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 3026.17 现货
RMB 7926.11 现货
有超大折扣
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客户使用Selleck生产的Pictilisib (GDC-0941)发表文献375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 M1rsbWtqdmG|ZTDBd5NigQ>? Mn7ENUBp M{fJWGROW09? MlP6TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCmZXz0ZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZUB4cXSqIFnDOVAhd2ZiMD6wNFMh|ryP MnvXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
Sf9 MmTsT4lv[XOnIFHzd4F6 NUXYb4U6OSCq NITlbZdFVVOR NWnySIlLUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEhzMES3MXIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiY3;lfJBz\XO|aX7nJJA5PWGucHjhJJdqfGhiSVO1NEBw\iByLkCwN{DPxE1? NVr3XIdwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
Sf9 NU\4SGNMU2mwYYPlJGF{e2G7 MVSxJIg> M{m0e2ROW09? NWXEZmRmUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDi[ZRiKEV3NEWtT{BufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegdFg2[WyyaHGge4l1cCCLQ{WwJI9nKDBwMECzJO69VQ>? M4jXZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{W0OlU1Lz5zOEe1OFY2PDxxYU6=
Sf9 MXPLbY5ie2ViQYPzZZk> MWixJIg> NFz2O2FFVVOR NFnHSmRKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFM{KM7:TR?= MkX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
Sf9 M{S5WmtqdmG|ZTDBd5NigQ>? NIS4W5cyKGh? NHToSmVFVVOR NXfUe3BxUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDQTVNMKHBzMUDhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJINw\XiycnXzd4lv\yCyOEXhcJBp[Q>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
MDA-MB-361 M1;ES2Z2dmO2aX;uJGF{e2G7 M1OzVlIhcA>? NILncmZFVVOR MV3Jcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE2GQT3NRk0{PjFiY3XscJMhf2m2aDDQTWs{S0FiRUW0OU1MKG23dHH0bY9vKHerdHigTWM2OCCxZjCwMlAzQCEQvF2= Mn3zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
PC3 M4n1NGZ2dmO2aX;uJGF{e2G7 MmS1NkBp NUT4epRFTE2VTx?= NGnjUIpKdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHnuJHBVTU5vboXscEBpfW2jbjDQR|Mh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? NWj2XYZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
U87MG MXnGeY5kfGmxbjDBd5NigQ>? NYHp[YQyOiCq MYrEUXNQ Mn[zTY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDQWGVPNW63bHygbJVu[W5iVUi3UWch[2WubIOge4l1cCCLQ{WwJI9nKDBwMES2JO69VQ>? NV7oSW9jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
MDA-MB-361 NVqyUHpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS5OkBp Mn\wSG1UVw>? MknMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOzZzIHPlcIx{KHerdHigVGlMO0ODIFW1OFUuUyCvdYTheIlwdiC5aYToJGlEPTBib3[gNE44OiEQvF2= NHnFb5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe1OFY2PCd-MUi3OVQ3PTR:L3G+
A2780 NWDqcYMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojLPVYhcA>? NVHxe3pqTE2VTx?= NWnqb2l1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIGDJT|NESSCjbnSgVHRGViCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4yPCEQvF2= NWjzO401RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
PC3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjENHM6PiCq M3z3UWROW09? NFnwT2pKSzVyPUCuNlgh|ryP Mlf2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
U87MG M{\ON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[5OkBp M4KxVWROW09? NVPxXJN5UUN3ME2wMlk2KM7:TR?= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
Sf9 M2rnc2tqdmG|ZTDBd5NigQ>? NWjNOZlZOzBibXnu MVXEUXNQ MlfUTY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHHtc5VvfCCxZjDBWHAh[2:wc4Xt[YQhf2m2aDDJR|UxKG:oIECuNFQzKM7:TR?= M3HzUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUS4N|QzLz5{MkW0PFM1OjxxYU6=
RAW 264.7 NWXTd215U2mwYYPlJGF{e2G7 NG\sfGk6OCCvaX6= NI\I[nJFVVOR MXjJcohq[mm2aX;uJI9nKGi3bXHuJHBKO0upYX3tZUBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlI6QCEQvF2= M3L0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUS4N|QzLz5{MkW0PFM1OjxxYU6=
Sf9 Mn7nT4lv[XOnIFHzd4F6 NIT0e3EyKGh? NVT2SpZQUW6qaXLpeIlwdiCxZjDHV3Qu\nW|ZXSgbJVu[W5icnXjc41jcW6jboSgVGk{U2KndHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPGPUBk\WyuczD3bZRpKEmFNUCgc4YhOC5yMUeg{txO MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0OUc,OjN3NEC2OFU9N2F-
Sf9 MXfLbY5ie2ViQYPzZZk> NITL[W0yKGh? MYHJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPL[IVtfGFiZYjwdoV{e2Wm NEj4bos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1PSd-MkO1OFA3PDV:L3G+
Sf9 NETxUnBMcW6jc3WgRZN{[Xl? M13uNVEhcA>? M4PyTmlvcGmkaYTpc44hd2ZiR2PUMYZ2e2WmIHj1cYFvKHKnY3;tZolv[W62IGDJN2to[W2vYTDlfJBz\XO|ZXS= M4DqV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ2Lz5{M{W0NFY1PTxxYU6=
Sf9 MnPTT4lv[XOnIFHzd4F6 NWnqcYZGOSCq MVHJcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2Wm NEjJfGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1PSd-MkO1OFA3PDV:L3G+
SKOV3 NFnNbVRMcW6jc3WgRZN{[Xl? M1G1[|Eh|ryP M37ESFEhcA>? NX\YPIhFTE2VTx?= MmO4TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdg>? NEjn[VM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O2NFM1QCd-MkOzOlA{PDh:L3G+
MCF7 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PsW|Eh|ryP M4S4Z|k3KGh? MVXEUXNQ NF;3ZWJIUTVyPUCuNFcxOiEQvF2= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN4MEO0PEc,OjN|NkCzOFg9N2F-
SKOV3 NUO5U5VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixJO69VQ>? NGnmS2w6PiCq NYXFbIlMTE2VTx?= MVvHTVUxRTBwMUS3OkDPxE1? M2PrcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{[wN|Q5Lz5{M{O2NFM1QDxxYU6=
PC3 M2Dpe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml76O|IhcA>? NHvH[WpFVVOR NF;yR4pKSzVyPUCuNlgh|ryP M2nIOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUixO|E1Lz5{MUm4NVcyPDxxYU6=
MCF7.1 M125c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi3NkBp Mn3kSG1UVw>? Mo\MRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BJTVJ{IHflcoUhf2m2aDDJR|UxKG:oIECuNlgh|ryP NGrMSW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm4NVcyPCd-MkG5PFE4OTR:L3G+
MCF7-neo/Her2 M{TE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTzeVJKPzJiaB?= M4nOW2ROW09? MVLJR|UxRTBwMkmg{txO MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4MkmwN{c,OjN4NkK5NFM9N2F-
MCF7-neo/Her2 MkHlT4lv[XOnIFHzd4F6 M3fwTmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNid3n0bEBKSzVyIH;mJFAvODB5IN88US=> NHrZWXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2NlkxOyd-MkO2OlI6ODN:L3G+
PC3 MnLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTBOnBqPzJiaB?= MXPEUXNQ NE\od4NGSzVyPUCuN|Qh|ryP NIHYZW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm4OVY{QSd-MkG5PFU3Ozl:L3G+
MCF7.1 MlW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M331W|czKGh? MX;EUXNQ NGrJcnlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDFR|UxKG:oIECuN|kh|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl6NU[zPUc,OjF7OEW2N|k9N2F-
PC3 NVfxcJBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rleFczKGh? MXvEUXNQ Mor6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiZHXmbYNq\W62IHnuJHBVTU5id3n0bEBKSzVyIH;mJFAvOzlizszN NHizXJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC1NFY3QSd-MkCwOVA3Pjl:L3G+
MCF7.1 M{HaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u5eVczKGh? Ml;CSG1UVw>? NEHHd|VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlcvOSClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCvdYThcpQhf2m2aDDJR|UxKG:oIECuN|Qh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB3ME[2PUc,OjByNUC2Olk9N2F-
MCF7.1 NUDQS2hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL0O|IhcA>? NFG1[otGSzVyPUCuO|Ih|ryP NEjzeJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OlY2Pid-MkCzOFY3PTZ:L3G+
NCI-H1975 Ml[1R5l1d3SxeHnjJGF{e2G7 NEPzU3Y4OiCq NGmydFZKSzVyPUCuNlch|ryP MmL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNUm1OFUoRjJ|MEW5OVQ2RC:jPh?=
H460 M1vzfWN6fG:2b4jpZ{BCe3OjeR?= NH3HU4o4OiCq NEX0TXBKSzVyPUCuPFch|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3OUW0OUc,OjNyNUm1OFU9N2F-
HT-29 NHnqN4VEgXSxdH;4bYMhSXO|YYm= NGrhWYE4OiCq NInBd5lKSzVyPUCuOlYh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3OUW0OUc,OjNyNUm1OFU9N2F-
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