LY3009120

目录号:S7842 别名: DP-4978

仅限科研使用

LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。

LY3009120 Chemical Structure

CAS: 1454682-72-4

规格 价格 库存 购买数量
RMB 1207.33 现货
RMB 3906.82 现货
RMB 8154.89 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LY3009120发表文献43篇:

产品安全说明书

Raf抑制剂选择性比较

相关Raf产品

生物活性

产品描述 LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。
靶点
C-Raf [1]
(Cell-free assay)
BRAF(V600E) [1]
(Cell-free assay)
BRAF WT [1]
(Cell-free assay)
4.3 nM 5.8 nM 15 nM
体外研究

LY3009120抑制A375和 HCT116细胞的生长,IC50分别为9.2和220 μM。LY3009120抑制酪氨酸激酶KDR,IC50为3.9 μM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 NH7FXmJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXL0b|MxPzJiaILz MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHKnc3H6eZJqdiCjc4PhfUwhUUN3ME2wMlAxQTMQvF2u MlfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 MkjzSpVv[3Srb36gZZN{[Xl? NHLyfVkyPSCvaX7z NUfSemU4S2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDFdIhCOiCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDF3IH3pcpMhcW5icILld4Vv[2Vib3[gRXRRKGGwYXzv[5VmNCCLQ{WwQVAvODMQvF2u M4LTT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NWS5N4ZETnWwY4Tpc44h[XO|YYm= NXL0[mZNOTVibXnudy=> MYnDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEKUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkCzNe69VS5? NETtW5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 NEjMOoxHfW6ldHnvckBie3OjeR?= MmrqO|IhcHK| NGPHXnRKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO|Uh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDFVmsheGixc4Doc5J6dGG2aX;uJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDFUGlUSSCjc4PhfUwhUUN3ME2wMlA{P87:TT6= MmP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 NW\KeGNnTnWwY4Tpc44h[XO|YYm= MoXKNVUhdWmwcx?= NESzUphEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIGrBT{BqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFM6|ryPLh?= NF;TcYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 MVXGeY5kfGmxbjDhd5NigQ>? NYT6SG41OTVibXnudy=> Mn;4R49ueGW2aYTpeoUh[mmwZHnu[{Bi\m[rbnn0fUB1dyCFUlHGJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6wOFLPxE1w M{HwelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 MlnXSpVv[3Srb36gZZN{[Xl? NWPXTpFXOTVibXnudy=> M4ryVmNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iQWLBSkBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFQ1|ryPLh?= NFvmNII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 MlrBSpVv[3Srb36gZZN{[Xl? NULx[493OTVibXnudy=> MV\Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKHB|ODDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwME[x{txONg>? NGLLRZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 MVrGeY5kfGmxbjDhd5NigQ>? MljtNVUhdWmwcx?= MWDDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKE[\TjDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwMEmx{txONg>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NEHIenFHfW6ldHnvckBie3OjeR?= M3i5OFE2KG2rboO= M3r2dWNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iTVHQN2syKGmwIHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhOTVibXnud{BqdiCycnXz[Y5k\SCxZjDBWHAh[W6jbH;neYUtKEmFNUC9NE4xQTkQvF2u NYTwSYdKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 NH7Yfo5HfW6ldHnvckBie3OjeR?= NFy3TIIyPSCvaX7z MXjDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEWyaFK0JIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6x{txONg>? NGDvZXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
HCT116 NFPO[HBHfW6ldHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKEuUQWOgS|E{TCCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRWLLJJBpd3OyaH;yfYxifGmxbjDifUBGVEmVQTygTWM2OD1yLkG1{txONg>? MmOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 MXrGeY5kfGmxbjDhd5NigQ>? M4C5PGlvKH[rdn:gbY5pcWKrdHnvckBw\iCEUlHGJHY3ODCHIH31eIFvfCCrbjDoeY1idiCDM{e1JINmdGy|IIjlco9oemGodHXkJIlvKHCxIHTvd4VlKE6LSDDueYRmKHKjdDDhd5Nme3OnZDDhd{BxdGG|bXGgZ49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IFXST{BxcG:|cHjvdplt[XSrb36gZpkhPTBnLDDJUmg:OC5zNkZOwG0v MkHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
HCT116 NULzWo9CSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mmm4OlchcHK| NV3CVWE4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOlchcHK|IHL5JJJme2G8dYLpckBie3OjeTygTWM2OD1yLkKy{txONg>? MoDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 NFz3c4FHfW6ldHnvckBie3OjeR?= MoTwNVUhdWmwcx?= NIrmfVBEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFPTT{BqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNlnPxE1w NXmyc3VvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 Mo[zSpVv[3Srb36gZZN{[Xl? MXqxOUBucW6| M1zYcGNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iU2LDJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6zNe69VS5? NVz1elczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 MY\GeY5kfGmxbjDhd5NigQ>? MkDvNVUhdWmwcx?= NEX5dVdEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFHCUEBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuN|jPxE1w MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NWjZdoI5TnWwY4Tpc44h[XO|YYm= NV;vW2ZNOTVibXnudy=> MlS1R49ueGW2aYTpeoUh[mmwZHnu[{Bi\m[rbnn0fUB1dyCLUlHLNUBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuN|nPxE1w NX3qNllwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 NV3LV5J3TnWwY4Tpc44h[XO|YYm= M1y1ZVE2KG2rboO= NEK4fVBEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFfDUlIhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlQ2|ryPLh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NELWOmNHfW6ldHnvckBie3OjeR?= NHvCfWMyPSCvaX7z NGXSRnREd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFrOT{BqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuOFfPxE1w M1TFUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NVjNRYtzTnWwY4Tpc44h[XO|YYm= NEjJSJoyPSCvaX7z NUjlOVVES2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDNRXAzUzViaX6gbJVu[W5iQUO3OUBk\WyuczDh[pRmeiBzNTDtbY5{KGmwIIDy[ZNmdmOnIH;mJGFVWCCjbnHsc4d2\SxiSVO1NF0xNjkQvF2u NX\Hco9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 M{LMT2Z2dmO2aX;uJIF{e2G7 MoTWNVUhdWmwcx?= MYTDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEuKU{GgbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkm3{txONg>? NETyRVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
HCT116 NFXBbIdHfW6ldHnvckBie3OjeR?= NV;j[W1yRDFyMDDuUS=> NXPweYpuWGG{YXTvfIlk[WxiYXP0bZZifGmxbjDv[kBTSVNxUlHGM21GUyC|aXfuZYxqdmdicHH0bJdigSCrbjDoeY1idiCKQ2SxNVYh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhSlKDRjDhd5Nme3OnZDDhd{BGWkticHjvd5Bpd3K7bHH0bY9vKGG2IEyxNFAhdk1? NWL1PYVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 M3LKUWZ2dmO2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGSnc4TobY9jcW:2aX6tRXRRKGGleXzwbI9{eGijdHWgdJJw[mViYnnu[Ilv\yC2bzDCMXJi\iCrbjDoeY1idiCDM{e1JINmdGy|IHL5JG1UKGGwYXz5d4l{NCCLQ{WwQVAvODNzzszNMi=> NVjYdGN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk2PDNpPkOwOVI6PTR|PD;hQi=>
A375 MmDUSpVv[3Srb36gZZN{[Xl? MlH3TY5pcWKrdHnvckBw\iCmZYP0bIlw[mmxdHnuMWFVWCCjY4nsdIhwe3CqYYTlJJBzd2KnIHLpcoRqdmdidH:gR{1T[WZiaX6gbJVu[W5iQUO3OUBk\WyuczDifUBOWyCjbnHsfZNqeyxiSVO1NF0xNjB2Mt88UU4> M4qwO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
A375 NETsOI5HfW6ldHnvckBie3OjeR?= NFPYcGZKdmirYnn0bY9vKG:oIHTld5RpcW:kaX;0bY4uSVSSIHHjfYxxcG:|cHjheIUheHKxYnWgZolv\GmwZzD0c{BCNVKjZjDpckBpfW2jbjDBN|c2KGOnbHzzJIJ6KE2VIHHuZYx6e2m|LDDJR|UxRTBwMES0{txONg>? M2TrU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
MV4-11 NFfpXnJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVy3NkBpenN? MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD6x{txONg>? MlLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm1OFMoRjNyNUK5OVQ{RC:jPh?=
SK-MEL-2 Mln2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2TvUVczKGi{cx?= NHHJT2lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuLWTpeIVzKEeubzDhd5NigSxiSVO1NF0xNjMQvF2u MnTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm1OFMoRjNyNUK5OVQ{RC:jPh?=
A375 MmDpRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NILJTVY4OiCqcoO= MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHytWIl1\XJiR3zvJIF{e2G7LDDJR|UxRTBwM988UU4> NFfhTJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
SW579 M1XGbmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MX[3NkBpenN? MoDLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{W3PUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD65{txONg>? NHrlPVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
HT-29 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIPue3I4OiCqcoO= NXjtdIZqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdC2WaYTldkBIdG9iYYPzZZktKEmFNUC9NE46|ryPLh?= NVzB[5pJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk2PDNpPkOwOVI6PTR|PD;hQi=>
HepG2 NH33blZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NG\vbpA4OiCqcoO= MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygTWM2OD1{LkdOwG0v NGHLR|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
Assay
Methods Test Index PMID
Western blot p-EGFR / EGFR / p-BRAF / BRAF / p-CRAF / CRAF / p-MEK / MEK / p-AKT / AKT Beclin-1 / Mcl-1 / LC3 / p62 27999210 28382170
体内研究 在负荷BRAF V600E ST019VR PDX肿瘤的大鼠体内,LY3009120 (15 or 30 mg/kg, p.o.)剂量依赖性抑制肿瘤生长。在负荷A375异种移植物的裸鼠体内,LY3009120 (3到50 mg/kg, p.o.)单剂量口服治疗剂量依赖性抑制磷酸-ERK,4.36 mg/kg剂量下抑制50%磷酸- ERK (EC50),68.9 ng/mL或165 nM血浆浓度下达到50%磷酸- ERK (EC50) 抑制率。[1]

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:[2]
  • 使用KiNativ试验测定激酶活性:

    化合物在A375细胞裂解物中使用基于ATP的探针在5 µM下筛选。IC50值以微摩尔单位表示。细胞沉淀重悬浮在4体积裂解缓冲液[25 mM Tris pH 7.6,150 mM NaCl,1% CHAPS,1% Tergitol NP-40 型,1% v/v 磷酸酶抑制剂混合物II]中,使用尖端超声波仪声处理,并均质化。裂解产物通过100,000 g下离心分离30分钟除去。澄清的裂解液通过0.22 μM注射过滤器和凝胶过滤到反应缓冲液[20 mM Hepes pH 7.8,150 mM NaCl,0.1% triton X-100,1% v/v 磷酸酶抑制剂混合物II]。抑制剂处理和探针标记之前,将终浓度为20 mM 的MnCl2加入裂解液。用于IC50测定的终抑制剂浓度为10,1,0.1,和 0.01 μM。ATP竞争性实验在1,000,100,10,和1 μM ATP下进行。所有抑制剂的处理在室温下进行。

细胞实验:[1]
  • Cell lines: A375 和 HCT116 细胞
  • Concentrations: 0.51 μM
  • Incubation Time: 67 h
  • Method: 简而言之,细胞在DMEM高浓度葡萄糖中生长,用10%胎牛血清和1%青霉素/链霉素/L-谷氨酰胺增补,在37℃,5% CO2,和95%湿度下培育。允许细胞扩增到70-95%的融合度。连续稀释的测试化合物分配加入到384孔黑色透明底板。每孔加入包含625个细胞的50 μL完全生长培养基。板在37℃,5% CO2,和95%湿度下培育67小时。然后,10 μL包含440 μM 刃天青的PBS溶液加入板的每孔中,板在37℃,5% CO2,和95%湿度下再培育5小时。板在Synergy2阅读器上使用540 nm激发波长和600 nm发射波长读取。得到的数据使用Prism软件分析以计算IC 50值。
动物实验:[1]
  • Animal Models: 负荷BRAF V600E ST019VR PDX肿瘤的雌性 NIH裸鼠
  • Dosages: 30 mg/kg
  • Administration: p.o.

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):
0.5% CMC Na

30mg/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 424.51
化学式

C23H29FN6O

CAS号 1454682-72-4
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
NCT02014116 Terminated Drug: LY3009120 capsule Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms Eli Lilly and Company November 26 2013 Phase 1

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

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常见问题及建议解决方法

问题 1:
I am trying to figure out solubility of the drug LY3009120 Catalog #7842 for in vivo studies. I need some details on the formulation and how it is made to dissolve the chemical?

回答:
It can dissolve in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 1 mg/ml clearly, and in 0.5% CMC Na at 30 mg/ml as a suspension.