSzVyIH;mJFAvOzlizszN MYGyNFA2ODZ4OR?=
MCF7.1 NIHzT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf2PIpNPzJiaB?= M4fORWROW09? M3Lkc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKG23dHHueEB4cXSqIFnDOVAhd2ZiMD6zOEDPxE1? MYKyNFA2ODZ4OR?=
MCF7.1 MkP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUC3NkBp M{LDSWVEPTB;MD63NkDPxE1? MVOyNFM1PjZ3Nh?=
NCI-H1975 MWrDfZRwfG:6aXOgRZN{[Xl? MX63NkBp MojxTWM2OD1yLkK3JO69VQ>? NVi1fmNkOjNyNUm1OFU>
H460 Mlr5R5l1d3SxeHnjJGF{e2G7 MoWxO|IhcA>? NIPlTlNKSzVyPUCuPFch|ryP M3Tx[FI{ODV7NUS1
HT-29 NV\YOnNrS3m2b4TvfIlkKEG|c3H5 NX\rTWZsPzJiaB?= MorKTWM2OD1yLk[2JO69VQ>? NETkUFMzOzB3OUW0OS=>
HepG2 M{fVc2N6fG:2b4jpZ{BCe3OjeR?= M{LhWlczKGh? NHLCXWxKSzVyPUGg{txO MYCyN|A2QTV2NR?=
SGC7901 MXPDfZRwfG:6aXOgRZN{[Xl? NY\oSXZUPzJiaB?= MkPETWM2OD1zLkig{txO NUjKc5BIOjNyNUm1OFU>
NCI-H226 MkX2R5l1d3SxeHnjJGF{e2G7 MonqO|IhcA>? NXLXd4I5UUN3ME2yMlkh|ryP MXyyN|A2QTV2NR?=
A549 MluzR5l1d3SxeHnjJGF{e2G7 M3jrZ|czKGh? M3LRVGlEPTB;Nj65JO69VQ>? NEHpfnIzOzB3OUW0OS=>
U87MG NWnkepZtS3m2b4TvfIlkKEG|c3H5 NX74[G81PzJiaB?= M17wdmlEPTB;Nz63O{DPxE1? MnPDNlMxPTl3NEW=
HBC4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjnfHBRdG:pR1m1NF0uPi5yMzDN MXyyNlM{PjJ2Nh?=
BSY1 NFTpZnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\scpNtd2eJSUWwQU03NjlyIF2= Mm\iNlI{OzZ{NE[=
HBC5 NIrQVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPoWG1rdG:pR1m1NF0uPi54MDDN NE[4Z4EzOjN|NkK0Oi=>
MCF7 M{XaXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDsc4dIUTVyPT23MlM{KE1? NXy1W2RyOjJ|M{[yOFY>
MDA-MB-231 M1\Oemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPrRZlzdG:pR1m1NF0uPS52NjDN NIGxUW8zOjN|NkK0Oi=>
U251 Mn\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq1N3Rtd2eJSUWwQU02NjVyIF2= MWeyNlM{PjJ2Nh?=
SF268 NXjNU25kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfsc4dIUTVyPT21MlM6KE1? NWjsSolXOjJ|M{[yOFY>
SF295 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33YSoxw\0eLNUC9MVYvOzdiTR?= M3mxSVIzOzN4MkS2
SF539 MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHsc4dIUTVyPT22MlUxKE1? NWPxNIxXOjJ|M{[yOFY>
SNB75 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzBRoRtd2eJSUWwQU04NjFyIF2= M1PDXlIzOzN4MkS2
SNB78 M1PFNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXsc4dIUTVyPT22MlUzKE1? NH\KO28zOjN|NkK0Oi=>
HCC2998 NITDXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO0cI9oT0l3ME2tOk4zQSCP NXTVUHlzOjJ|M{[yOFY>
KM12 NIHU[mNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7scI9oT0l3ME2tOU44PiCP MnjFNlI{OzZ{NE[=
HT-29 NEPQV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDjcI9oT0l3ME2tOk4{OCCP M3SzXFIzOzN4MkS2
HCT15 NFvPUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljocI9oT0l3ME2tOk4yOiCP MY[yNlM{PjJ2Nh?=
HCT116 NHPUNZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M173Noxw\0eLNUC9MVUvQDdiTR?= NW[0Nll3OjJ|M{[yOFY>
NCI-H23 M3LDcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXqcI9oT0l3ME2tOU44OyCP MYGyNlM{PjJ2Nh?=
NCI-H226 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvLZ5Y6dG:pR1m1NF0uPi5{MTDN NEfoS|czOjN|NkK0Oi=>
NCI-H522 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Psb4xw\0eLNUC9MVYvPThiTR?= MVmyNlM{PjJ2Nh?=
NCI-H483 NH7hT4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXf5OIFXdG:pR1m1NF0uPi53NjDN MmDqNlI{OzZ{NE[=
A549 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPBfoVtd2eJSUWwQU03NjF3IF2= M3vPTVIzOzN4MkS2
DMS273 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M332[Ixw\0eLNUC9MVYvPDNiTR?= NX60c4Z3OjJ|M{[yOFY>
DMS114 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHGzdpdtd2eJSUWwQU02Njl{IF2= M{nVTlIzOzN4MkS2
LOXIMVI M3S1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rPXYxw\0eLNUC9MVYvOjliTR?= NULhTIdROjJ|M{[yOFY>
OVCAR3 MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;uTot5dG:pR1m1NF0uPi55MTDN MWKyNlM{PjJ2Nh?=
OVCAR4 M4H4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DXW4xw\0eLNUC9MVUvPzZiTR?= NIDwWGYzOjN|NkK0Oi=>
OVCAR5 M4fhbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\obnVEdG:pR1m1NF0uPi5{NjDN MWeyNlM{PjJ2Nh?=
OVCAR8 Mk\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEezb4xtd2eJSUWwQU02Njd|IF2= M4DsOFIzOzN4MkS2
SKOV3 NUf5dZMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO0Sodtd2eJSUWwQU03NjV{IF2= NIHscIkzOjN|NkK0Oi=>
RXF631L NWDCR3pPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnld3dtd2eJSUWwQU03Njh6IF2= NH\RRm8zOjN|NkK0Oi=>
ACHN M2\aVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LPNIxw\0eLNUC9MVYvODdiTR?= MUGyNlM{PjJ2Nh?=
St-4 NE\Ze|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnsc4dIUTVyPT21MlU3KE1? Ml:1NlI{OzZ{NE[=
MKN1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHPcYFtd2eJSUWwQU04NjB6IF2= NGfqblczOjN|NkK0Oi=>
MKN7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULsc4dIUTVyPT22MlUxKE1? NVPWeYJCOjJ|M{[yOFY>
MKN28 NWK5RpN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDHcI9oT0l3ME2tOU42OiCP NGO1WI8zOjN|NkK0Oi=>
MKN45 NIruZ|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7Fc29{dG:pR1m1NF0uPi53NTDN MU[yNlM{PjJ2Nh?=
MKN74 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjGOXFodG:pR1m1NF0uPi5yMjDN MYeyNlM{PjJ2Nh?=
DU145 M176S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHnVZBMdG:pR1m1NF0uPS56NTDN NF25PJkzOjN|NkK0Oi=>
PC3 M2nKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPtdJRHdG:pR1m1NF0uPi54NjDN NGTOe5UzOjN|NkK0Oi=>
ES5 M4PNdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq5VoFKSzVyPUWwMlIyKG6P NIPrbmRUSU6JRWK=
HH M33rOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK1TWM2OD1zMUGuNFghdk1? M3H0[3NCVkeHUh?=
MHH-PREB-1 NFHiPZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFzND6zJI5O Ml\EV2FPT0WU
NCI-H1770 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLLPHRKSzVyPUGyN{45PiCwTR?= MnzrV2FPT0WU
HuO9 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[yOZVoUUN3ME2yNFYvODJibl2= MWXTRW5ITVJ?
HAL-01 NX;kN3o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;y[HZKSzVyPUKwOk44OyCwTR?= NF21RWxUSU6JRWK=
NOS-1 Mn\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nKV2lEPTB;MkGxMlgzKG6P MUPTRW5ITVJ?
HGC-27 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3iTWM2OD1{MUKuOVchdk1? NWLGc3lrW0GQR1XS
NB69 M4LDSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmqwTWM2OD1{NEWuNlchdk1? MnPJV2FPT0WU
RS4-11 NWPjWYF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jSZmlEPTB;Mk[xMlc3KG6P NVfSc|hkW0GQR1XS
DOK NWK2coozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jXSmlEPTB;M{CxMlchdk1? MV7TRW5ITVJ?
LB2241-RCC NIPFfXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTNyMz64OEBvVQ>? MnHaV2FPT0WU
NCI-H1623 NHXySZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNyND6wPEBvVQ>? M3zkbHNCVkeHUh?=
YH-13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP3O2s2UUN3ME2zNFQvOzJibl2= NUfmdHBtW0GQR1XS
BPH-1 M2PnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfiXZRPUUN3ME2zNVQhdk1? MmS2V2FPT0WU
AN3-CA NWn0[XV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTN2MD6zO{BvVQ>? Mn7lV2FPT0WU
ES7 M{PoeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jHbGlEPTB;M{SxMlk6KG6P M2HvZXNCVkeHUh?=
MDA-MB-175-VII MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3njSWlEPTB;M{WyMlkzKG6P NG[0Z4RUSU6JRWK=
GAMG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml30TWM2OD1|N{CuPFUhdk1? NIqzNo9USU6JRWK=
CHL-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq0eGhCUUN3ME2zO|gvPjVibl2= NGSz[JBUSU6JRWK=
NB7 M4rnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;jS|l5UUN3ME2zPFkvQDNibl2= MWPTRW5ITVJ?
MFE-280 Mm\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XiTGlEPTB;NEG4MlIhdk1? MUTTRW5ITVJ?
HL-60 M4T4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPOTWM2OD12MkWuO|Uhdk1? MkfPV2FPT0WU
GCIY M2\Bb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHheod4UUN3ME20N|MvQCCwTR?= MV7TRW5ITVJ?
MDA-MB-361 M3\zS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3pXo43UUN3ME20N|kvOTNibl2= M{X2[3NCVkeHUh?=
LXF-289 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TtN2lEPTB;NES4MlI4KG6P NH7oVVFUSU6JRWK=
NBsusSR M3KxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX6TWM2OD12OEiuPFUhdk1? M3vSfHNCVkeHUh?=
KU-19-19 NVjre2ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzlepF[UUN3ME21NVYvODdibl2= MXrTRW5ITVJ?
A204 NHPW[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTV{Mj6zN{BvVQ>? MmjBV2FPT0WU
LB1047-RCC NU\EfZZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjRfXg2UUN3ME21NlIvQTNibl2= MorYV2FPT0WU
COLO-684 NXT4VZF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTV{Mz6xNUBvVQ>? MV;TRW5ITVJ?
PA-1 NEL6c3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTV|Mj60NUBvVQ>? M{XhbnNCVkeHUh?=
MG-63 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\uXWlEPTB;NUSxMlEyKG6P NEPPeJVUSU6JRWK=
BHT-101 M4nIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX6UYFKSzVyPUW0OE46PCCwTR?= M1[3UXNCVkeHUh?=
NKM-1 NEXwUlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HteWlEPTB;NUmzMlA6KG6P MVLTRW5ITVJ?
T47D M4XnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j6WWlEPTB;NUm3MlU3KG6P MlfJV2FPT0WU
MOLT-4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTZ{Mz62NkBvVQ>? NYThRXdzW0GQR1XS
IGROV-1 M1fkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX2TWM2OD14M{SuN|Ehdk1? M3\wOHNCVkeHUh?=
ES4 M2LIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzuTWM2OD14M{muOVQhdk1? MlqzV2FPT0WU
HuO-3N1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LvUWlEPTB;NkSyMlM5KG6P MnXCV2FPT0WU
NEC8 M2SycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTZ3Mz61O{BvVQ>? MVjTRW5ITVJ?
HO-1-N-1 MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\INpFKSzVyPU[1PU4yPyCwTR?= MXLTRW5ITVJ?
EPCL-272H MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LFeGlEPTB;Nki3MlIyKG6P NVXaVWxrW0GQR1XS
D-263MG MoLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i2UWlEPTB;N{G4MlEhdk1? MYHTRW5ITVJ?
MV-4-11 NHnWWm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm2VYk6UUN3ME23NlQvOzFibl2= NULDbZlkW0GQR1XS
SK-NEP-1 NWXsZYZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:xcpJkUUN3ME23NlUvQTRibl2= NGfWU2VUSU6JRWK=
SW872 NVLUR4VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrDdW9UUUN3ME23NlcvQDlibl2= M163W3NCVkeHUh?=
P30-OHK M12z[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T4UGlEPTB;N{OwMlcyKG6P NX2weWY{W0GQR1XS
OMC-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXjNY1KSzVyPUe1NU4xQSCwTR?= NFHE[WhUSU6JRWK=
LoVo MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDLTWM2OD15N{euPUBvVQ>? NEjpSWxUSU6JRWK=
LNCaP-Clone-FGC MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTd7Nj6zOEBvVQ>? NXTmTJZxW0GQR1XS
L-363 M3fuW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrKOJc5UUN3ME23PVgvPDJibl2= M2P3XnNCVkeHUh?=
ES8 NHfaRYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LXeGlEPTB;OEGwMlUzKG6P M{PIdnNCVkeHUh?=
697 M2PKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTh|MT61OUBvVQ>? MX3TRW5ITVJ?
HSC-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm0doVpUUN3ME24N|kvPTRibl2= M4j1VnNCVkeHUh?=
H4 NIrDdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPqTWM2OD16NUCuPFUhdk1? NEf0XmNUSU6JRWK=
QIMR-WIL MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;XTWM2OD16NkWuNkBvVQ>? MX7TRW5ITVJ?
OAW-42 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfVTWM2OD16N{KuNVkhdk1? NHXOXYhUSU6JRWK=
MCF7 NVroTnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXwWmFKSzVyPUi5PE42QSCwTR?= NVXKWVN1W0GQR1XS
SCC-25 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m5UmlEPTB;OUG0MlE6KG6P NUfPWnRHW0GQR1XS
NCI-H1563 NUnsWXVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTlzNT65PUBvVQ>? M3naT3NCVkeHUh?=
OVCAR-5 M2frSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHQO4RIUUN3ME25OFAvOTdibl2= MWrTRW5ITVJ?
HDLM-2 NG\1b25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTxTWM2OD17NEmuNkBvVQ>? MkO3V2FPT0WU
NB5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLJTWM2OD17NU[uOkBvVQ>? NH\wT|BUSU6JRWK=
NCI-H292 NW\pO4pPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDpPFZSUUN3ME25O|QvOzJibl2= MV7TRW5ITVJ?
A101D NXfCNGV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXy5O4NzUUN3ME25PVAvOTlibl2= MmfKV2FPT0WU
NCI-H1648 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW0TWM2OD17OUiuOVEhdk1? NWPU[21DW0GQR1XS
EKVX M4rBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHBOpNoUUN3ME2xMlAyOjlizszN MmnHV2FPT0WU
SW1710 M4TRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnpTWM2OD1zLkC0NlM{KM7:TR?= MVjTRW5ITVJ?
WM-115 NIHtd|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom0TWM2OD1zLkC2OlU3KM7:TR?= NUj6XVg3W0GQR1XS
CAL-54 NYPNV3J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwMEewPFEh|ryP Mo\2V2FPT0WU
TGBC24TKB M13PW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFwMEiwOFUh|ryP MlTHV2FPT0WU
NCI-H520 MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XGUGlEPTB;MT6wPFk3PyEQvF2= NV\C[VYyW0GQR1XS
D-423MG NYW2cFZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;MZ3puUUN3ME2xMlA6QTZ{IN88US=> MYfTRW5ITVJ?
BFTC-905 NYniXFVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fr[WlEPTB;MT6xN|Q1QSEQvF2= M1vIZnNCVkeHUh?=
HT NHvSdpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonYTWM2OD1zLkGzOFc5KM7:TR?= NH[0ephUSU6JRWK=
CTB-1 Ml21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3BSnBKSzVyPUGuNVQzQTNizszN MVXTRW5ITVJ?
Hs-578-T M3X3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwMUm1OlUh|ryP M2fHUXNCVkeHUh?=
HuH-7 NYLzfmZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIryRVRKSzVyPUGuNlA6PDlizszN NFPJcJBUSU6JRWK=
LB996-RCC NVrEWZBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjCXIdWUUN3ME2xMlIzOTd5IN88US=> NIL0dXRUSU6JRWK=
KYSE-270 M3TIWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKxTWM2OD1zLkK5O|M1KM7:TR?= NUm0UHFHW0GQR1XS
A4-Fuk MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHCXXI{UUN3ME2xMlI6QTl|IN88US=> MVPTRW5ITVJ?
A498 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\KXmlEPTB;MT6zNFQ4PCEQvF2= MVfTRW5ITVJ?
SK-MEL-1 M3jnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwM{C2O|kh|ryP M1HOSXNCVkeHUh?=
AU565 NX23PJJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7wTWM2OD1zLkOxPFY{KM7:TR?= MXXTRW5ITVJ?
Saos-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHxTWM2OD1zLkOzNlA2KM7:TR?= M1r1NHNCVkeHUh?=
A549 NFXuT25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrqTWM2OD1zLkO5PVch|ryP MUHTRW5ITVJ?
BFTC-909 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny0TWM2OD1zLkSzN|A2KM7:TR?= Ml\pV2FPT0WU
MDA-MB-415 M1\OTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr0XJhXUUN3ME2xMlQ5Pjl{IN88US=> M4Ty[nNCVkeHUh?=
639-V NUDLbo1IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XQPWlEPTB;MT61NFI1PSEQvF2= NEHqW|FUSU6JRWK=
A704 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfZTWM2OD1zLkWwO|g2KM7:TR?= MonJV2FPT0WU
PANC-03-27 Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHtR4RKSzVyPUGuOVE1ODhizszN M4LCcXNCVkeHUh?=
SK-MEL-28 NGPqNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXDe49WUUN3ME2xMlU3ODh3IN88US=> MlvQV2FPT0WU
Ramos-2G6-4C10 NV\mUFh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTFwNkC3OFYh|ryP NX7tbJc5W0GQR1XS
HuP-T4 NVLpS4pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{e4PWlEPTB;MT62NFc4QCEQvF2= MVTTRW5ITVJ?
VA-ES-BJ NWXNfGplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNkGyO{DPxE1? NFmwTm5USU6JRWK=
EFM-19 M3jzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:5fGlEPTB;MT62NVgyKM7:TR?= MXrTRW5ITVJ?
G-401 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3HTWM2OD1zLk[yNVY1KM7:TR?= NXnUS2hTW0GQR1XS
D-566MG NV\ZNGQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwNkK1N{DPxE1? MmroV2FPT0WU
JVM-3 M3XvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP2XGdmUUN3ME2xMlY1QDd3IN88US=> NYjuN2l[W0GQR1XS
TK10 M4\TT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL2TWM2OD1zLk[3NFg{KM7:TR?= NYPwZlVPW0GQR1XS
BT-20 MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLiTWM2OD1zLk[4PVAzKM7:TR?= M2\jc3NCVkeHUh?=
EGI-1 NYDobWZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrncIY6UUN3ME2xMlg1PzBzIN88US=> NFnuNZRUSU6JRWK=
EW-16 Mo\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\tUWlEPTB;MT64OVE5OiEQvF2= NHHJbIFUSU6JRWK=
NCI-H2228 NHvZdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:3RmlEPTB;MT64OVIxOyEQvF2= Ml7oV2FPT0WU
BB49-HNC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwOEi2PVIh|ryP NIn2N4VUSU6JRWK=
G-402 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm3dHI6UUN3ME2xMlg6Pzl5IN88US=> M{TSRXNCVkeHUh?=
NCI-H526 NGTzRoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K5eWlEPTB;MT65NVM6KM7:TR?= NVjkSnY2W0GQR1XS
ME-180 NHjIWWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jOW2lEPTB;MT65N|Q4PyEQvF2= M2LQe3NCVkeHUh?=
PFSK-1 M4izdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwOUS0OVgh|ryP NVnESHV7W0GQR1XS
TYK-nu NX\BSFZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLMTWM2OD1zLkm1PFI{KM7:TR?= NGGxUmdUSU6JRWK=
HOS M2nEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj0TWM2OD1zLkm3PVQ5KM7:TR?= NFvReJNUSU6JRWK=
T98G NE\SSWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r0bmlEPTB;MT65PVAxPiEQvF2= MlLYV2FPT0WU
SK-MES-1 M2rOfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJwMEGzN|Ih|ryP MWHTRW5ITVJ?
SNB75 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDETHFKSzVyPUKuNFE2PDFizszN MUfTRW5ITVJ?
LAMA-84 M3Xqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPwcFFKSzVyPUKuNFI3QDlizszN NEniSJBUSU6JRWK=
CAL-39 MmfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfmWoFRUUN3ME2yMlA{OjhizszN M{P5eHNCVkeHUh?=
LOXIMVI MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJwMESwPFQh|ryP NUizUok6W0GQR1XS
NH-12 NUHmfIJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jzO2lEPTB;Mj6wOVQzPCEQvF2= NGrBfHFUSU6JRWK=
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OVCAR-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PJT2lEPTB;MkCuOVgzOiEQvF2= NELJfoJUSU6JRWK=
HD-MY-Z NEDxcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWiydXhsUUN3ME2yNU4{Pjl4IN88US=> M3zVXXNCVkeHUh?=
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SCH MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3JTWM2OD1{Mj60PVYh|ryP MYLTRW5ITVJ?
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NCI-H1650 NYXLcYNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\QfGVWUUN3ME2yN{46OjRzIN88US=> NILJXo1USU6JRWK=
ACHN NWjIb3NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LjdWlEPTB;MkSuOFY2PiEQvF2= MkPnV2FPT0WU
M059J M4H6d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zPTmlEPTB;MkSuOVY{PCEQvF2= MWHTRW5ITVJ?
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KG-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqyfpBCUUN3ME2yOU42PDl2IN88US=> MVrTRW5ITVJ?
COLO-824 MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJ3LkW1PVkh|ryP Mn;SV2FPT0WU
NCI-H1155 MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjPOnVKSzVyPUK1MlU5PDdizszN M13kTnNCVkeHUh?=
NCI-H441 NULHeFd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HVd2lEPTB;MkWuO|Q3PSEQvF2= NFiwWVRUSU6JRWK=
J-RT3-T3-5 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTTTWM2OD1{Nj6zNFI4KM7:TR?= NWDXO|B3W0GQR1XS
JEG-3 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\6ZZlKSzVyPUK2MlY5ODVizszN NUL4eGVxW0GQR1XS
RKO MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ4Lke2N|Ih|ryP NYrieGlVW0GQR1XS
CAL-85-1 M3XSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nYUmlEPTB;MkeuNlEyQCEQvF2= M175UnNCVkeHUh?=
CAL-120 NF21bHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJ5Lk[5NVQh|ryP MkfVV2FPT0WU
NCI-H2452 M3j3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTnTWM2OD1{Nz63O|E3KM7:TR?= MkS2V2FPT0WU
NCI-H1395 MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJ5Lke4N|Mh|ryP Mln1V2FPT0WU
KYSE-450 NIrzUHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ5Lkm4OlIh|ryP M3nG[3NCVkeHUh?=
S-117 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJ7LkO4OVch|ryP M121VXNCVkeHUh?=
SW13 NGnvcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHmTWM2OD1{OT64OVE6KM7:TR?= MWXTRW5ITVJ?
ES3 NVz0eZdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTNyLkO3N|Mh|ryP M{\pdHNCVkeHUh?=
HCT-116 NGrPT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K2bmlEPTB;M{CuOVU2PCEQvF2= Mn3nV2FPT0WU
NCI-H1693 NWTve|ZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHsTWM2OD1|MD61PVQzKM7:TR?= MlvGV2FPT0WU
VM-CUB-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HsSmlEPTB;M{CuOlQyOyEQvF2= MWfTRW5ITVJ?
NCI-H2170 NV;DT4pQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTNzLkW3PFQh|ryP NEXtdIZUSU6JRWK=
ALL-PO MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnCSHM3UUN3ME2zNU45PDJ6IN88US=> MXzTRW5ITVJ?
NCI-H661 NWTIR5dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fOVmlEPTB;M{KuNFYzOyEQvF2= MWLTRW5ITVJ?
NCI-H2347 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN{LkS4N|ch|ryP M{T3VHNCVkeHUh?=
FTC-133 NXXVfJZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTN{LkewOkDPxE1? Ml;RV2FPT0WU
COLO-829 Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTN|LkO0Olch|ryP NYnDZ2pzW0GQR1XS
GOTO NHfyR5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TJVWlEPTB;M{OuOVI2QCEQvF2= NV:2ToJwW0GQR1XS
YAPC NWDT[Hh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXOxbWdJUUN3ME2zN{45OTV7IN88US=> MWXTRW5ITVJ?
LCLC-103H NE\sWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HBc2lEPTB;M{SuNVYzPCEQvF2= MoDnV2FPT0WU
SiHa NFriTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTN2LkO4NVch|ryP M1[3OnNCVkeHUh?=
LK-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTN2LkW3NFgh|ryP M3PjUnNCVkeHUh?=
KP-N-YS NVXMT4Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzKTWM2OD1|ND63NlAzKM7:TR?= NYHQT3lMW0GQR1XS
NCI-SNU-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLhTWM2OD1|NT6xO|kh|ryP MYLTRW5ITVJ?
KNS-81-FD NWLM[GlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfhTWM2OD1|NT62OlMh|ryP NITiXGtUSU6JRWK=
SCC-9 NXnFXJJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN4LkexOFYh|ryP MVfTRW5ITVJ?
SH-4 NUX6dWppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofETWM2OD1|Nj63N{DPxE1? M4X5WnNCVkeHUh?=
HCC-1954 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfxTWM2OD1|Nz6yO|I6KM7:TR?= M{HCN3NCVkeHUh?=
BALL-1 NWK4SJdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K5XmlEPTB;M{euOVMyPiEQvF2= NE\nNHZUSU6JRWK=
BE-13 NF;vbGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTN5LkewNVgh|ryP Ml;kV2FPT0WU
COLO-678 M4nSPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnG[3VKSzVyPUO3Mlk1OzdizszN NYWxNm5ZW0GQR1XS
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OAW-28 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\RNWlEPTB;M{iuOlM6KM7:TR?= MXzTRW5ITVJ?
CAMA-1 NEnobIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjSfW5MUUN3ME2zPE46PjlzIN88US=> MVnTRW5ITVJ?
C2BBe1 MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\PemlEPTB;M{muPFE5KM7:TR?= MljIV2FPT0WU
A3-KAW MlqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTRyLkO2OlEh|ryP MVjTRW5ITVJ?
SK-MEL-24 NIrtTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTRyLkW5N|Eh|ryP M4H2[3NCVkeHUh?=
KYSE-140 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTRyLkexOlUh|ryP NWjuTXFnW0GQR1XS
MOLT-16 NEXhUm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fmSGlEPTB;NEGuNVU{PiEQvF2= NUixU3VYW0GQR1XS
CFPAC-1 Mn73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\QVIp1UUN3ME20Nk42OjFzIN88US=> MlrQV2FPT0WU
NB14 NFvYUYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHuTWM2OD12Mj63NFI4KM7:TR?= NWCzXXBCW0GQR1XS
COLO-792 M4XvW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHXTWM2OD12Mj64PVYyKM7:TR?= NGfLepFUSU6JRWK=
RH-1 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zkZmlEPTB;NEOuOFg{PiEQvF2= NI\1UJVUSU6JRWK=
NCI-H522 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTR2LkO1Olgh|ryP MXvTRW5ITVJ?
Ca-Ski MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR2LkixNVQh|ryP NUKwelBTW0GQR1XS
KGN NFvXV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v0eGlEPTB;NEiuN|A3OyEQvF2= NEPNeWhUSU6JRWK=
UACC-62 M13mfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfFTWM2OD12OD60NFczKM7:TR?= NFPSfFFUSU6JRWK=
NCI-H358 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTR7LkOwNVgh|ryP MXzTRW5ITVJ?
LS-411N NV3MRXZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTUWIttUUN3ME20PU4{OTF6IN88US=> MkD6V2FPT0WU
IST-MES1 NIC4[5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDhb3ZnUUN3ME20PU42PjJ3IN88US=> MoHpV2FPT0WU

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-FoxO3a / FoxO3a / PUMA; 

PubMed: 29137323     


HCT116 cells were treated with 4μmol/L NVP-BKM120 or 4μmol/L Pictilisib for 24 hours. Indicated protein levels were analyzed by Western blotting.

p-S6RP / S6RP; 

PubMed: 30042442     


Western blot analysis of proteins as indicated in 4T1 cells treated with 1 µM GDC-0941 or vehicle for 24 h. Vinculin was used as a loading control. 

p-4EBP1 / 4EBP1; 

PubMed: 25857298     


Cells were treated with 0.5 μM GDC-0941 for the indicated time course and then collected for Western blot analysis of p-4EBP1. 

p-LRP6 / LRP6; 

PubMed: 25857298     


MDAMB-231, HCC1937 and MCF7 cells were treated with 0.5 µM GDC-0941 for 1 hr, and cell lysates were used for immunoblot analyses.

p-PAK / PAK1 / p-CRAF / RAF / p-MEK / MEK / p-ERK / ERK; 

PubMed: 24327733     


Cells were treated with 1 μM GDC-0941 for the indicated times, and lysates were probed with the indicated antibodies. Independent experiments were performed at least three times, and a representative result is shown.

29137323 30042442 25857298 24327733
Immunofluorescence
p65; 

PubMed: 30042442     


Representative images of immunofluorescent staining of p65 cellular localization in 4T1 cells treated with 1 µM GDC-0941 or vehicle for 24 h. 4T1 cells were cultured alone or co-cultured with RAW264.7 macrophages. Representative images of three independent experiments are shown. 

beta-catenin; 

PubMed: 25857298     


Cells were seeded on coverslips the day before the experiment and treated with 0.5 µM GDC-0941 for 18 hr. The immunofluorescence (IF) of beta-catenin is indicated as red fluorescence, and double staining with DAPI is blue. Magnification: 400 X for the left three panels. The right panel shows enlarged images from the white squares.

30042442 25857298
Growth inhibition assay
Cell viability; 

PubMed: 27117832     


The viability of the indicated cells treated with increasing concentrations of GDC-0941 (ranging from 70nM to 20 μM) for 72 hours, determined by CellTiter Glo Viability assay. The IC50 concentrations were calculated using GraphPad Prism program. The assay was performed in triplicate, and the error bars represent standard deviations.

27117832
体内研究 在微粒体中，GDC-0941仅有有限的代谢，其口服生物利用度为78%[5]。GDC-0941 每天按 75 mg/kg剂量处理携带人U87MG 恶性胶质移植瘤的雌性NCr无胸腺小鼠，显著抑制生长，肿瘤生长抑制率为 83%。[1]GDC-0941 每天按 150 mg/kg剂量口服处理携带HER2扩增的抗Trastuzumab的MDA-MB-361.1移植瘤 的小鼠，抑制肿瘤生长，且显著延迟肿瘤衰退，与肿瘤中强诱导型凋亡相关。[2] GDC-0941 每天按75 mg/kg剂量处理携带自发性B细胞滤泡性淋巴瘤的PTEN+/-LKB1+/hypo小鼠，持续2周，诱导肿瘤体积下降~40%，伴随着AKT, S6K 和SGK(血清和糖皮质激素蛋白激酶)蛋白激酶的磷酸化被切除。GDC-0941抑制肿瘤细胞增殖，诱导凋亡和抑制中心母细胞数。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验：

[1]
- 合并

闪烁接近检测:

使用p85α调节亚基，使重组人PI3Kα, PI3Kβ, 和PI3Kδ在 Sf9 杆状病毒系统中共表达，在谷胱甘肽-琼脂糖凝胶上进行亲和层析而纯化GST-融合蛋白。重组人 PI3Kγ表达作为单体 GST融合，也想上述相似方法纯化。GDC-0941 溶于DMSO，加到含200 μg硅酸钇(Ysi) 聚赖氨酸SPA 磁珠, 4 mM MgCl2, 1 mM 二硫苏糖醇 (DTT), 1 μM ATP, 0.125 μCi [γ-33P]-ATP, 和4% (v/v) DMSO的20 mM Tris-HCl (pH 7.5)上，总体积为 50 μL。PI3Kα (5 ng), PI3Kβ(5 ng), PI3Kδ(5 ng), 或PI3Kγ(5 ng)的重组GST-融合 ，加到实验混合物中，开始激酶反应。在室温下温育1小时后, 加入150 μL PBS终止反应。混合物在2000 rpm 转速下离心2分钟，然后使用Wallac Microbeta计数器读数。在 MDL Assay Explorer系统中使用S型，剂量-反应曲线，计算进行至少2次独立重复实验，取平均值，作为IC50值。
细胞实验：

[2]
- 合并
  • Cell lines: SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, 和MKN-7
  • Concentrations: 溶于DMSO,终浓度为~10 μM
  • Incubation Time: 48,和72小时
  • Method:

    使用不同浓度 GDC-0941处理细胞48,和 72小时。通过CellTiter-Glo Luminescent细胞活性检测实验测定细胞增殖/活力。通过Western Blot分析pAKT (Ser473), cleaved caspase-3, 和cleaved PARP通过 Caspase-Glo 3/7实验和细胞死亡检测 ELISAplus 实验分别测定caspase 3/7活性, 和凋亡。


    (Only for Reference)
动物实验：

[2]
- 合并
  • Animal Models: 移植MDA-MB-361.1细胞的NCR裸鼠, 皮下移植BT474-M1 细胞的SCID, C.B-17/IcrHsd-Prkdcscid 小鼠
  • Dosages: ~150 mg/kg/day
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 44 mg/mL (85.66 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
 5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 513.64
化学式

C23H27N7O3S2
CAS号 957054-30-7
储存条件 粉状
溶于溶剂
别名 RG7321

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02092831 Completed Drug: GDC-0941 Healthy Volunteer Genentech Inc. April 2014 Phase 1
NCT01740336 Completed Drug: GDC-0941|Drug: Placebo|Drug: Paclitaxel Breast Cancer Genentech Inc. February 6 2013 Phase 2
NCT01474668 Completed Drug: GDC-0941 Healthy Volunteer Genentech Inc. October 2011 Phase 1
NCT01240226 Completed Drug: GDC-0941|Drug: ketoconazole Healthy Volunteer Genentech Inc. November 2010 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

  • 泛PI3K抑制剂

    LY294002 : Pan-PI3Kα/δ/β inhibitor, IC50=0.5 μM/0.57 μM/0.97 μM.

  • 活性最高的PI3K抑制剂

    Duvelisib (IPI-145, INK1197) : PI3K δ, IC50=1 nM.

  • FDA批准的PI3K抑制剂

    CAL-101 (Idelalisib, GS-1101) : Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.

  • 最新的PI3K抑制剂

    GSK2636771 : Potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines.

相关PI3K产品

  • Taselisib (GDC 0032) New

    Taselisib (GDC 0032, RG7604) 是一种有效，下一代的β亚型PI3K抑制剂，作用于PI3Kα/δ/γ， IC50分别为0.29 nM/0.12 nM/0.97nM，比作用于PI3Kβ选择性高10倍以上。

  • Pilaralisib (XL147) New

    Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Phase 1/2。

  • GNE-317 New

    GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。

  • LY294002

    LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。

    Features:LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA, NSC 66389) 是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。3-Methyladenine (3-MA)可成功应用于抑制线粒体自噬。现配现用（加热助溶）。

  • Idelalisib (CAL-101, GS-1101)

    Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。

    Features:Calistoga 暗示 CAL-101治疗血液恶性肿瘤可能有更广泛的应用价值。

  • Wortmannin

    Wortmannin (KY 12420)是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。

  • Dactolisib (BEZ235)

    Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。

  • Buparlisib (BKM120)

    Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34，mTOR，DNAPK 的作用效果下降，而对 PI4Kβ几乎没有活性。Buparlisib 可诱导凋亡。Phase 2。

    Features:BKM120是可用于口服的生物有效的PI3K抑制剂。

  • Alpelisib (BYL719)

    Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID