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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。

CAS: 1454682-72-4

规格	价格	库存
5mg	RMB 1207.33	现货
25mg	RMB 3906.82	现货
100mg	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

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+

Click to View More Cell Line Experimental Data

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]

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.

参考文献	[1] Henry JR, et al. J Med Chem. 2015, 58(10), 4165-4179. [2] Patricelli MP, et al. Chem Biol.?011, 18(6), 699-710.

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 点击购买： 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
储存条件	2年	-80°C	溶于溶剂

Download LY3009120 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
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.

C1=C0/X	C1:	LOG(C1):
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C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):