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Agerafenib (RXDX-105)

Name: Agerafenib (RXDX-105)
Brand: Selleck Chemicals
SKU: S8015
Rating: 5 (6 reviews)

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 K_d 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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Raf Signaling Pathway Map

Biological Activity

Description

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)	Click to View More Targets

In vitro

CEP-32496 inhibits A375 cell (BRAF^V600E) 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	MUHGeY5kfGmxbjDhd5NigQ>?		NXfXWJJHOSCqch?=	NFTmWYZKdmirYnn0bY9vKG:oIFzDT{BqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG\|c3H5MEBM\D1yLkCwNu69VS5?	NUe3WXRMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293	MUfGeY5kfGmxbjDhd5NigQ>?		MV:xJIhz	NG\NTGRKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDpckBpfW2jbjDISWszQTNiY3XscJMh[W[2ZYKgNUBpeiCkeTDjc41x\XSrdHnvckBjcW6maX7nJIF{e2G7LDDL[F0xNjByMt88UU4>	MofNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293	MmjtSpVv[3Srb36gZZN{[Xl?		MlPQNUBpeg>?	NGDtXnVKdmirYnn0bY9vKG:oIHPLbZQhcW5iaIXtZY4hUEWNMkmzJINmdGy\|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wNFLPxE1w	NVq1PHV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293	Mn\DSpVv[3Srb36gZZN{[Xl?		MYWxJIhz	NFfyZW5KdmirYnn0bY9vKG:oIGLleEBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG\|c3H5MEBM\D1yLkCwNu69VS5?	NYPDO2dyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293	NF\uOIlHfW6ldHnvckBie3OjeR?=		NF;hSIUyKGi{	NGDHOFhKdmirYnn0bY9vKG:oIFHicFEhcW5iaIXtZY4hUEWNMkmzJINmdGy\|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wNFPPxE1w	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293	M3XadGZ2dmO2aX;uJIF{e2G7		NH7QOm8yKGi{	M3HucWlvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKEiHS{K5N{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGOxbYDleIl1cW:wIHLpcoRqdmdiYYPzZZktKEumPUCuNFA5\|ryPLh?=	NEXmZpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
HEK293	MlHBSpVv[3Srb36gZZN{[Xl?		M1jPN\|EhcHJ?	M13pU2lvcGmkaYTpc44hd2ZiQ2PGNXIhcW5iaIXtZY4hUEWNMkmzJINmdGy\|IHHmeIVzKDFiaIKgZpkh[2:vcHX0bZRqd25iYnnu[Ilv\yCjc4PhfUwhU2R;MD6wNFnPxE1w	M3nZc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293	NYPTO5dQTnWwY4Tpc44h[XO\|YYm=		MnTaNUBpeg>?	MXjJcohq[mm2aX;uJI9nKEWSSFGyJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO\|YYmsJGtlRTBwMEG0{txONg>?	M4fDe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293	NIjzemtHfW6ldHnvckBie3OjeR?=		NWWxUG9yOSCqch?=	NWrHSHpFUW6qaXLpeIlwdiCxZjDCVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDISWszQTNiY3XscJMh[W[2ZYKgNUBpeiCkeTDjc41x\XSrdHnvckBjcW6maX7nJIF{e2G7LDDL[F0xNjBzNN88UU4>	NX;IZVBFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
HEK293	NWLkSHJ7TnWwY4Tpc44h[XO\|YYm=		MYWxJIhz	M3nFSWlvcGmkaYTpc44hd2ZiRVfGVkBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG\|c3H5MEBM\D1yLkCyNu69VS5?	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HEK293	Mmj3SpVv[3Srb36gZZN{[Xl?		MnnyNUBpeg>?	Mmm2TY5pcWKrdHnvckBw\iC5aXzkJJR6eGViQmLBSkBqdiCqdX3hckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOSCqcjDifUBkd22yZYTpeIlwdiCkaX7kbY5oKGG\|c3H5MEBM\D1yLkCzOu69VS5?	MoX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
COLO205	NULIOWs{S3m2b4TvfIlkcXS7IHHzd4F6		M1rPNFczKGi{cx?=	NFPxdHREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEV0yRMkC1JINmdGy\|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKgZox2\SCjc4PhfUwhTUN3ME2wMlA{Ps7:TT6=	M1XXc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293	MoH4SpVv[3Srb36gZZN{[Xl?		M3zkU\|EhcHJ?	MX\Jcohq[mm2aX;uJI9nKEOUQV[gbY4hcHWvYX6gTGVMOjl\|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:OC5yM{pOwG0v	NHj6OpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
A375	MXnDfZRwfG:6aXPpeJkh[XO\|YYm=		MkfsO\|IhcHK\|	M4nIe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE{PzViY3XscJMh\XiycnXzd4lv\yCEUlHGJHY3ODCHIH31eIFvfCCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmeiCkbIXlJIF{e2G7LDDJR\|UxRTBwMEe4{txONg>?	MlrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
A375	MWXGeY5kfGmxbjDhd5NigQ>?		NIXPZYUzKGi{cx?=	NW\KRm9xUW6qaXLpeIlwdiCxZjDCVmFHKFZ4MEDFJI12fGGwdD3t[YRq[XSnZDDNSWsheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNkBpenNuIFnDOVA:OC5yOENOwG0v	Mm\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HCC827	NIHNTJlHfW6ldHnvckBie3OjeR?=			M3nHZ2Rqe3CuYXPlcYVvfCCxZjDbN2heNWO7Y3zvdIFucW6nIH\yc40hW02RIG[0NFROKG23dHHueEBqdiCpZX\peIlvcWJicnXzbZN1[W62IHj1cYFvKEiFQ{iyO{Bk\WyuczDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDLbV0xNjF6N{lOwG0v	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd6N{G1Okc,Ojh5OEexOVY9N2F-
COLO679	M1W1Z2N6fG:2b4jpZ4l1gSCjc4PhfS=>		MlP5O\|IhcHK\|	NWT1fphrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0:OT{[3PUBk\WyuczDlfJBz\XO\|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyJIJtfWViYYPzZZktKEWFNUC9NE4zOTIQvF2u	M4D5[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HT144	NEjSeGVEgXSxdH;4bYNqfHliYYPzZZk>		NFf1S4I4OiCqcoO=	NGLrUYtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDF2NDDj[YxteyCneIDy[ZN{cW6pIFLSRWYhXjZyMFWgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{IHLseYUh[XO\|YYmsJGVEPTB;MD6yNljPxE1w	MlvSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
SK-MEL-28	NXPxOGdMS3m2b4TvfIlkcXS7IHHzd4F6		NIP4bXg4OiCqcoO=	MoPCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy\|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKgZox2\SCjc4PhfUwhTUN3ME2wMlQ2PM7:TT6=	MnntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293	MlexSpVv[3Srb36gZZN{[Xl?		NHLm[mMyKGi{	Mnn1TY5pcWKrdHnvckBw\iClTVXUJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO\|YYmsJGtlRTBwNUGz{txONg>?	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
HCT116	MnHGR5l1d3SxeHnjbZR6KGG\|c3H5		NUXGSZg3PzJiaILz	MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVAvPjZ7zszNMi=>	NIn6VHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
Hs578T	M1Lxe2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NYfxXYNwPzJiaILz	NX;NeFc3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUHN3N{jUJINmdGy\|IHX4dJJme3Orbnege4lt\CC2eYDlJGJTSUZiYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJiYnz1[UBie3OjeTygSWM2OD1{LkezOu69VS5?	NFP0TYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG2PFYzPid-MkKxOlg3OjZ:L3G+
DU145	NVe3Z2FKS3m2b4TvfIlkcXS7IHHzd4F6		MnHIO\|IhcHK\|	NWHFUWs5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgRnJCTiCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmeiCkbIXlJIF{e2G7LDDFR\|UxRTJwOUGx{txONg>?	M1XnWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293	NEfseZFHfW6ldHnvckBie3OjeR?=		NV7xS\|NbOSCqch?=	MVLJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gTGVMOjl\|IHPlcIx{KGGodHXyJFEhcHJiYomgZ49ueGW2aYTpc44h[mmwZHnu[{Bie3OjeTygT4Q:PC55zszNMi=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-
PC3	MnHtR5l1d3SxeHnjbZR6KGG\|c3H5		NWjHbnR2PzJiaILz	NITSXGJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQmLBSkBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldkBjdHWnIHHzd4F6NCCHQ{WwQVYvOjV5zszNMi=>	NYHHXVdURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlg3OjZpPkKyNVY5PjJ4PD;hQi=>
LNCAP	NV;y[49IS3m2b4TvfIlkcXS7IHHzd4F6		MXe3NkBpenN?	M2[2TGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFLSRWYh[W[2ZYKgO\|IhcHK\|IHL5JINmdGxidHn0[ZIh[my3ZTDhd5NigSxiRVO1NF03NjZ\|Md88UU4>	M2LkXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[4OlI3Lz5{MkG2PFYzPjxxYU6=
HEK293	MWTGeY5kfGmxbjDhd5NigQ>?		NWf6fIFmOSCqch?=	MkXmTY5pcWKrdHnvckBw\iCPRVuxJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO\|YYmsJGtlRTdwMd88UU4>	MoDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
HEK293	MUPGeY5kfGmxbjDhd5NigQ>?		NHftW3oyKGi{	Mnu5TY5pcWKrdHnvckBw\iCPRVuyJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjZoTldkAyKGi{IHL5JINwdXCndHn0bY9vKGKrbnTpcoch[XO\|YYmsJGtlRThwM988UU4>	MlywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
COLO205	NGfpeJdCdnSrdIXtc5Ih[XO\|YYm=	MlXTNVAhdWdxa3e=	M4W2V\|E1KGSjeYO=	NVLT[W02SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52\GVibX;1d4Uh[XRiMUCgcYcwc2duIIDvJIJq\CCob4KgNVQh\GG7cx?=	MorkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
COLO205	NED0cnpCdnSrdIXtc5Ih[XO\|YYm=	MYCzNEBu\y:tZx?=	NYfFOG5COTRiZHH5dy=>	Ml;aRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU\|IxPSClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDheIh6dWmlIH71[IUhdW:3c3WgZZQhOzBibXevb4ctKHCxIHLp[EBnd3JiMUSg[IF6ew>?	MlK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNki2NlYoRjJ{MU[4OlI3RC:jPh?=
COLO205	MknsRY51cXS3bX;yJIF{e2G7	MVGxNFAhdWdxa3e=	MYCxOEBl[Xm\|	M4rJdWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMhgGWwb3fyZYZ1\WRiaX6gZZRpgW2rYzDueYRmKG2xdYPlJIF1KDFyMDDt[{9s\yxicH:gZollKG[xcjCxOEBl[Xm\|	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF4OE[yOkc,OjJzNki2NlY9N2F-

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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 t_1/2 > 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

References

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

Chemical Information

Molecular Weight	517.46
Formula	C₂₄H₂₂F₃N₅O₅
CAS No.	1188910-76-0
Storage	3 years	-20°C	powder
Storage	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

Download Agerafenib (RXDX-105) SDF

In vivo Formulation Calculator (Clear solution)

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

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