Agerafenib (RXDX-105)

For research use only.

Catalog No.S8015 Synonyms: CEP-32496

6 publications

Agerafenib (RXDX-105) Chemical Structure

CAS No. 1188910-76-0

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.

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

Purity & Quality Control

Choose Selective Raf Inhibitors

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]
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 MULGeY5kfGmxbjDhd5NigQ>? MVGxJIhz NGXlU5ZKdmirYnn0bY9vKG:oIFzDT{BqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D1yLkCwNu69VS5? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 MkjrSpVv[3Srb36gZZN{[Xl? M1HqSVEhcHJ? MmjLTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iSFXLNlk{KGOnbHzzJIFnfGW{IEGgbJIh[nliY3;tdIV1cXSrb36gZolv\GmwZzDhd5NigSxiS3S9NE4xODMQvF2u NWiyfGM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293 MYDGeY5kfGmxbjDhd5NigQ>? NHfib2QyKGi{ Mk\wTY5pcWKrdHnvckBw\iClS3n0JIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO|YYmsJGtlRTBwMECy{txONg>? M1ftXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 MXrGeY5kfGmxbjDhd5NigQ>? Mm\BNUBpeg>? M3jhNmlvcGmkaYTpc44hd2ZiUnX0JIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO|YYmsJGtlRTBwMECy{txONg>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 MV\GeY5kfGmxbjDhd5NigQ>? MkjPNUBpeg>? M3z3SmlvcGmkaYTpc44hd2ZiQXLsNUBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D1yLkCwN:69VS5? M1Tx[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 M4rJcmZ2dmO2aX;uJIF{e2G7 NEDUUJcyKGi{ MYXJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D1yLkCwPO69VS5? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293 M1;sV2Z2dmO2aX;uJIF{e2G7 NVfsRpViOSCqch?= MkDWTY5pcWKrdHnvckBw\iCFU1[xVkBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D1yLkCwPe69VS5? NHvye5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293 M13VTGZ2dmO2aX;uJIF{e2G7 NH73fWUyKGi{ NEjKPGJKdmirYnn0bY9vKG:oIFXQTGEzKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuNFE1|ryPLh?= M4PtdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293 NV3lUY9nTnWwY4Tpc44h[XO|YYm= MnrWNUBpeg>? MULJcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51KGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuNFE1|ryPLh?= NEnxdmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293 MUDGeY5kfGmxbjDhd5NigQ>? Mmj3NUBpeg>? M17xUGlvcGmkaYTpc44hd2ZiRVfGVkBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D1yLkCyNu69VS5? Mn;NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 MVnGeY5kfGmxbjDhd5NigQ>? NWfCdJFlOSCqch?= NHXtdnZKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDCVmFHKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuNFM3|ryPLh?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
COLO205 M3WwbGN6fG:2b4jpZ4l1gSCjc4PhfS=> MoLnO|IhcHK| MnW2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyCneIDy[ZN{cW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{IHLseYUh[XO|YYmsJGVEPTB;MD6wN|bPxE1w MlnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 MkXmSpVv[3Srb36gZZN{[Xl? NILT[2oyKGi{ MWPJcohq[mm2aX;uJI9nKEOUQV[gbY4hcHWvYX6gTGVMOjl|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:OC5yM{pOwG0v NVvISZZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
A375 NVPmTXN5S3m2b4TvfIlkcXS7IHHzd4F6 NIDRT3E4OiCqcoO= MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIV5eHKnc4PpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIh[my3ZTDhd5NigSxiSVO1NF0xNjB5ON88UU4> NEP2RW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
A375 MWnGeY5kfGmxbjDhd5NigQ>? M1;kblIhcHK| MlvwTY5pcWKrdHnvckBw\iCEUlHGJHY3ODCHIH31eIFvfC2vZXTpZZRm\CCPRVugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiMjDodpMtKEmFNUC9NE4xQDMQvF2u MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HCC827 NEDabWhHfW6ldHnvckBie3OjeR?= MXvEbZNxdGGlZX3lcpQhd2ZiW{PIYU1kgWOub4DhcYlv\SCocn;tJHNOVyCYNEC0UUBufXSjboSgbY4h\2WoaYTpcoljKHKnc3nzeIFvfCCqdX3hckBJS0N6MkegZ4VtdHNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiS3m9NE4yQDd6zszNMi=> NGT1W4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe4O|E2Pid-Mki3PFcyPTZ:L3G+
COLO679 MlrYR5l1d3SxeHnjbZR6KGG|c3H5 NEf5R|k4OiCqcoO= MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDU2xQPjd7IHPlcIx{KGW6cILld5NqdmdiQmLBSkBXPjByRTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJiYnz1[UBie3OjeTygSWM2OD1yLkKxNe69VS5? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HT144 M3jISmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYC3NkBpenN? MmjBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQyPDRiY3XscJMh\XiycnXzd4lv\yCEUlHGJHY3ODCHIH31eIFvfCCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmeiCkbIXlJIF{e2G7LDDFR|UxRTBwMkK4{txONg>? NFfNV4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
SK-MEL-28 NVKzVJl6S3m2b4TvfIlkcXS7IHHzd4F6 NFrTenM4OiCqcoO= MknYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKgZox2\SCjc4PhfUwhTUN3ME2wMlQ2PM7:TT6= MkLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 NXPRWG5lTnWwY4Tpc44h[XO|YYm= MmryNUBpeg>? NW[2NWpzUW6qaXLpeIlwdiCxZjDjUWVVKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuOVE{|ryPLh?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HCT116 Ml24R5l1d3SxeHnjbZR6KGG|c3H5 MX[3NkBpenN? MmLvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFLSRWYh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIh[my3ZTDhd5NigSxiRVO1NF0xNjZ4Od88UU4> NIezTJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
Hs578T M3HsWWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2PVPFczKGi{cx?= M4TNXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGh{PTd6VDDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDCVmFHKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzKGKudXWgZZN{[XluIFXDOVA:Oi55M{dOwG0v MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
DU145 Mmj5R5l1d3SxeHnjbZR6KGG|c3H5 NULrT2U3PzJiaILz MnmyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVIvQTFzzszNMi=> NVnGblUzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293 M4PmVmZ2dmO2aX;uJIF{e2G7 MXKxJIhz NXOxeGU5UW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUSuO:69VS5? Mmn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
PC3 MX7DfZRwfG:6aXPpeJkh[XO|YYm= NF30OFY4OiCqcoO= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhSlKDRjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncjDicJVmKGG|c3H5MEBGSzVyPU[uNlU4|ryPLh?= NFnTNpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
LNCAP M3i0XmN6fG:2b4jpZ4l1gSCjc4PhfS=> NVLmbXc5PzJiaILz Mor3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVYvPjNzzszNMi=> NFPSW|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293 NE\UR|hHfW6ldHnvckBie3OjeR?= M1XRZ|EhcHJ? M3[xSWlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG|c3H5MEBM\D15LkJOwG0v MmqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293 M3XyO2Z2dmO2aX;uJIF{e2G7 MWexJIhz MULJcohq[mm2aX;uJI9nKE2HS{KgbY4hcHWvYX6gTGVMOjl|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:QC5|zszNMi=> MlKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
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COLO205 M4LDUGFvfGm2dX3vdkBie3OjeR?= M1fqOlExOCCvZz;r[y=> NF\udm4yPCCmYYnz M2flU2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMhgGWwb3fyZYZ1\WRiaX6gZZRpgW2rYzDueYRmKG2xdYPlJIF1KDFyMDDt[{9s\yxicH:gZollKG[xcjCxOEBl[Xm| MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 31695841     


Cell viability was assessed with alamarBlue assays performed after 72 hours of incubation with RXDX-105, and dose-response curves (left) and calculated IC50 values (right) are shown.

31695841
Western blot
p-RET / RET / p-PLCγ / PLCγ / p-ERK / ERK / p-MEK / MEK ; 

PubMed: 28011461     


Inhibition of phosphorylation of RET and downstream pathways by RXDX-105 in TT cells (RET C634W). 

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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Colo-205 xenograft mouse model
  • Dosages: 100 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 9 mg/mL (17.39 mM)
Water Insoluble
Ethanol Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 517.46
Formula

C24H22F3N5O5

CAS No. 1188910-76-0
Storage powder
in solvent
Synonyms CEP-32496
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID