Ipatasertib (GDC-0068)

目录号:S2808 别名: RG7440

仅限科研使用

Ipatasertib (GDC-0068, RG7440)是一种高选择性的pan-Akt抑制剂,靶向作用于Akt1/2/3,在无细胞试验中IC50为5 nM/18 nM/8 nM,比作用于PKA选择性高620倍。Phase 2。

Ipatasertib (GDC-0068) Chemical Structure

CAS: 1001264-89-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3094.44 现货
RMB 2192.93 现货
RMB 6626.67 现货
RMB 13677.3 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ipatasertib (GDC-0068)发表文献96篇:

产品安全说明书

Akt抑制剂选择性比较

相关Akt产品

生物活性

产品描述 Ipatasertib (GDC-0068, RG7440)是一种高选择性的pan-Akt抑制剂,靶向作用于Akt1/2/3,在无细胞试验中IC50为5 nM/18 nM/8 nM,比作用于PKA选择性高620倍。Phase 2。
靶点
Akt1 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
体外研究

对一大组230种激酶测试,GDC-0068只抑制3种激酶,浓度为 1 μM 时抑制70%以上,(抑制PRKG1α,PRKG1β,和p70S6K时, IC50分别为98 nM, 69 nM, 和 860 nM)。GDC-0068 作用于Akt比作用于PKA 选择性高100倍以上,抑制Akt时 IC50为3.1 μM。GDC-0068处理LNCaP, PC3 和 BT474M1 细胞,抑制Akt底物PRAS40磷酸化,IC50分别为157 nM, 197 nM, 和208 nM。而且, GDC-0068选择性抑制细胞周期进展和Akt信号驱动的癌细胞活力, 包括肿瘤抑制基因PTEN缺陷,PIK3CA致癌基因突变, 和HER2扩增,在HER2+和Luminal 亚型中作用效果最强。[1-4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  NFi2eldHfW6ldHnvckBCe3OjeR?= NGT5dHkyKM7:TR?= NV3PV2pJOjRiaB?= MWjpcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{KGGwZDDpcoR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gLIFkfGm4YYTpc44qKG:oIHLveIghTUeIUjDhcoQhUEWUMx?= M4m5dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[3N|c3Lz5{NE[2O|M4PjxxYU6=
MDA-MB-468  MVXGeY5kfGmxbjDBd5NigQ>? MlfsNUDPxE1? M4KyXlI1KGh? MlTpbY5kemWjc3XzJJRp\SCjYoXu[IFv[2Vib3[gTGVTOw>? NFjWVmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
HCC70  NYnQN25DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[wZlEh|ryP NFrsdGQ2KGR? M1PPPYVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MmG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkezO|YoRjJ2Nk[3N|c3RC:jPh?=
MDA-MB-468  M3LrfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr6ZWcyKM7:TR?= MXG1JIQ> MVLlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW|cH;ud4U> NF7LS2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
PC-3 MYPGeY5kfGmxbjDBd5NigQ>? MY[wMlAxOzhvMj61JO69VQ>? NU\xeY5vOSCq NILicZdFVVOR Mn22bY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiYn;0bEBVcHJ|MElCpEhVOzB6KTDhcoQhW2W{NEez MnqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
BT474M1 M3nvZWZ2dmO2aX;uJGF{e2G7 M2\iUFAvODB|OD2yMlUh|ryP MnTzNUBp MWnEUXNQ MkjHbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiYn;0bEBVcHJ|MElCpEhVOzB6KTDhcoQhW2W{NEez NVf2T|RvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
IGROV-1 NFnPT4tHfW6ldHnvckBCe3OjeR?= NWn3fHJ{OC5yMEO4MVIvPSEQvF2= NEXaPY0yKGh? M{W1TGROW09? NUPmWYV3cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ M3H1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mki3OVY{Lz5{M{K4O|U3OzxxYU6=
PC-3 NE\ZSIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxM|UwOTBizszN M2DvRlI1NzR6L{eyJIg> NVjOVnRxTE2VTx?= MVLkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
MCF7-neo/HER2 NIe5bWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HJSlEwPS9zMDFOwG0> NXvwN4YyOjRxNEivO|IhcA>? MV;EUXNQ NUH2PVBR\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= MmL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
BT474M1 NETDWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonXNU82NzFyIN88US=> MnO2NlQwPDhxN{KgbC=> NFLUOZZFVVOR MkXK[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG|ZYOgeIhmKEdy4pETS|HDqHCqYYPlJJBweHWuYYTpc47DqA>? MlPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
PC-3 NHnPUGVCeG:ydH;zbZMhSXO|YYm= M1Lqd|EwPS9zMDFOwG0> NUCzelloOTVxNEivO|IhcA>? M2H3fWROW09? Mkm1Z4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= M{LpdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mki3OVY{Lz5{M{K4O|U3OzxxYU6=
MCF7-neo/HER2 MWDBdI9xfG:|aYOgRZN{[Xl? NELKNXIyNzVxMUCg{txO NVHoVlR3OTVxNEivO|IhcA>? Mlq1SG1UVw>? NI\ae2tk[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> NHjC[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
BT474M1 MoLiRZBweHSxc3nzJGF{e2G7 NGrJTIQyNzVxMUCg{txO MoTaNVUwPDhxN{KgbC=> MVvEUXNQ MmDIZ4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
LNCAP MmO0R5l1d3SxeHnjbZR6KGG|c3H5 MkXtO|IhcHK| M{TodmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBz\XOjeoXybY4hfG9icnXzc5J2\mmwIHHmeIVzKDd{IHjyd{whUUN3MDC9JFAvODl3IN88UU4> M{\ET|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
LNCAP NH7ISJBHfW6ldHnvckBie3OjeR?= MnzkNU42KGi{cx?= NFT3ZVJKdmirYnn0bY9vKG:oIFHreFEhcW5iaIXtZY4hVE6FQWCgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1cW:wIH;mJHBTSVN2MDDheEBVcHJ{NE[gZYZ1\XJiMT61JIhzeyxiSVO1NEA:KDBwMUW3JO69VS5? NWfCRZhVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3 MknISpVv[3Srb36gZZN{[Xl? M17wXFUxKG2pL3vn NVnh[o04QSCqcoO= MkfBVIxie22jIHPvcoNmdnS{YYTpc44hcW5iboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCSQ{OgZ4VtdHNiYYSgOVAhdWdxa3esJJBwKGG2IEmgbJJ{KGK7IFzDM21UN02VIHHuZYx6e2m|LDDDdEA:KDBwNTFOwG0v NYTBUpZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
BT474M1 MUXDfZRwfG:6aXPpeJkh[XO|YYm= NFq4Sow6PiCqcoO= NGrrNHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDR5NF2xJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDD[YxtXGm2cnWtS4xwKGG|c3H5MEBKSzVyIE2gNUDPxE1w MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
PC3 M3\yNWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYe5OkBpenN? NYHVZ4lIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1emVvR3zvJIF{e2G7LDDJR|UxKD1iMTFOwG0v M3HGZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
MCF7 NWG5OWJGS3m2b4TvfIlkcXS7IHHzd4F6 MkjOPVYhcHK| Mln4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDI[ZIzKGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1emVvR3zvJIF{e2G7LDDJR|UxKD1iMTFOwG0v MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
PC3 NHnobHNHfW6ldHnvckBie3OjeR?= M{TUcVUxKG2pL3vn NWPuOXFvOSCqch?= NYLz[XRYWGyjc33hJINwdmOnboTyZZRqd25iaX6gcpUwdnVibX;1d4UhgGWwb3fyZYZ1\WRid3n0bEBpfW2jbjDQR|Mh[2WubIOgZZQhPTBibXevb4ctKHCxIHH0JFEhcHJiYomgUGMwVVNxTWOgZY5idHm|aYOsJGNxKD1iNz60JO69VS5? NFH5cWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
PC3 MUfGeY5kfGmxbjDhd5NigQ>? NWT0fGV3OTByIH3nM4to Mon5PEBpenN? NHfGNoVKdmirYnn0bY9vKG:oIFHreEBqdiCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB1fW2xcjDwMXM3WlBibHX2[Ywh[XRiMUCwJI1oN2upLDDwc{BifCB6IHjyd{BjgSCHTFnTRUBz\WyjdHn2[UB1dyC2b4ThcEBUPlKS NIf0dYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
MCF7 MUTGeY5kfGmxbjDhd5NigQ>? M1TKSWlvcGmkaYTpc44hd2ZiQXv0NU1u\WSrYYTl[EBRWkGVNECgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3DSlch[2WubIOgc5ZmemW6cILld5NqdmdiSHXyNi=> NGnVfnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
BT474M1 MlzxSpVv[3Srb36gZZN{[Xl? NHL5U2FKdmirYnn0bY9vKG:oIFHreFEudWWmaXH0[YQhWFKDU{SwJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDCWFQ4PE1zIHPlcIx{ NHTrc|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
PC3 MXTGeY5kfGmxbjDhd5NigQ>? M3G5ZmlvcGmkaYTpc44hd2ZiQXv0NU1u\WSrYYTl[EBRWkGVNECgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGDDN{Bk\Wyucx?= MlrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
LNCAP MUnGeY5kfGmxbjDhd5NigQ>? Mn7VTY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTF7DRXAh[2WubIO= NGj5O2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
A673 MnTZdWhVWyCjc4PhfS=> NXK3XohGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY NXHIR3M3eUiWUzDhd5NigQ>? MV7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? M4C3R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MUHxTHRUKGG|c3H5 NFvjb3pyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz NUHaOI9NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MlnmdWhVWyCjc4PhfS=> MnHldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| NF;YOFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MmnhdWhVWyCjc4PhfS=> NGW5d49yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MoLidWhVWyCjc4PhfS=> M{jZW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NFHxR|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 M{LVU5FJXFNiYYPzZZk> MlO2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M{PN[5FJXFNiYYPzZZk> MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? Mny5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 M1LSe5FJXFNiYYPzZZk> MnnKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MUTxTHRUKGG|c3H5 M3XaTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 M2TNSpFJXFNiYYPzZZk> MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> Mli0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH M2HTR5FJXFNiYYPzZZk> M3zZZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? NX;hdmZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NYnsdItNeUiWUzDhd5NigQ>? MVTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? M1fWb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M3jvW5FJXFNiYYPzZZk> MofhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> NHPoe4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 MnPBdWhVWyCjc4PhfS=> MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFMxKGOnbHzz MkfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MoDIdWhVWyCjc4PhfS=> NWHDS4N1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? NWfq[ZR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NXfDflBCeUiWUzDhd5NigQ>? M320OJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz M{T6ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NXvG[XZzeUiWUzDhd5NigQ>? MkTNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 NWXQ[IVTeUiWUzDhd5NigQ>? MnnOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= NF;r[mE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MX3xTHRUKGG|c3H5 MoPkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M1XrbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 NUHGN|lFeUiWUzDhd5NigQ>? NFfGXHlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NUjOUmtWeUiWUzDhd5NigQ>? M37jXpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? Mmq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 NG\IZ4lyUFSVIHHzd4F6 NYTZeoNueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? NWLsepVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 M2nZWJFJXFNiYYPzZZk> NYnZbJVteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NHu3OXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Assay
Methods Test Index PMID
Western blot p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1 cleaved-caspase3 Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1 p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 PUMA 26469692 30185800
体内研究 GDC-0068口服处理给药PC3前列腺移植瘤模型,诱导p-PRAS40下调。GDC-0068 处理BT474-Tr移植瘤,降低 pS6 和 peIF4G 水平,重新定位FOXO3a到细胞核,且诱导 HER3 和pERK的反馈上调。GDC-0068 处理多种移植瘤模型,具有有效抗癌活性,包括PTEN-缺陷的前列腺癌模型LNCaP 和 PC3, PIK3CA H1047R 突变的乳腺癌模型 KPL-4, 和 MCF7-neo/HER2肿瘤模型。[1-4]

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)

动物实验:[1]
  • Animal Models: 携带LNCaP, PC3, KPL-4, 或MCF7移植瘤的雌性裸鼠
  • Dosages: ~100 mg/kg/day
  • Administration: 口服处理

溶解度(25°C)

体外

* 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 458
化学式

C24H32ClN5O2

CAS号 1001264-89-6
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01090960 Completed Drug: GDC-0068 Solid Cancers Genentech Inc. March 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技术支持

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操作手册

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