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
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客户使用Selleck生产的Pictilisib (GDC-0941)发表文献363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
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Sf9 M4LQU2tqdmG|ZTDBd5NigQ>? NISwcHUyKGh? MmHMSG1UVw>? MYLJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCLM1ugdFEyOGKndHGgTFExPDdvUjDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> Ml3aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
Sf9 MmPOT4lv[XOnIFHzd4F6 MlnrNUBp MXTEUXNQ MnHaTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCkZYThJGU2PDVvSzDteZRidnRiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bkd2W6cILld5NqdmdicEi1ZYxxcGFid3n0bEBKSzVyIH;mJFAvODB|IN88US=> NWrDN2JSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
Sf9 M12x[GtqdmG|ZTDBd5NigQ>? NFfZWIgyKGh? MnHpSG1UVw>? NI\GdXhKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGDJN2sheDFzMHLleIEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcocheDh3YXzwbIEhf2m2aDDJR|UxKG:oIECuNFM{KM7:TR?= MmLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
Sf9 M3jKfmtqdmG|ZTDBd5NigQ>? M{HlbFEhcA>? MkK0SG1UVw>? Mkm5TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCSSUPLJJAyOTCjbIDoZUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHPv[ZhxemW|c3nu[{BxQDWjbIDoZS=> NGrEeWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe1OFY2PCd-MUi3OVQ3PTR:L3G+
MDA-MB-361 NGfacFhHfW6ldHnvckBCe3OjeR?= NETmU4EzKGh? NXzXXIwxTE2VTx?= Moi5TY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPRFGtUWIuOzZzIHPlcIx{KHerdHigVGlMO0ODIFW1OFUuUyCvdYTheIlwdiC5aYToJGlEPTBib3[gNE4xOjhizszN NXr3[XkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
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U87MG MVvGeY5kfGmxbjDBd5NigQ>? M17WcVIhcA>? NVTa[WRRTE2VTx?= M{nVSmlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iaX6gVHRGVi2wdXzsJIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiSVO1NEBw\iByLkC0OkDPxE1? M3zMbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{W0OlU1Lz5zOEe1OFY2PDxxYU6=
MDA-MB-361 NFr4N5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD5PVYhcA>? MVPEUXNQ M3HBfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTN4MTDj[YxteyC5aYToJHBKUzOFQTDFOVQ2NUtibYX0ZZRqd25id3n0bEBKSzVyIH;mJFAvPzJizszN NVe0d5ZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3OVQ3PTRpPkG4O|U1PjV2PD;hQi=>
A2780 M2jzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHns[m46PiCq MVzEUXNQ MoL5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczD3bZRpKFCLS{PDRUBidmRiUGTFUkBufXSjdHnvckB4cXSqIFnDOVAhd2ZiMD6xOEDPxE1? Mly1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5NUS2OVQoRjF6N{W0OlU1RC:jPh?=
PC3 M{P1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK4VGpUQTZiaB?= MVzEUXNQ M32wc2lEPTB;MD6yPEDPxE1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
U87MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV76c5VJQTZiaB?= NW\EVohqTE2VTx?= NITG[HdKSzVyPUCuPVUh|ryP MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd3NE[1OEc,OTh5NUS2OVQ9N2F-
Sf9 NYDJNmw3U2mwYYPlJGF{e2G7 M2K3NlMxKG2rbh?= MmS0SG1UVw>? NWThTnBIUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPL[4FudWFiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJIFud3WwdDDv[kBCXFBiY3;ud5Vu\WRid3n0bEBKSzVyIH;mJFAvODR{IN88US=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2OEO0Nkc,OjJ3NEizOFI9N2F-
RAW 264.7 M1zqOWtqdmG|ZTDBd5NigQ>? MlLOPVAhdWmw MkezSG1UVw>? Ml\1TY5pcWKrdHnvckBw\iCqdX3hckBRUTONZ3HtcYEh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4zQThizszN MoPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEizOFIoRjJ{NUS4N|QzRC:jPh?=
Sf9 NFrqb3NMcW6jc3WgRZN{[Xl? M{PTelEhcA>? MY\Jcohq[mm2aX;uJI9nKEeVVD3meZNm\CCqdX3hckBz\WOxbXLpcoFvfCCSSUPLZoV1[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW0Z7IHPlcIx{KHerdHigTWM2OCCxZjCwMlAyPyEQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0OUc,OjN3NEC2OFU9N2F-
Sf9 NYnMcplrU2mwYYPlJGF{e2G7 NYLJcZNWOSCq MlvETY5pcWKrdHnvckBw\iCJU2St[pV{\WRiaIXtZY4hemWlb33ibY5idnRiUFmzT4RmdHSjIHX4dJJme3OnZB?= MkK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFUoRjJ|NUSwOlQ2RC:jPh?=
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MCF7-neo/Her2 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPQbmVpPzJiaB?= MmLESG1UVw>? NFnTenhKSzVyPUCuNlkh|ryP NWW4SYEyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OlI6ODNpPkKzOlYzQTB|PD;hQi=>
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MCF7.1 NIHHbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWC3NkBp M17wPWROW09? MnuxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3MlEh[2WubIOg[ZhxemW|c3nu[{BRUTONYXzwbIEhdXW2YX70JJdqfGhiRVO1NEBw\iByLkO5JO69VQ>? NX\EVGh6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5PFU3OzlpPkKxPVg2PjN7PD;hQi=>
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MCF7.1 NV;acIpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TEfFczKGh? MYDFR|UxRTBwN{Kg{txO NWrxZXBWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFY3PTZpPkKwN|Q3PjV4PD;hQi=>
NCI-H1975 NEjLfphEgXSxdH;4bYMhSXO|YYm= M3LobFczKGh? Mn3JTWM2OD1yLkK3JO69VQ>? M1vlSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEW5OVQ2Lz5{M{C1PVU1PTxxYU6=
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