LY3009120

Catalog No.S7842 Synonyms: DP-4978

For research use only.

LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.

LY3009120 Chemical Structure

CAS No. 1454682-72-4

Selleck's LY3009120 has been cited by 43 publications

Purity & Quality Control

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Biological Activity

Description LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Targets
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
In vitro

LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 3.9 μM.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 M13KSGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVu3NkBpenN? NEfNSIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IILld4F7fXKrbjDhd5NigSxiSVO1NF0xNjByOUNOwG0v NV7LUYRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 MWHGeY5kfGmxbjDhd5NigQ>? MWSxOUBucW6| MXjDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEWyaFGyJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6wNu69VS5? MlLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 Mm\OSpVv[3Srb36gZZN{[Xl? NIOzPIMyPSCvaX7z MV3Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEKUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkCzNe69VS5? MoLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 M{LTbGZ2dmO2aX;uJIF{e2G7 NIO2dnE4OiCqcoO= MVjJcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51KGmwIHj1cYFvKEF|N{WgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCHUlugdIhwe3Cqb4L5cIF1cW:wIH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCHTFnTRUBie3OjeTygTWM2OD1yLkCzO:69VS5? MlWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 MW\GeY5kfGmxbjDhd5NigQ>? NUL5dJY2OTVibXnudy=> MVTDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKFqDSzDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwMEO5{txONg>? NYm4UnRYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 NH\kN3VHfW6ldHnvckBie3OjeR?= NF7qZmIyPSCvaX7z MV;Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEOUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkC0Nu69VS5? NITlbZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 MXXGeY5kfGmxbjDhd5NigQ>? M4nsTlE2KG2rboO= MVfDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEGUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkC0OO69VS5? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MU\GeY5kfGmxbjDhd5NigQ>? M4TXV|E2KG2rboO= MXHDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKHB|ODDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwME[x{txONg>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MnvqSpVv[3Srb36gZZN{[Xl? M{XM[|E2KG2rboO= NYDLN5hzS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDGXW4hcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlA6Oc7:TT6= NYP4W3RNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 NGnhbIFHfW6ldHnvckBie3OjeR?= M4HpbFE2KG2rboO= MUnDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKE2DUEPLNUBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFk5|ryPLh?= Mn;xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 NYnubGw4TnWwY4Tpc44h[XO|YYm= MlXhNVUhdWmwcx?= NEDoXplEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFXwbGI1KGmwIHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhOTVibXnud{BqdiCycnXz[Y5k\SCxZjDBWHAh[W6jbH;neYUtKEmFNUC9NE4y|ryPLh?= MoDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
HCT116 M4fUNmZ2dmO2aX;uJIF{e2G7 NHjS[|ZKdmirYnn0bY9vKG:oIFvSRXMhTzF|RDDteZRidnRiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXJMKHCqb4PwbI9zgWyjdHnvckBjgSCHTFnTRUwhUUN3ME2wMlE2|ryPLh?= NHnVOnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 M37S[GZ2dmO2aX;uJIF{e2G7 NIX0W2JKdiC4aY\vJIlvcGmkaYTpc44hd2ZiQmLBSkBXPjByRTDteZRidnRiaX6gbJVu[W5iQUO3OUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCybzDkc5Nm\CCQSVigcpVl\SC{YYSgZZN{\XO|ZXSgZZMheGyjc33hJINwdmOnboTyZZRqd25icnXxeYlz\WRidH:gbY5pcWKrdDDFVmsheGixc4Doc5J6dGG2aX;uJIJ6KDVyJTygTW5JRTBwMU[1{txONg>? NGm3bpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
HCT116 NHPlZmhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXiz[2FXPjdiaILz NVPmSXI6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOlchcHK|IHL5JJJme2G8dYLpckBie3OjeTygTWM2OD1yLkKy{txONg>? MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 MoOySpVv[3Srb36gZZN{[Xl? MXSxOUBucW6| MX\Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEOVSzDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwMkpOwG0v M4HF[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NVLjNFRUTnWwY4Tpc44h[XO|YYm= NW\oe3ZwOTVibXnudy=> M3X6VWNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iU2LDJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6zNe69VS5? NInNblU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 NGLHO3ZHfW6ldHnvckBie3OjeR?= MYexOUBucW6| M37RTmNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iQVLMJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6zPO69VS5? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MWrGeY5kfGmxbjDhd5NigQ>? MmnkNVUhdWmwcx?= MUXDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEmUQVuxJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6zPe69VS5? M3jVNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 MWnGeY5kfGmxbjDhd5NigQ>? MY[xOUBucW6| MV7Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEeFTkKgbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkS1{txONg>? M4LSR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NFzqd2pHfW6ldHnvckBie3OjeR?= M1;jSVE2KG2rboO= NX\sZmpsS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDKUmshcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlQ4|ryPLh?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MVnGeY5kfGmxbjDhd5NigQ>? MVexOUBucW6| NGT1TJFEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIF3BVFJMPSCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDF3IH3pcpMhcW5icILld4Vv[2Vib3[gRXRRKGGwYXzv[5VmNCCLQ{WwQVAvQM7:TT6= MnO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
A375 Ml\FSpVv[3Srb36gZZN{[Xl? MXGxOUBucW6| NXfoN4pVS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDLTHMyKGmwIHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhOTVibXnud{BqdiCycnXz[Y5k\SCxZjDBWHAh[W6jbH;neYUtKEmFNUC9NE46P87:TT6= NFnucIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
HCT116 MYTGeY5kfGmxbjDhd5NigQ>? NX7aNHJmRDFyMDDuUS=> NIX3eJNR[XKjZH;4bYNidCCjY4TpeoF1cW:wIH;mJHJCWy:UQV[vUWVMKHOrZ37hcIlv\yCyYYToe4F6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBDWkGIIHHzd4V{e2WmIHHzJGVTUyCyaH;zdIhwenmuYYTpc44h[XRiPEGwNEBvVQ>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NVPDeZI5TnWwY4Tpc44h[XO|YYm= MnHoTY5pcWKrdHnvckBw\iCmZYP0bIlw[mmxdHnuMWFVWCCjY4nsdIhwe3CqYYTlJJBzd2KnIHLpcoRqdmdidH:gRk1T[WZiaX6gbJVu[W5iQUO3OUBk\WyuczDifUBOWyCjbnHsfZNqeyxiSVO1NF0xNjB|Md88UU4> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV{OUW0N{c,OzB3Mkm1OFM9N2F-
A375 MXTGeY5kfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGSnc4TobY9jcW:2aX6tRXRRKGGleXzwbI9{eGijdHWgdJJw[mViYnnu[Ilv\yC2bzDDMXJi\iCrbjDoeY1idiCDM{e1JINmdGy|IHL5JG1UKGGwYXz5d4l{NCCLQ{WwQVAvODR{zszNMi=> M{Hqe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
A375 M2O2XmZ2dmO2aX;uJIF{e2G7 MnXhTY5pcWKrdHnvckBw\iCmZYP0bIlw[mmxdHnuMWFVWCCjY4nsdIhwe3CqYYTlJJBzd2KnIHLpcoRqdmdidH:gRU1T[WZiaX6gbJVu[W5iQUO3OUBk\WyuczDifUBOWyCjbnHsfZNqeyxiSVO1NF0xNjB2NN88UU4> M{TsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
MV4-11 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1zMU|czKGi{cx?= MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD6x{txONg>? NIDrPFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
SK-MEL-2 M4fncWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MlO0O|IhcHK| M1LvNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGxvVHn0[ZIhT2yxIHHzd4F6NCCLQ{WwQVAvOs7:TT6= NHHWPFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
A375 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MmDJO|IhcHK| M3zBbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD6z{txONg>? NVLIVVlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk2PDNpPkOwOVI6PTR|PD;hQi=>
SW579 MoLVRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NY\yW5lrPzJiaILz MnXNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{W3PUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD65{txONg>? MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm1OFMoRjNyNUK5OVQ{RC:jPh?=
HT-29 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUDlVFBPPzJiaILz MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygTWM2OD1yLkpOwG0v MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV{OUW0N{c,OzB3Mkm1OFM9N2F-
HepG2 NIL1bZpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{e3NlczKGi{cx?= M3nFfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwuXGm2ZYKgS4xwKGG|c3H5MEBKSzVyPUKuOu69VS5? M3\2dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
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
In vivo In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 165 nM.[1]

Protocol (from reference)

Kinase Assay:[2]
  • Kinase activity measurement using KiNativ assays:

    Compounds are screened in A375 cell lysates using the ATP-based probe at 5 µM. IC50 values are reported in micromolar units. Cell pellets are resuspended in four volumes of lysis buffer [25 mM Tris pH 7.6, 150 mM NaCl, 1% CHAPS, 1% Tergitol NP-40 type, 1% v/v phosphatase inhibitor cocktail II], sonicated using a tip sonicator, and dounce homogenized. Lysates are cleared by centrifugation at 100,000 g for 30 min. The cleared lysates are filtered through a 0.22 μM syringe filter, and gel filtered into reaction buffer [20 mM Hepes pH 7.8, 150 mM NaCl, 0.1% triton X-100, 1% v/v phosphatase inhibitor cocktail II]. MnCl2 is then added to the lysate to a final concentration of 20 mM prior to inhibitor treatment and probe labeling. Final inhibitor concentrations used for IC50 determinations are 10, 1, 0.1, and 0.01 μM. ATP competition experiments are performed at 1,000, 100, 10, and 1 μM ATP. All inhibitor treatments are performed at room temperature.

Cell Research:[1]
  • Cell lines: A375 and HCT116 cells
  • Concentrations: 0.51 μM
  • Incubation Time: 67 h
  • Method: Briefly, cells are grown in DMEM high glucose supplemented with 10% characterized fetal bovine serum and 1% penicillin/streptomycin/L -glutamine at 37℃, 5% CO2, and 95% humidity. Cells are allowed to expand until 70-95% confluency. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate. 625 cells are added per well in 50 μL of complete growth medium. Plates are incubated for 67 h at 37℃, 5% CO2 , and 95% humidity. Then, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37℃, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism software to calculate IC 50 values.
Animal Research:[1]
  • Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumors
  • Dosages: 30 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 3 mg/mL warmed
(7.06 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% CMC Na
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 424.51
Formula

C23H29FN6O

CAS No. 1454682-72-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 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?

Answer:
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.

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