Foretinib (GSK1363089)

目录号:S1111 别名: EXEL-2880, XL-880, GSK089

仅限科研使用

Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。

Foretinib (GSK1363089) Chemical Structure

CAS: 849217-64-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2340.27 现货
RMB 1374.78 现货
RMB 7124.95 现货
大包装 有超大折扣
大剂量询单有大折扣!

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Foretinib (GSK1363089)发表文献75篇:

产品安全说明书

c-Met抑制剂选择性比较

相关c-Met产品

生物活性

产品描述 Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。
靶点
Met [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
Tie-2 [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
点击更多
0.4 nM 0.86 nM 1.1 nM 2.8 nM 3 nM
体外研究

XL880抑制HGF受体家族酪氨酸激酶,对Met和Ron 的IC50 值分别为0.4 nM和3 nM。XL880也会抑制KDR,Flt-1,和Flt-4,IC50值分别为0.9 nM,6.8 nM和2.8 nM。XL880抑制B16F10,A549 和HT29细胞集落生长,IC50分别为40 nM,29 nM和165 nM。[1]一项最近的研究表明,XL880差异性影响胃癌细胞系MKN-45和KATO-III的细胞生长。XL880抑制MKN-45细胞中MET和下游信号分子的磷酸化,而在KATO-III细胞中靶向作用于GFGR2。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Daoy  NHfNWodHfW6ldHnvckBCe3OjeR?= Ml;uNE42NzFxMj61JO69VQ>? MV6yOEBp MlrNSG1UVw>? Mn3abY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v NF3J[|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
ONS76 Ml\0SpVv[3Srb36gRZN{[Xl? Mk\tNE42NzFxMj61JO69VQ>? NXXkbJpmOjRiaB?= NYPXcXdyTE2VTx?= MkLGbY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v MlT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
Daoy  NHjPT3FHfW6ldHnvckBCe3OjeR?= MV[wMlUwOS9{LkWg{txO MUKyOEBp MXzEUXNQ NFfq[JhqdmirYnn0d{BJT0ZvbXXkbYF1\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> NVzi[3F{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
ONS76 Mn75SpVv[3Srb36gRZN{[Xl? NH7FVJYxNjVxMT:yMlUh|ryP NVvtdW9jOjRiaB?= NHrpZ|BFVVOR MmPvbY5pcWKrdIOgTGdHNW2nZHnheIVlKG2rZ4LheIlwdiCjbnSgbY53[XOrb36= NWPVU3NCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
Daoy  M4XM[mFxd3C2b4Ppd{BCe3OjeR?= NInY[3MyKM7:TR?= MUOyOEBp NVTNc4FVTE2VTx?= M16yV4lv\HWlZYOgZZBweHSxc3nz MkfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
Daoy  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMlUwOS9{LkWg{txO M2PzW|I1NTl4IHi= NF3mXpZFVVOR M3XIZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2HT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{mxNlQyLz5{NUO5NVI1OTxxYU6=
U251 NXHXXHE1TnWwY4Tpc44hSXO|YYm= NXzaXFQzOTByL{OwNE86ODBibl2= NHHvUVgyKGh? M1T5bGROW09? MojObY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCPZYLUT:Kh NXrOeGpIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 NGqzWnRHfW6ldHnvckBCe3OjeR?= NYKwdoZ6OTByL{OwNE86ODBibl2= NYiycVZHOSCq M{G2cWROW09? NH;Eb2lqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF3ldnRMyqB? NYjGd4M5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 MorMSpVv[3Srb36gRZN{[Xl? MUixNFAwOzByL{mwNEBvVQ>? MV2xJIg> M3PFVWROW09? NEHtU5VqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF3ldnRMyqB? M2fVN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 NXvXUW57TnWwY4Tpc44hSXO|YYm= NGLObmgyODBxM{CwM|kxOCCwTR?= NVHzUnhsOSCq MYDEUXNQ NXvzc2hzcW6qaXLpeJMhfGinIHHjeIl3cXS7IH;mJGF5dCxiVInyc|M> Mli4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
A172 NVe5UnNOTnWwY4Tpc44hSXO|YYm= NGfnR|kyODBxM{CwM|kxOCCwTR?= NIDTTHcyKGh? NI[xTZpFVVOR Mo[5bY5pcWKrdIOgeIhmKGGldHn2bZR6KG:oIFH4cEwhXHm{b{O= NH;jSmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 M{nyZmZ2dmO2aX;uJGF{e2G7 NX7wd2ZROTByL{OwNE86ODBibl2= M133V|EhcA>? MWnEUXNQ M4fyUIlvcGmkaYTzJJRp\SCjY4Tpeol1gSCxZjDBfIwtKFS7cn:z M1HGSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 M1Py[mZ2dmO2aX;uJGF{e2G7 MnftNVAxNzNyMD:5NFAhdk1? M2HKe|EhcA>? M336fGROW09? MoPE[IVkemWjc3XzJGFsfCCyaH;zdIhwenmuYYTpc44hcW5iYTDjc45k\W62cnH0bY9vKGSncHXu[IVvfCCvYX7u[ZI> NEnLcFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 NH[3ZYpHfW6ldHnvckBCe3OjeR?= MU[xNFAwOzByL{mwNEBvVQ>? MVSxJIg> M1zE[2ROW09? M2n4TYRm[3KnYYPld{BCc3RicHjvd5Bpd3K7bHH0bY9vKGmwIHGgZ49v[2WwdILheIlwdiCmZYDlcoRmdnRibXHucoVz M4TQfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
SF188 NIPBWllHfW6ldHnvckBCe3OjeR?= MV2xNFAwOzByL{mwNEBvVQ>? M1:wVVEhcA>? M1HpXWROW09? MYHk[YNz\WG|ZYOgRYt1KHCqb4PwbI9zgWyjdHnvckBqdiCjIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51KG2jbn7ldi=> NH;D[mU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 M1OySGZ2dmO2aX;uJGF{e2G7 MY[xNFAwOzByL{mwNEBvVQ>? NUnDcYNSOjhiaB?= MoH3SG1UVw>? MUPpcoR2[2W|IGDBVnAh[2ynYY\h[4U> NIXZdZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 NF;1Z4lHfW6ldHnvckBCe3OjeR?= MUWxNFAwOzByL{mwNEBvVQ>? MoDuNlghcA>? NWO5PZVVTE2VTx?= NUC0d2U3cW6mdXPld{BRSVKSIHPs[YF3[Wen Ml7jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzM[lE5OTByL{OwNE86ODBibl2= MXW0PEBp M1\TbGROW09? Mk\GdoVlfWOnczDj[YxtKHO3co\peoFtKGG2IEmwNEBvVSC|aXfubYZq[2GwdHz5 M{nqS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7NSosyODBxM{CwM|kxOCCwTR?= NX\3eI55PDhiaB?= MkH6SG1UVw>? NHTZfXZz\WS3Y3XzJINmdGxic4Xyeol3[WxiYYSgPVAxKG6PIIPp[45q\mmlYX70cJk> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
A172 NH[1b3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki5NVAxNzNyMD:5NFAhdk1? MUG0PEBp MULEUXNQ MWLy[YR2[2W|IHPlcIwhe3W{dnn2ZYwh[XRiOUCwJI5OKHOrZ37p[olk[W62bIm= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
SF188 M2XYb2Z2dmO2aX;uJGF{e2G7 MkjnNVAxNzNyMD:5NFAhdk1? NWOyd5VROjRiaB?= NIT3NZJFVVOR NH7QTGZi[nKxZ3H0[ZMhdWmpcnH0bY9vKGGwZDDpcpZie2mxbjDv[kBodGmxbXGgZ4VtdHNiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4rKWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 M13BfGZ2dmO2aX;uJGF{e2G7 M33ydlExOC9|MECvPVAxKG6P M4XGTFI1KGh? MULEUXNQ NV:xbVFk[WK{b3fheIV{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gc4Yh\2yrb33hJINmdGy|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NEXDSY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 M{HtNGZ2dmO2aX;uJGF{e2G7 Mmm1NVAxNzNyMD:5NFAhdk1? M3ztd|I1KGh? NHKwOVVFVVOR MUHhZpJw\2G2ZYOgcYloemG2aX;uJIFv\CCrbo\hd4lwdiCxZjDncIlwdWFiY3XscJMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NWDKfFNNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
Ba/F3 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2LOPFAvODByMT2xNEDPxE1? NFXycHI4OiCq NFTnc|hqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3W0clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG4OVg6Lz5{NEKxPFU5QTxxYU6=
HCC78 NWnuVJBMS2WubDDWbYFjcWyrdImgRZN{[Xl? MXiwMlAyNTFyIN88US=> MYe3NkBp MmP4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NEKw[ZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxPFU5QSd-MkSyNVg2QDl:L3G+
SK-HEP1 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXSwMlI2NTFwNTFOwG0> MlvENlTDqGh? Mnv4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MlSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzOEexO|EoRjJ{MUi3NVcyRC:jPh?=
SK-HEP2 MlezSpVv[3Srb36gRZN{[Xl? NV7Zcm9HOSEQvF2= M3LEO|I1KGh? MlWzZoxw[2u|IFjHSk1qdmS3Y3XkJINmdGxibX;0bYxqfHl? NIrSdm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
SK-HEP2 M3j1NmZ2dmO2aX;uJGF{e2G7 NILlWFYyKM7:TR?= M3TXfVI1KGh? MXfjZZV{\XNiR{KvUUBxcGG|ZTDhdpJme3Rid3n0bEBz\WS3Y4Tpc44hcW5idHjlJGcxN0dzwrDhcoQhWyCyaHHz[ZM> NHvjPIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
MKN-45  M2rzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSwMlAyNTFyIN88US=> MniwOUBl M{DseWlEPTB;ODDuUS=> NGHNUYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
KATO-III NYP6OIE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4mzW|AvODFvMUCg{txO M{PhVFUh\A>? NHfTVVJKSzVyPUOwJI5O MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
MKN-45  NIDmT2tHfW6ldHnvckBCe3OjeR?= MmLGNUDPxE1? NEPKNYwzPCCq MlHTbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJG1GXCxiQXv0MEBidmRiRWLLNU8zKGmwIF3LUk01PQ>? M3j6RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkW1PVE5Lz5{MU[1OVkyQDxxYU6=
KATO-III MkPCSpVv[3Srb36gRZN{[Xl? MVOxJO69VQ>? MknJNlQhcA>? NYOyeoh4cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKE2HVDygRYt1NCCjbnSgSXJMOS9{IHnuJG1MVi12NR?= MnjJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF4NUW5NVgoRjJzNkW1PVE5RC:jPh?=
H1648 MnzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrNe2xKSzVyPUGuNlghyrFyLkGyJO69VQ>? MnnhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
H1573 M1P4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwNkKgxtEhOC5yNTFOwG0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ3MkK4OEc,OjF{NUKyPFQ9N2F-
H596 NG[5[GhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTFwMkGgxtEhOC5zNzFOwG0> NVjrTmhJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOVIzQDRpPkKxNlUzOjh2PD;hQi=>
HOP92 NIHFV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3kUo9KSzVyPUCuPFEhyrFiMD6yPUDPxE1? M{DyUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkWyNlg1Lz5{MUK1NlI5PDxxYU6=
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SK-N-MC NHjySG9yUFSVIHHzd4F6 NYfPVXVFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NXjYZmhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M4Kx[pFJXFNiYYPzZZk> M1fpPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NFL0dnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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NB1643 NUOzcmJneUiWUzDhd5NigQ>? NH3FUFZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M3\Zb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 MkHmdWhVWyCjc4PhfS=> NIHCXIhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= M3X0WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 NFXxNppyUFSVIHHzd4F6 NHzXfFByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MX7xTHRUKGG|c3H5 MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? MkjXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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MG 63 (6-TG R) M2HlepFJXFNiYYPzZZk> M2K0ZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells MlHydWhVWyCjc4PhfS=> M3LZOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| M2Hj[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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NB1643 MmHudWhVWyCjc4PhfS=> MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM> NVTid2pmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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BT-12 MnHDdWhVWyCjc4PhfS=> MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0yOiClZXzsdy=> NVTObIJzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SJ-GBM2 M2nBPJFJXFNiYYPzZZk> NInCdWRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| MlHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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MDA-MB-231 M2m2RmN6fG:2b4jpZ4l1gSCjc4PhfS=> NXvwNFJOPzJiaILz MUfDfZRwfG:6aXPpeJkhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC53MjFOwG0v NYjifmo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwO|k6PjdpPkOxNFc6QTZ5PD;hQi=>
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NCI-H1993 MljRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4r1UlMh\GG7cx?= M2\1d2dzd3e2aDDpcohq[mm2aX;uJI9nKHerbHSgeJlx\SCqdX3hckBPS0lvSEG5PVMh[2WubIOgbY5kfWKjdHXkJIZweiB|IHThfZMh[nliY3XscEB1cXSncj3ncI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGdKPTBiPTCwMlA3OTZ4IN88UU4> NWDwbotJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
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NCI-1993 Mn\FSpVv[3Srb36gZZN{[Xl? NYrCd4xyOSC3TR?= M1XjOVQhcHK| M2jkTmlvcGmkaYTpc44hd2ZiYz3NSXQhcW5iaIXtZY4hVkOLLUG5PVMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NYfRc2ZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
NCI-H1993 NGPnWZZHfW6ldHnvckBie3OjeR?= MmDWNUB2VQ>? Ml32OEBpenN? NITmfG1KdmirYnn0bY9vKG:oIHOtUYV1KERzMkK4WkBufXSjboSgdIhwe3Cqb4L5cIF1cW:wIHnuJGNTUVOSUj;DZZM6KG2xZHnmbYVlKGi3bXHuJG5EUS2KMUm5N{Bk\WyuczDheEAyKHWPIHHmeIVzKDRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NWK3[WplRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
sf21 NF;YdYtHfW6ldHnvckBie3OjeR?= MlXMRolv\GmwZzDh[oZqdmm2eTD0c{B4cWymIIT5dIUhVi22ZYLtbY5idCCQSD30ZYdo\WRiYX7kJIF3cS22YXfn[YQh\GWyaH;zdIhwenmuYYTl[EBkNU2HVDCoPVU3KHSxIEGzPVAhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIIPmNlEh[2WubIOgZpkhW1CUIHHuZYx6e2m| MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|MUKwOEc,OzF3M{GyNFQ9N2F-
sf21 NV;xdGdlTnWwY4Tpc44h[XO|YYm= MX;CbY5lcW6pIHHm[olvcXS7IITvJG4ufGW{bXnuZYwhVkhvdHHn[4VlKGGwZDDheokufGGpZ3XkJIRmeGixc4Doc5J6dGG2ZXSgZ{1OTVRiREGyNlhXKG23dHHueEApQTV4IITvJFE{QTBicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJJNnOjFiY3XscJMh[nliU2DSJIFv[Wy7c3nz MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|MUKwOEc,OzF3M{GyNFQ9N2F-
A549 MoXoRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MYS3NkBpenN? MlfMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNk41KM7:TT6= MnfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NE[xPVcoRjNzNUS2NVk4RC:jPh?=
MCF7 NWjiRVc6SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnTtO|IhcHK| MlvlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNk41KM7:TT6= M1X2NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUS2NVk4Lz5|MUW0OlE6PzxxYU6=
HepG2 NFzhd3dCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXS3NkBpenN? M2DlZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAzNjRizszNMi=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV2NkG5O{c,OzF3NE[xPVc9N2F-
MKN45 NH3OOXREgXSxdH;4bYNqfHliYYPzZZk> M4Dk[VczKGi{cx?= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> MnzJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4Mkm2N|EoRjNzNkK5OlMyRC:jPh?=
H460 MorvR5l1d3SxeHnjbZR6KGG|c3H5 NE\ie4g4OiCqcoO= MoXqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS5zNDFOwG0v M1LKUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
A549 MW\DfZRwfG:6aXPpeJkh[XO|YYm= MmOyO|IhcHK| MmDhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS52OTFOwG0v M1z5bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
HT-29 M3;hXmN6fG:2b4jpZ4l1gSCjc4PhfS=> M4LpTlczKGi{cx?= M133TGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLke2JO69VS5? NYPqUHA6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2Nlk3OzFpPkOxOlI6PjNzPD;hQi=>
U87MG Ml3qR5l1d3SxeHnjbZR6KGG|c3H5 M1jkT|czKGi{cx?= NV;NS|dES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTh5TVegZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKuNVch|ryPLh?= NUm2NoszRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2Nlk3OzFpPkOxOlI6PjNzPD;hQi=>
Assay
Methods Test Index PMID
Western blot pROS1 / tROS1 / pSHP2 / pERK / ERK p-MDM2 / p53 / PUMA p-Met / Met / p-Akt / Akt 24218589 29854314
Growth inhibition assay Cell viability 29854314
体内研究 XL880(100 mg/kg,单一剂量,口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如,HGFor VEGF)诱导的肝脏中Met和肺中Flk-1/KDR受体磷酸化,两者都能持续24小时。XL880 (30-100 mg/kg,每天一次,口服强喂)处理导致肿瘤负荷减少。30和100 mg/kg XL880处理后,肺表面肿瘤负荷分别减少50%和58%。XL880处理负荷B16F10实体瘤的小鼠也会导致剂量依赖性肿瘤生长抑制,30和100 mg/kg分别导致64%和87%的抑制。对于这两项研究,XL880给药具有良好的耐受性,并且没有显著的体重损失。[1] XL880通过Met可以进一步以HGF的反常信号为作用靶点,同时靶向作用于几个参与肿瘤血管生成的受体酪氨酸激酶。XL880给药2到4小时后,引起人异种移植物中肿瘤出血坏死,96小时(给药5天后)观察到最大肿瘤坏死,导致完全的肿瘤消退。[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]

  • 激酶抑制试验:

    激酶抑制使用三种测定形式中的一种进行研究:[33P]磷酰基转移法,荧光素酶耦合的化学发光法,或AlphaScreen酪氨酸激酶技术。IC50s使用XLFit通过非线性回归分析计算。33P-磷酰基转移激酶实验反应在384孔白色,透明底,高结合力微量滴定板(Greiner,Monroe,NC)中进行。板用50 μL体积的涂层缓冲液中的2 μg/well蛋白质或多肽底物涂覆,涂层缓冲液包含40 μg/mL底物(poly(Glu, Tyr) 4:1,22.5 mM Na2CO3,27.5 mM NaHCO3,50 mM NaCl 和3 mM NaN 3。涂层的板用50 μL实验缓冲液洗涤一次,然后在室温下(RT)过夜培养。测试化合物和酶与33P-γ-ATP (3.3 μCi/nmol)结合,总体积为20 μL。反应混合物在室温下培养2小时,然后通过抽吸终止。随后微量滴定板用0.05% Tween-PBS缓冲液(PBST)清洗6次。加入闪烁液(50 μL/well),整合的33P使用MicroBeta闪烁计数器通过液体闪烁光谱法测量。荧光素酶耦合的化学发光反应在384孔白色,含培养基的微量滴定板(Greiner)中进行。第一步,酶和化合物结合,并培养60分钟;加入终体积为20 μL的ATP与多肽底物(poly(Glu, Tyr) 4:1)起始反应,在室温下培养2-4小时。接下来进行激酶反应,加入20 μL等分激酶Glo (Promega,Madison,WI),荧光信号使用Victor酶标仪测量。总ATP消耗限制在50%。AlphaScreenTM酪氨酸激酶测定使用链霉亲和素涂覆的供体珠和PY100抗磷酸酪氨酸抗体涂覆的受体珠进行。生物素化的聚(Glu,Tyr) 4:1用作底物。通过加入供体/受体珠,随后形成供体/受体珠复合物产生荧光测量底物磷酸化。激酶与测试化合物结合,并预培养60分钟,随后加入总体积为20 μL 的ATP,和生物素化的聚(Glu, Tyr)在384孔白色,含培养基的微量滴定板(Greiner)中。反应混合物在室温下培养1小时。然后加入包含75 mM Hepes,pH 7.4,300 mM NaCl,120 mM EDTA,0.3% BSA和0.03% Tween-20的10 μL 15-30 μg/mL AlphaScreen 珠悬浮液淬灭反应。室温下培养2-16小时后,板使用AlphaQuest阅读器读取数据。

细胞实验:

[1]

  • Cell lines: B16F10,A549,和 HT29 细胞
  • Concentrations: 40 nM
  • Incubation Time: 12 到 14 天
  • Method: B16F10,A549,和HT29细胞(1.2×103/孔)与软琼脂混合,并接种于包含超过琼脂层的10% FBS 和EXEL-2880的96孔板。对于含氧量正常的条件,板在21%氧气,5% CO2,和74% 氮气中培养(37 ℃)12到14天,而低氧条件下的培养(37℃)在1% 氧气,5% CO2,和94%氮气的低氧培养室中进行。每个条件下的集落数量在加入50% Alamar Blue,进行荧光检测后评估。
动物实验:

[1]

  • Animal Models: B16F10 肿瘤细胞(2×10 5)通过胃部静脉注射植入5到8周大的无胸腺裸鼠(NCr 或 BALB/c)
  • Dosages: 100 mg/kg
  • Administration: 口服强饲

溶解度(25°C)

体外

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):
30% propylene glycol, 5% Tween 80, 65% D5W

30 mg/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 632.65
化学式

C34H34F2N4O6

CAS号 849217-64-7
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
NCT00920192 Completed Drug: Foretinib Carcinoma Hepatocellular GlaxoSmithKline August 12 2009 Phase 1
NCT00742261 Completed Drug: GSK1363089 Solid Tumours GlaxoSmithKline August 11 2008 Phase 1
NCT00725764 Completed Drug: GSK1363089 (foretinib) Neoplasms Head and Neck GlaxoSmithKline August 27 2007 Phase 2
NCT00725712 Completed Drug: GSK1363089 (formerly XL880) Neoplasms Gastrointestinal Tract GlaxoSmithKline March 31 2007 Phase 2
NCT00743067 Completed Drug: GSK1363089 (formerly XL880) Solid Tumours GlaxoSmithKline August 9 2006 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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