PLX-4720

Catalog No.S1152

Molecular Weight(MW): 413.83

PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Cited by 97 Publications

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Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description

Targets

C-Raf-1 (Y340D/Y341D) ^[1] (Cell-free assay)	B-Raf (V600E) ^[1] (Cell-free assay)	BRK ^[1] (Cell-free assay)	B-Raf ^[1] (Cell-free assay)
6.7 nM	13 nM	130 nM	160 nM

In vitro

PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-Raf^V600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-Raf^V600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-Raf^V600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells. ^[1] PLX-4720 treatment (10 μM) significantly induces >14-fold expression of BIM in the PTEN⁺ cells, compared with the PTEN- cell lines (4-fold), giving an explanation of the resistance of PTEN^- cells to PLX-4720-induced apoptosis. ^[2]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
DU-4475	NFTlb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NESwOVVKSzVyPUCuNFc1PTdizszN	Mnr4V2FPT0WU
EoL-1-cell	MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkTNTWM2OD1yLkG0NVY3KM7:TR?=	NV3RNnNTW0GQR1XS
C32	NIDj[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUPJR\|UxRTBwMUWxN\|Eh\|ryP	NHfQVXBUSU6JRWK=
M14	M4HlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGi5VJRKSzVyPUCuNlE4PTdizszN	MoDtV2FPT0WU
CP50-MEL-B	NUj2U2RjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml;nTWM2OD1yLkK5O\|g1KM7:TR?=	NHuyNYtUSU6JRWK=
A101D	NILmdZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX3wN4RCUUN3ME2wMlMzPTh7IN88US=>	M36xV3NCVkeHUh?=
G-361	MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFT3No1KSzVyPUCuN\|Q3OzdizszN	NHW1[nVUSU6JRWK=
HT-144	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUfJR\|UxRTBwM{[zNlkh\|ryP	M4HP[nNCVkeHUh?=
ACN	M4jx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVLJR\|UxRTBwM{i0O\|ch\|ryP	MVnTRW5ITVJ?
COLO-829	Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF\vS3ZKSzVyPUCuN\|g6PjhizszN	NI[5cVVUSU6JRWK=
MEL-HO	NUfIWmpXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVTJR\|UxRTBwNEGxO\|kh\|ryP	NVnx[pU1W0GQR1XS
SH-4	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnnMTWM2OD1yLkSxOFIzKM7:TR?=	MWXTRW5ITVJ?
SK-MEL-3	M1nNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{fsRWlEPTB;MD61NVU3QCEQvF2=	NEHqV4pUSU6JRWK=
A375	NH\xeHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVjJR\|UxRTBwNkezOVkh\|ryP	M4m2PHNCVkeHUh?=
MMAC-SF	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NG\IS2xKSzVyPUCuOlg3OTRizszN	NX;XSohRW0GQR1XS
BHT-101	MmDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlS1TWM2OD1yLkewO\|AzKM7:TR?=	NXrW[Y5SW0GQR1XS
K5	M13RXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4DlVmlEPTB;MD63OlE1QCEQvF2=	MlvxV2FPT0WU
BV-173	M3LI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYTzbmdYUUN3ME2wMlc6PjR2IN88US=>	NHe5TlZUSU6JRWK=
RVH-421	NXTZb2ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NW\POXdjUUN3ME2wMlg3Pzl4IN88US=>	NIewW2lUSU6JRWK=
HCC2218	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NF7VS\|VKSzVyPUCuPFc5PDRizszN	M2ruenNCVkeHUh?=
WM-115	M1fq[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1u2PWlEPTB;MD64PFY6OiEQvF2=	M{TieXNCVkeHUh?=
SK-MEL-28	Mm[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFGzZXhKSzVyPUGuNFQ2PjlizszN	NYXnb\|drW0GQR1XS
COLO-679	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEXwXFFKSzVyPUGuNVA1PjRizszN	NFj1eXJUSU6JRWK=
MZ7-mel	NYrseWdUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NG\GOZhKSzVyPUGuNVQ6PjNizszN	NWHsUHlDW0GQR1XS
SK-MEL-30	M2\zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2m2b2lEPTB;MT6zN\|M5PiEQvF2=	MlfTV2FPT0WU
NCI-H209	NFHJdGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{HFRWlEPTB;MT62NFg3KM7:TR?=	NVzVZ4FFW0GQR1XS
HTC-C3	Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3LIe2lEPTB;MT62OlI6PCEQvF2=	Mnu2V2FPT0WU
KARPAS-45	M{fFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYrJR\|UxRTJwMES5O\|gh\|ryP	NYXpeW9sW0GQR1XS
NCI-SNU-5	M1jCb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4O4PGlEPTB;Mj6xNVk3QSEQvF2=	MoDMV2FPT0WU
KP-4	NX3SdGJRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml3lTWM2OD1{LkOwO\|g4KM7:TR?=	M13rVHNCVkeHUh?=
PA-1	MnPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWT3VYF[UUN3ME2yMlczPjd\|IN88US=>	M{Dp[3NCVkeHUh?=
HuO-3N1	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYjJR\|UxRTJwOEe5OFYh\|ryP	NXrLWZNLW0GQR1XS
NCI-H358	NVHIT2RPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NI\zeY9KSzVyPUKuPVIzOzJizszN	MVLTRW5ITVJ?
CTB-1	NEXHWWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3LYW2lEPTB;Mz60NFE4PiEQvF2=	MnPVV2FPT0WU
697	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1vGemlEPTB;Mz61OVI3PiEQvF2=	NXjtbWFTW0GQR1XS
CP66-MEL	MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXLJR\|UxRTRwMUW5Nlch\|ryP	MkX4V2FPT0WU
NB13	NVLBRXN5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVLJR\|UxRTRwNEmxO\|kh\|ryP	NX;6PYlbW0GQR1XS
DBTRG-05MG	NIfNUYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUXLV29uUUN3ME20MlU{OzJ3IN88US=>	MoTnV2FPT0WU
A2058	M2P3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NX;Ud4FmUUN3ME20MlczOTZ2IN88US=>	NFW4bIxUSU6JRWK=
KG-1	NXnGcmhQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{\nWWlEPTB;ND63N\|kxQCEQvF2=	M{PxUnNCVkeHUh?=
8305C	NWHFNG9ST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MljiTWM2OD13LkG4O\|Mh\|ryP	MlfjV2FPT0WU
RPMI-7951	MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXrUeIxuUUN3ME21MlgxOjh\|IN88US=>	NIH5enVUSU6JRWK=
CHL-1	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH;i[2lKSzVyPUWuPVc3ODNizszN	NH;KXXNUSU6JRWK=
TI-73	NILmU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXvJR\|UxRTZwMEC5NFIh\|ryP	MWDTRW5ITVJ?
HT-1080	NHPmfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYjJR\|UxRTZwMUC5OFYh\|ryP	NV;yXINvW0GQR1XS
ES5	M3TNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1HVN2lEPTB;Nj6xOFkzPCEQvF2=	M4[4THNCVkeHUh?=
8-MG-BA	M2TIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIDkPGdKSzVyPU[uNVgyOjlizszN	MneyV2FPT0WU
NB7	M2j3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4rtZmlEPTB;Nj6yNVM4OyEQvF2=	MYDTRW5ITVJ?
H4	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUnJR\|UxRTZwMkK0PVMh\|ryP	Mk\BV2FPT0WU
CAL-72	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1zJcWlEPTB;Nj60OVQzOyEQvF2=	NWnuVYRFW0GQR1XS
HCC1806	M2LJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1LrN2lEPTB;Nj64NVk{OSEQvF2=	MYjTRW5ITVJ?
BCPAP	NHrzVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2DLOmlEPTB;Nz6yNVc3PCEQvF2=	M4DlN3NCVkeHUh?=
LB2241-RCC	MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWfJR\|UxRTdwM{[5NFch\|ryP	MkftV2FPT0WU
COLO-741	MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1HKZWlEPTB;OD6wNVY4QSEQvF2=	M1[3UHNCVkeHUh?=
HSC-3	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHfmOnNKSzVyPUiuNFcxPjhizszN	NHvudXJUSU6JRWK=
SW982	Mo\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4r5NmlEPTB;OD60NVUyPiEQvF2=	NFuzNGJUSU6JRWK=
GCT	NYW5WJY4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEXMTFJKSzVyPUiuO\|U{OTRizszN	NUXHOlJpW0GQR1XS
KY821	M{\qbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYq1W2RLUUN3ME25MlA2OTd6IN88US=>	M3H1dHNCVkeHUh?=
JVM-3	MlrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVjJR\|UxRTlwNU[5PVkh\|ryP	NFfiUVJUSU6JRWK=
RS4-11	MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFH5foFKSzVyPUmuOlA1QCEQvF2=	NVO4cnJ1W0GQR1XS
VA-ES-BJ	NYfWd29[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3TSb2lEPTB;MUCuNFE1QSEQvF2=	M4TO[HNCVkeHUh?=
A431	Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NV20eoFxUUN3ME2xNE41OjF{IN88US=>	M2D5XHNCVkeHUh?=
LXF-289	NX6ydoZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX;JR\|UxRTFyLkS1PEDPxE1?	MkO3V2FPT0WU
SK-MEL-24	M4nqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MY\JR\|UxRTFyLkiyO\|Qh\|ryP	NX3MVXptW0GQR1XS
NOS-1	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MoTOTWM2OD1zMD64OFczKM7:TR?=	NGXKXVhUSU6JRWK=
KNS-62	MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXrhXG9nUUN3ME2xNU4zPDB2IN88US=>	MmK3V2FPT0WU
SK-HEP-1	MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnPBTWM2OD1zMT6zOVI4KM7:TR?=	NHfYfmJUSU6JRWK=
A3-KAW	NVm2O2N6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvSTWM2OD1zMT63NVc5KM7:TR?=	NV\Ge2I4W0GQR1XS
SK-LU-1	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4rmPWlEPTB;MUKuNlY2PSEQvF2=	NV;TNYhrW0GQR1XS
TYK-nu	NGXLbJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXL6SFF4UUN3ME2xNk4{QTN{IN88US=>	MmS1V2FPT0WU
NMC-G1	MlzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWTJR\|UxRTF{Lk[wOlIh\|ryP	MWrTRW5ITVJ?
BB65-RCC	NWrITnZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3rtVWlEPTB;MUKuO\|E3QSEQvF2=	M37QeXNCVkeHUh?=
QIMR-WIL	M2rNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXPJR\|UxRTF{Lki4N\|Mh\|ryP	M1\tU3NCVkeHUh?=
D-566MG	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1S3bWlEPTB;MUOuPVU4PiEQvF2=	MUjTRW5ITVJ?
KYSE-140	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NF;xUJlKSzVyPUG0MlA4PTNizszN	NGjyRotUSU6JRWK=
SCC-4	M3XwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIDBUFJKSzVyPUG0MlM{PTlizszN	NHi1[nFUSU6JRWK=
U251	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXLUVI9pUUN3ME2xOE45PDl{IN88US=>	M17acnNCVkeHUh?=
D-542MG	M1HxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnHNTWM2OD1zND65NlIzKM7:TR?=	NFrpT25USU6JRWK=
LAMA-84	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml7ZTWM2OD1zND65PVMzKM7:TR?=	MlK3V2FPT0WU
NCI-H720	NX\qcWkxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWHPV\|NsUUN3ME2xOU4zPjh2IN88US=>	M3W5cHNCVkeHUh?=
DEL	M3PnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHvmRmFKSzVyPUG1MlQzQTNizszN	NF7wUFBUSU6JRWK=
SBC-1	NUHGd4l7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGfQ[FZKSzVyPUG1MlQ{ODVizszN	NHzxe5FUSU6JRWK=
ECC10	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV;JR\|UxRTF3LkS0OVgh\|ryP	MmW0V2FPT0WU
Daoy	NU\YcXJZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkjTTWM2OD1zNT63OlE3KM7:TR?=	NF7BTHBUSU6JRWK=
SCH	Mn32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkfUTWM2OD1zNT63PFM2KM7:TR?=	MlTpV2FPT0WU
MZ2-MEL	M1LYfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlrkTWM2OD1zNj6wOlQ3KM7:TR?=	M4HFcXNCVkeHUh?=
CAL-12T	MkXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml6xTWM2OD1zNj60PFYzKM7:TR?=	MYjTRW5ITVJ?
KE-37	NFz0V4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoDWTWM2OD1zNj64NVA4KM7:TR?=	MVvTRW5ITVJ?
LS-411N	MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVzJR\|UxRTF5LkGxPEDPxE1?	NF7jcVlUSU6JRWK=
NCI-H2228	M1Tkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NI\TNWpKSzVyPUG3MlMxPzFizszN	MUfTRW5ITVJ?
SK-MEL-2	NGG2ZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M33wSmlEPTB;MUeuOFk3PSEQvF2=	M4WxNXNCVkeHUh?=
HN	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1TuW2lEPTB;MUeuO\|I1QCEQvF2=	M3fZbHNCVkeHUh?=
NCI-H1648	NXnlVGNST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVnHV5BDUUN3ME2xO{45OThizszN	MkP5V2FPT0WU
IA-LM	Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NUS2VYgyUUN3ME2xPE4{OTd{IN88US=>	NE\UNXRUSU6JRWK=
EW-13	NUT6UYVmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3zuXWlEPTB;MUiuOVcxQCEQvF2=	NHPrcpBUSU6JRWK=
YKG-1	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4\mVWlEPTB;MUmuOVcyOSEQvF2=	M4LzWXNCVkeHUh?=
KNS-81-FD	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmWzTWM2OD1zOT61PFU5KM7:TR?=	NWPvN2N5W0GQR1XS
23132-87	M{Hkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXz0e3JOUUN3ME2xPU44PjR{IN88US=>	M4XXWHNCVkeHUh?=
NUGC-3	MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF3OelJKSzVyPUG5Mlk5QDdizszN	M4W4VnNCVkeHUh?=
5637	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NELU[4pKSzVyPUKwMlA1PzhizszN	NEjwSIFUSU6JRWK=
NCI-H1755	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYXiU\|FwUUN3ME2yNE41PzZ2IN88US=>	NXTtSm9kW0GQR1XS
RH-18	M1H6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2XhdWlEPTB;MkCuOVc1QCEQvF2=	MUnTRW5ITVJ?
RXF393	Mnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1LOUWlEPTB;MkCuOlc2PiEQvF2=	MkHCV2FPT0WU
LU-134-A	MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYPJR\|UxRTJyLkewOVYh\|ryP	MX7TRW5ITVJ?
TE-12	MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHrtSI5KSzVyPUKwMlczODFizszN	MoXpV2FPT0WU
MOLT-4	NGTMfWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUTrZ4Y4UUN3ME2yNU4yQTF3IN88US=>	NFHLUJpUSU6JRWK=
IGR-1	MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NG\JNIpKSzVyPUKxMlM4QTZizszN	M1THWHNCVkeHUh?=
HOP-92	NHTPfI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXnhWZZLUUN3ME2yNU41QTh5IN88US=>	NY\oN\|VxW0GQR1XS
SK-MES-1	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVfhO2t4UUN3ME2yNU44OzhzIN88US=>	MX;TRW5ITVJ?
LU-65	Mlz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWTnRpFXUUN3ME2yNU45PjJ2IN88US=>	MmPnV2FPT0WU
MS-1	NID5XZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWDsSHo1UUN3ME2yNk4yOjB\|IN88US=>	M3vMdnNCVkeHUh?=
LoVo	NIGwcFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUPJR\|UxRTJ{LkK0OEDPxE1?	NY\UNWN6W0GQR1XS
A704	NFy2eHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX\JR\|UxRTJ{LkWxOVUh\|ryP	MXTTRW5ITVJ?
HT-1376	M13lRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVfPV4VbUUN3ME2yNk43ODV7IN88US=>	NVX5R\|FwW0GQR1XS
IST-MEL1	MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{PDdGlEPTB;MkKuOlc2OSEQvF2=	M2CxW3NCVkeHUh?=
Ramos-2G6-4C10	NWrZbIhYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlTaTWM2OD1{Mj63N\|Y3KM7:TR?=	NYfkPGhpW0GQR1XS
T47D	NV65T5FkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHTZOHFKSzVyPUKyMlc6PzlizszN	NI\acI9USU6JRWK=
HT-1197	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYXWRVA4UUN3ME2yN{4xQDF5IN88US=>	MW\TRW5ITVJ?
LB2518-MEL	NYixcXh2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGP5eJJKSzVyPUKzMlY1OTJizszN	NHLYTVBUSU6JRWK=
J-RT3-T3-5	M2LPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlPwTWM2OD1{ND63OVk2KM7:TR?=	MnzsV2FPT0WU
SK-NEP-1	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHTvXXJKSzVyPUK0Mlg4PDRizszN	M2\2U3NCVkeHUh?=
NCI-H526	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkHJTWM2OD1{NT6wNFI{KM7:TR?=	MlTDV2FPT0WU
IST-SL1	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnfjTWM2OD1{NT6yO\|UyKM7:TR?=	M3S5fnNCVkeHUh?=
HH	MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MW\JR\|UxRTJ3LkOxPVIh\|ryP	M2f6[3NCVkeHUh?=
NCI-H82	M4XCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NG[0fopKSzVyPUK1Mlk{QCEQvF2=	NFXHSJhUSU6JRWK=
SNU-449	M4Xwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIPV[W9KSzVyPUK3MlIxOThizszN	NX7j[m01W0GQR1XS
COR-L23	NIXvWodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mo\sTWM2OD1{Nz6yPFE{KM7:TR?=	NXi2ZZBpW0GQR1XS
LOXIMVI	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYrJR\|UxRTJ5LkO2PEDPxE1?	M1vocHNCVkeHUh?=
GR-ST	NVfscVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIXtUGRKSzVyPUK3MlY4ODZizszN	NF;DdoxUSU6JRWK=
NCI-SNU-1	M2S4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NEnZSmhKSzVyPUK3Mlk1PCEQvF2=	MlztV2FPT0WU
ALL-PO	M2rnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVrX[nhiUUN3ME2yPE4yPjB2IN88US=>	NXTwZ2V7W0GQR1XS
ML-2	MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmTLTWM2OD1{OD6yPFE1KM7:TR?=	M17NTnNCVkeHUh?=
HOP-62	NFjWbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1XkXWlEPTB;MkiuO\|E{KM7:TR?=	MmfKV2FPT0WU
EGI-1	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYLHcJM3UUN3ME2yPE45QDR3IN88US=>	NGjKOGNUSU6JRWK=
TCCSUP	MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4XJO2lEPTB;MkiuPVI4OiEQvF2=	NGnYSmdUSU6JRWK=
LB996-RCC	NHrtNWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVTJR\|UxRTJ7LkW2PFIh\|ryP	M1HsPHNCVkeHUh?=
LCLC-97TM1	NG\IWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MW\JR\|UxRTN{LkG5OlQh\|ryP	MWrTRW5ITVJ?
NCI-H1304	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{fvWWlEPTB;M{KuN\|MxOSEQvF2=	MYPTRW5ITVJ?
KP-N-YS	NXH6NnpvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYrJR\|UxRTN{LkW5O\|Mh\|ryP	NGDVSWZUSU6JRWK=
NCI-H1770	NYP5XVhYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnfXTWM2OD1\|Mz6xOlQ5KM7:TR?=	M1jJZXNCVkeHUh?=
EM-2	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4r0RWlEPTB;M{OuOlUxPCEQvF2=	NH\rS5NUSU6JRWK=
ChaGo-K-1	M3XqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2TMXmlEPTB;M{OuO\|I{PiEQvF2=	Mo\1V2FPT0WU
ACHN	NVXFXGdRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFHpT3JKSzVyPUOzMlg{QDVizszN	NYK5PWdLW0GQR1XS
MN-60	M1GyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{HiTWlEPTB;M{OuPFU1PCEQvF2=	MVTTRW5ITVJ?
EW-18	M1rMUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlLTTWM2OD1\|Mz64PVcyKM7:TR?=	MoPlV2FPT0WU
KGN	MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVHJR\|UxRTN3LkeyPVIh\|ryP	NXzmd\|NUW0GQR1XS
U031	NHHNTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIfM[pdKSzVyPUO1MlgyOzJizszN	NV7afpp5W0GQR1XS
HMV-II	NWDNbVVNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Moe2TWM2OD1\|Nj6wO\|c1KM7:TR?=	MXHTRW5ITVJ?
L-363	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4e5fGlEPTB;M{euOlQ2PSEQvF2=	M1fa[nNCVkeHUh?=
NCI-H1155	NIXxdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYrJR\|UxRTN6LkCwNVUh\|ryP	NYDxRoVmW0GQR1XS
NCI-H1793	M3;VO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGDQdmVKSzVyPUO4MlExOjZizszN	NH7RXW9USU6JRWK=
P30-OHK	M3LT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn;wTWM2OD1\|OD6xN\|MzKM7:TR?=	MYrTRW5ITVJ?
AN3-CA	NGjBcW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1\rfmlEPTB;M{iuNVYyPSEQvF2=	NWn6SpdLW0GQR1XS
UACC-257	NH3qdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NH;jVWFKSzVyPUO4Mlc6KM7:TR?=	M4npN3NCVkeHUh?=
MCF7	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnvGTWM2OD1\|OT64OlI6KM7:TR?=	M3ryXnNCVkeHUh?=
KP-N-YN	NI\TeFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVLJR\|UxRTRyLkSyPFUh\|ryP	NVHTTm93W0GQR1XS
T98G	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWnaUXNzUUN3ME20NE41QTV5IN88US=>	MUPTRW5ITVJ?
HGC-27	Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkjjTWM2OD12Mz6yO\|Qh\|ryP	MnTRV2FPT0WU
NCI-H1092	MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV7JR\|UxRTR\|LkK4PVUh\|ryP	MonNV2FPT0WU
KARPAS-299	NUnJdphPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXzFNWtMUUN3ME20N{4{ODdzIN88US=>	NYLUWGc6W0GQR1XS
LB1047-RCC	NXnxOJI3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIHGOJFKSzVyPUS0Mlk6PTlizszN	NELo[\|VUSU6JRWK=
786-0	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVywc\|VXUUN3ME20OU43PSEQvF2=	NUfue5lJW0GQR1XS
HCC2157	NXrwV\|FIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUHIPYwyUUN3ME20Ok4xOzV7IN88US=>	NEXQeW9USU6JRWK=
NY	NF\vNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmPLTWM2OD12Nj6xO\|c5KM7:TR?=	NEC5dI5USU6JRWK=
EFM-19	NIjTZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYj4UGRzUUN3ME20Ok44PTN\|IN88US=>	MUDTRW5ITVJ?
EW-16	NFnNTlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mme5TWM2OD12Nj63PFA3KM7:TR?=	NWT1XHBZW0GQR1XS
UM-UC-3	NGPke3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXvJR\|UxRTR4LkiwOVkh\|ryP	NHO0SWxUSU6JRWK=
HT-29	NXPQSGFRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2i2XGlEPTB;NEeuPFc6OiEQvF2=	NXnyboo6W0GQR1XS
LN-405	NETVVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NI\KOJFKSzVyPUS4MlA5OjdizszN	NWrqd2FGW0GQR1XS
NCI-H727	NYrQb\|JnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGHWXI5KSzVyPUS4Mlc4OjZizszN	NFvIc3hUSU6JRWK=
D-502MG	M2P4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NESwNYNKSzVyPUS4Mlk3PzZizszN	MX;TRW5ITVJ?
GMS-10	NIDVe29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1HES2lEPTB;NEmuNlk4PCEQvF2=	MnTmV2FPT0WU
MEL-JUSO	NHjX[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1\OSWlEPTB;NEmuN\|Q4KM7:TR?=	NWLwTmxvW0GQR1XS

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Assay

Methods	Test Index	PMID
Western blot	p-MEK / MEK / p-ERK / ERK / p-FAK(S910); PubMed: 23076151 J Biol Chem WM793 and WM793-Res NRAS cells were seeded overnight in the absence of PLX4720 and then treated with 1 μm PLX4720 for times ranging from 0 to 24 h. Samples were analyzed by Western blotting for phospho-MEK, total MEK, phospho-ERK1/2, total ERK1/2, phospho-S910 FAK, and total FAK. p-EGFR 1173 / EGFR / p-Akt / Akt; PubMed: 26023796 Oncotarget Three BRAF(V600E) glioma cell lines, NMC-G1, AM38 and DBTRG-05MG were subjected to a 24 hour time course treatment with 5 μM PLX4720 in the presence or absence of 1 μM HKI-272. These cells were serum starved for 16 hours before being stimulated with 10% FBS and harvested for immunoblotting analysis. Cells treated with PLX4720 alone showed an initial suppression of MEK and ERK phosphorylation followed by a profound rebound of MAPK pathway activation as early as one hour post-PLX4720 treatment. Elevated levels of EGFR phosphorylation were also observed in the PLX4720 treated cells. The extent of Akt phosphorylation increased upon PLX4720 treatment, although the extent varies between cell lines. In contrast, no reactivation of EGFR, MEK, ERK or Akt was observed in cells pre-treated with HKI-272. p27 / Cyclin D1 / pRb; PubMed: 21828154 Invest Ophthalmol Vis Sci Immunoblot analysis revealed that PLX4720 (3 μM) decreased levels of phosphorylated ERK, decreased levels of cyclin D1, increased levels of p27, and decreased levels of phosphorylated Rb in BRAF-mutant (OCM3) cells. On the contrary, in Gα-mutant (OMM1.3) UM cells, PLX4720 induced a paradoxical increase in phosphorylated ERK and Rb levels and an early increase in cyclin D1 levels but did not stimulate p27 levels. pAkt(Ser473) / pAkt(Thr308); PubMed: 21828154 Invest Ophthalmol Vis Sci Immunoblot analysis revealed that both AZD6244 and PLX4720 induced an early (within 2–6 hours of exposure) increase in the levels of phosphorylated Akt (at residues Ser473 and Thr308) in both BRAF-mutant OCM3 and Gα-mutant OMM1.3 cells. Eventually, and with prolonged drug exposure, the phosphorylation of Akt returned to baseline in Gα-mutant OMM1.3 cells and decreased even below baseline levels in BRAF-mutant OCM3 cells.	23076151 26023796 21828154
Immunofluorescence	LAMP1; PubMed: 30979895 Nat Commun Representative images of LysoTracker Red (red) and LAMP1 (green) immunostaining of PLX4720 (1 μM, 12 h-treated) A375 cells with depletion of the indicated genes. Note the reduced lysosome staining in PLX4720-treated cells upon TFEB depletion. ZKSCAN3 / TFEB ; PubMed: 30979895 Nat Commun Representative confocal images of subcellular translocation of endogenous TFEB (green) and ZKSCAN3 (red) in A375 cells treated with PLX4720 (1 μM, 12 h). n = 3 independent experiments.	30979895
Growth inhibition assay	Cell viability; PubMed: 27848137 J Neurooncol AM-38 and DBTRG-05MG cells were treated for 5 days. Media was changed once every 3 days. Cell viability was measured using WST-1 assay. Error bars indicate the variation between triplicate measurements. PLX4720 and PD0325901 alone or in combination reduced cell viability significantly. However, combined therapy led to the most significant cell viability reduction compared to either monotherapy in both AM-38 and DBTRG-05MG cell lines.	27848137
ELISA	mIFN-γ; PubMed: 23204132 Clin Cancer Res (C, D and E) IFN-γ secretion by pmel-1 T cells co-cultured with transduced melanoma cells (after cell sorting) that had been pre-treated with the indicated concentrations of PLX4720, as determined by ELISA. (P<0.05, * P<0.01) Data are representative of 3 independent experiments.	23204132

In vivo

Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-Raf^V600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-Raf^V600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation. ^[1] PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases. ^[3]

Protocol

Kinase Assay:^[1]	- Collapse In vitro Raf kinase activities: The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.
Cell Research:^[1]	- Collapse Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells Concentrations: Dissolved in DMSO, final concentrations ~1 mM Incubation Time: 24, 48, and 72 hours Method: Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37 °C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells Formulation: Suspended in vehicle (5% DMSO, 1% methylcellulose) Dosages: 5, 20, or 100 mg/kg Administration: Oral gavage once or twice daily (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	83 mg/mL (200.56 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+50% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing.	5mg/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 Download PLX-4720 SDF

Molecular Weight	413.83
Formula	C₁₇H₁₄ClF₂N₃O₃S
CAS No.	918505-84-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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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:
What would you recommend to make working solution for intraperitoneal injection into mice?
Answer:
PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

Pan Raf Inhibitor

AZ 628 : Pan-Raf inhibitor, BRAF, IC50=105 nM; BRAFV600E, IC50=34 nM; c-Raf-1, IC50=29 nM.
FDA-approved Raf Inhibitor

Sorafenib Tosylate : Approved by FDA for advanced renal cancer。
Newest Raf Inhibitor

TAK-632 ^New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

Related Raf Products

LY3009120 ^New

LY03009120 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. Phase 1.
Ravoxertinib (GDC-0994) ^New

GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Ulixertinib (BVD-523, VRT752271) ^New

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Vemurafenib (PLX4032, RG7204)

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.

Features:A novel and potent inhibitor of the B-RAF^V600E oncoprotein.
Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Sorafenib

Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.
Sorafenib Tosylate

Sorafenib Tosylate is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.
TAK-632

TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.
GDC-0879

GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
GW5074

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

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PLX-4720

Cited by 97 Publications

Purity & Quality Control

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Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download PLX-4720 SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

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Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

Tech Support

Frequently Asked Questions

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

Related Raf Products

Choose Your Country or Region

By Signaling Pathways

By product type

PLX-4720

Cited by 97 Publications

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download PLX-4720 SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

Tech Support

Frequently Asked Questions

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

Related Raf Products

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