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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
10mM (1mL in DMSO)	RMB 3094.44	现货
5mg	RMB 2192.93	现货
25mg	RMB 6626.67	现货
100mg	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

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-
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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+
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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+

Click to View More Cell Line Experimental Data

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]

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

参考文献	[1] Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01. [2] James F. Blake. 2011. [3] Tabernero J, et al. Ann Oncol, 2011, 22(suppl 3), abstract IL33. [4] Heidi M. Savage, et al. Cancer Res, 2012, 72(8 Supplement), 966. [5] Roel Funke, et al. American Society of Clinical Oncology (ASCO) Annual Meeting, 1-5, 2012. + 展开

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
储存条件	2年	-80°C	溶于溶剂

Download Ipatasertib (GDC-0068) SDF

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 μL 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

%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，注：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：取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：取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
=	×	×

稀释计算器分子量计算器

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)

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