Agerafenib (RXDX-105)

Catalog No.S8015 Synonyms: CEP-32496

For research use only.

Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.

Agerafenib (RXDX-105) Chemical Structure

CAS No. 1188910-76-0

Selleck's Agerafenib (RXDX-105) has been cited by 6 Publications

Purity & Quality Control

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Biological Activity

Description Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Features High binding affinity for both BRAF (V600E) mutation and related c-Raf, but no significant affinity for other kinases of MAPK pathway.
Targets
c-Kit [1] LCK [1] PDGFRβ [1] RET [1] Abl1 [1] Click to View More Targets
2 nM(Kd) 2 nM(Kd) 2 nM(Kd) 2 nM(Kd) 3 nM(Kd)
In vitro

CEP-32496 inhibits A375 cell (BRAFV600E) proliferation with EC50 of 78 nM. CEP-32496 exhibits more sensitive cytotoxicity for tumor cell lines (A375, SK-MEL-28, Colo-205, Colo-679, and HT-144) expressing mutant BRAF than those expressing wild-type BRAF (HCT116, Hs578T, LNCaP, DU145, and PC-3). [1] CEP-32496 inhibits mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) in human melanoma (A375) and colorectal cancer (Colo-205) cell lines with IC50 of 78 nM and 60 nM, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 M{fMd2Z2dmO2aX;uJIF{e2G7 Mkf5NUBpeg>? NUnwOW8xUW6qaXLpeIlwdiCxZjDMR2shcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wNFLPxE1w NHTOTJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293 MUTGeY5kfGmxbjDhd5NigQ>? MmDJNUBpeg>? MmPKTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iSFXLNlk{KGOnbHzzJIFnfGW{IEGgbJIh[nliY3;tdIV1cXSrb36gZolv\GmwZzDhd5NigSxiS3S9NE4xODMQvF2u Ml7RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 M3rMbGZ2dmO2aX;uJIF{e2G7 Mlj4NUBpeg>? MWnJcohq[mm2aX;uJI9nKGONaYSgbY4hcHWvYX6gTGVMOjl|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:OC5yMENOwG0v MkW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 NVrt[llbTnWwY4Tpc44h[XO|YYm= Mm\hNUBpeg>? MUnJcohq[mm2aX;uJI9nKFKndDDpckBpfW2jbjDISWszQTNiY3XscJMh[W[2ZYKgNUBpeiCkeTDjc41x\XSrdHnvckBjcW6maX7nJIF{e2G7LDDL[F0xNjByMt88UU4> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 Mny1SpVv[3Srb36gZZN{[Xl? MlHZNUBpeg>? MmHtTY5pcWKrdHnvckBw\iCDYnyxJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO|YYmsJGtlRTBwMECz{txONg>? M1XyWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 MmLOSpVv[3Srb36gZZN{[Xl? Mme3NUBpeg>? NVzDbGNNUW6qaXLpeIlwdiCxZjDWSWdHWjJiaX6gbJVu[W5iSFXLNlk{KGOnbHzzJIFnfGW{IEGgbJIh[nliY3;tdIV1cXSrb36gZolv\GmwZzDhd5NigSxiS3S9NE4xODkQvF2u NI\TRlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293 NGrJe3FHfW6ldHnvckBie3OjeR?= NX;QdJNUOSCqch?= M{XxfWlvcGmkaYTpc44hd2ZiQ2PGNXIhcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wNFnPxE1w MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 NFrnNJVHfW6ldHnvckBie3OjeR?= MWixJIhz NXHGOph1UW6qaXLpeIlwdiCxZjDFVGhCOiCrbjDoeY1idiCKRVuyPVMh[2WubIOgZYZ1\XJiMTDodkBjgSClb33w[ZRqfGmxbjDibY5lcW6pIHHzd4F6NCCNZE2wMlAyPM7:TT6= M3nzV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 MoX1SpVv[3Srb36gZZN{[Xl? MUexJIhz NWHyXoxOUW6qaXLpeIlwdiCxZjDCVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDISWszQTNiY3XscJMh[W[2ZYKgNUBpeiCkeTDjc41x\XSrdHnvckBjcW6maX7nJIF{e2G7LDDL[F0xNjBzNN88UU4> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 M4\MUGZ2dmO2aX;uJIF{e2G7 MVqxJIhz Mn23TY5pcWKrdHnvckBw\iCHR1\SJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO|YYmsJGtlRTBwMEKy{txONg>? M{POUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 MXvGeY5kfGmxbjDhd5NigQ>? M4LnOFEhcHJ? M3ew[mlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFLSRWYhcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wN|bPxE1w NEjNdpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
COLO205 MmftR5l1d3SxeHnjbZR6KGG|c3H5 Mnn6O|IhcHK| NHrhd3FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEV0yRMkC1JINmdGy|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKgZox2\SCjc4PhfUwhTUN3ME2wMlA{Ps7:TT6= NX2yZnVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293 NWrJZWtETnWwY4Tpc44h[XO|YYm= NWfwblduOSCqch?= NUHTTIdyUW6qaXLpeIlwdiCxZjDDVmFHKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuNFM6|ryPLh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
A375 M1\lVGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mnj3O|IhcHK| MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIV5eHKnc4PpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIh[my3ZTDhd5NigSxiSVO1NF0xNjB5ON88UU4> NUPuVlU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
A375 NEXTb3VHfW6ldHnvckBie3OjeR?= M4X4UFIhcHK| NHy2[mdKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62LX3l[IlifGWmIF3FT{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCyJIhzeyxiSVO1NF0xNjB6Mt88UU4> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HCC827 NGjVOlhHfW6ldHnvckBie3OjeR?= M3P5[GRqe3CuYXPlcYVvfCCxZjDbN2heNWO7Y3zvdIFucW6nIH\yc40hW02RIG[0NFROKG23dHHueEBqdiCpZX\peIlvcWJicnXzbZN1[W62IHj1cYFvKEiFQ{iyO{Bk\WyuczDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDLbV0xNjF6N{lOwG0v MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd6N{G1Okc,Ojh5OEexOVY9N2F-
COLO679 NWXlNWF[S3m2b4TvfIlkcXS7IHHzd4F6 NITiSnY4OiCqcoO= Ml:wR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR29NVzZ5OTDj[YxteyCneIDy[ZN{cW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{IHLseYUh[XO|YYmsJGVEPTB;MD6yNVHPxE1w M4POdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HT144 MnGyR5l1d3SxeHnjbZR6KGG|c3H5 M2\kR|czKGi{cx?= NFe4RpdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDF2NDDj[YxteyCneIDy[ZN{cW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{IHLseYUh[XO|YYmsJGVEPTB;MD6yNljPxE1w MkW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
SK-MEL-28 MXHDfZRwfG:6aXPpeJkh[XO|YYm= MVu3NkBpenN? M3:0fmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD2yPEBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyJIJtfWViYYPzZZktKEWFNUC9NE41PTUQvF2u NWjoUIxqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293 MYnGeY5kfGmxbjDhd5NigQ>? NXr6PY14OSCqch?= NGLBe45KdmirYnn0bY9vKG:oIHPNSXQhcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD61NVPPxE1w MlXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HCT116 MUXDfZRwfG:6aXPpeJkh[XO|YYm= NVfCO3N5PzJiaILz NVToSnVwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGJTSUZiYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJiYnz1[UBie3OjeTygSWM2OD1yLk[2Pe69VS5? Mlu2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
Hs578T NGT1RpNEgXSxdH;4bYNqfHliYYPzZZk> Ml3BO|IhcHK| MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDId|U4QFRiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVIvPzN4zszNMi=> NF\lS5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
DU145 M1y4VGN6fG:2b4jpZ4l1gSCjc4PhfS=> NVjXWGdxPzJiaILz M3\Kd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFLSRWYh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIh[my3ZTDhd5NigSxiRVO1NF0zNjlzMd88UU4> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 M2DKOGZ2dmO2aX;uJIF{e2G7 M3v1NlEhcHJ? MV7Jcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gTGVMOjl|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:PC55zszNMi=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
PC3 NVuxfFJNS3m2b4TvfIlkcXS7IHHzd4F6 NXTq[oZ2PzJiaILz NH3LZVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVYvOjV5zszNMi=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
LNCAP NGrNbXlEgXSxdH;4bYNqfHliYYPzZZk> NHHIXnU4OiCqcoO= NYjXbYhiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgRnJCTiCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmeiCkbIXlJIF{e2G7LDDFR|UxRTZwNkOx{txONg>? NW\JOW1XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293 M3fUVmZ2dmO2aX;uJIF{e2G7 NFPlb|EyKGi{ MVTJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gTGVMOjl|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:Py5zzszNMi=> M4PCdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 MYfGeY5kfGmxbjDhd5NigQ>? MXyxJIhz NHrOcmVKdmirYnn0bY9vKG:oIF3FT|IhcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;OD6z{txONg>? M2DvclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
COLO205 MV7BcpRqfHWvb4KgZZN{[Xl? MYOxNEBu\y:tZx?= NYS1cYpkOTRiZHH5dy=> MXrBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJJhmdm:pcnHmeIVlKGmwIHH0bJlucWNiboXk[UBud3W|ZTDheEAyOCCvZz;r[{wheG9iYnnkJIZweiBzNDDkZZl{ MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
COLO205 MWTBcpRqfHWvb4KgZZN{[Xl? NGjaTGM{OCCvZz;r[y=> MnS1NVQh\GG7cx?= NWXU[YdZSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52\GVibX;1d4Uh[XRiM{CgcYcwc2duIIDvJIJq\CCob4KgNVQh\GG7cx?= NH7L[2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
COLO205 NXzjNZRsSW62aYT1cY9zKGG|c3H5 NYDWOphwOTByIH3nM4to M4jzRlE1KGSjeYO= NXn3TJRxSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52\GVibX;1d4Uh[XRiMUCwJI1oN2upLDDwc{BjcWRiZn;yJFE1KGSjeYO= NGfHRZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 31695841
Western blot p-RET / RET / p-PLCγ / PLCγ / p-ERK / ERK / p-MEK / MEK 28011461
In vivo CEP-32496 exhibits good stability in mouse, dog, monkey, and human liver microsomal preparations with measured intrinsic clearance values of <23 (μL/min)/mg and t1/2 > 60 min in all assays. CEP-32496 (30 mg/kg, orally, BID) exhibits tumor stasis and a 40% incidence of partial tumor regressions (PRs) in Colo-205 xenograft mouse model, whereas the 100 mg/kg dose group exhibits both tumor stasis and an 80% incidence of PRs. CEP-32496 (30 mg/kg, orally, BID) leads to a 50% and 75% inhibition of normalized pMEK in tumor lysates at the 2 hours and 6 hours postdose time point, respectively, while a 55 mg/kg dose results in a 75% to 57% inhibition of pMEK at 2 hours through 10 hours post administration in Colo-205 xenograft mouse model. [1] CEP-32496 is orally bioavailable in multiple preclinical species (>95% in rats, dogs, and monkeys). CEP-32496 (100 mg/kg) results in inhibition of pMEK and pERK and sustained tumor stasis and regressions in BRAF(V600E) colon carcinoma xenografts in nude mice. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Binding assay:

    Kinases are produced displayed on T7 phage or by expression in HEK-293 cells and tagged with DNA. Binding reactions are performed at room temperature for 1 hour, and the fraction of kinase not bound to test compound is determined by capture with an immobilized affinity ligand and quantitation by quantitative PCR. Each kinase is tested individually against CEP-32496. Kd values are determined using eleven serial 3-fold dilutions and presented as mean values from experiments performed in duplicate. Variability between individual values is less than 2-fold.

Cell Research:[1]
  • Cell lines: A375 cell lines
  • Concentrations: 78 nM
  • Incubation Time: 72 hours
  • Method: Cells are seeded at 104 cells per well in DMEM with 10% fetal calf serum and allowed to attach. The cells are washed with PBS and switched to DMEM with 0.5% of serum and incubated overnight. CEP-32496 is then added at various concentrations with a final DMSO concentration of 0.5% and incubated for 72 h. At the end of incubation, a Cell Titer Blue is added per instructions, and incubation is continued for 3 hours. Remaining viable cells are quantified by measuring the strength of the fluorescence signal using SoftMax Pro (excitation at 560 nm and emission at 590 nm). IC50 values are derived using a 9-point curve fitted with Igor Pro and are presented as mean values from experiments performed in duplicate. Variability between individual values is less than 2-fold.
Animal Research:[1]
  • Animal Models: Colo-205 xenograft mouse model
  • Dosages: 100 mg/kg
  • Administration: oral gavage

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.

15 mg/mL

Chemical Information

Molecular Weight 517.46
Formula

C24H22F3N5O5

CAS No. 1188910-76-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C1=CC(=NO1)NC(=O)NC2=CC(=CC=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(F)(F)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

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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