PLX-4720

Catalog No.S1152

PLX-4720 Chemical Structure

Molecular Weight(MW): 413.83

PLX4720 is a potent and selective inhibitor of B-RafV600E 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.

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In DMSO USD 156 In stock
USD 120 In stock
USD 270 In stock
USD 670 In stock

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Cited by 45 Publications

9 Customer Reviews

  • Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.

    Cancer Discov 2013 3, 350-62. PLX-4720 purchased from Selleck.

    (D)Melanoma cell lines were treated with 0.5 uM Pi-103 and/or 2 uM PLX4720 for 4 h. Samples were analyzed by Western blotting for the indicated proteins. β-Actin served as a loading control. (E) Melanoma cell lines were treated with a dilution series of Pi-103 either alone or in combination with the BRAFV600E inhibitor PLX4720 at a concentration of 3 uM (D10) or 1 uM (453A0) for 3 d. Total cell numbers were determined with a cell titer blue assay. The Y-axis represents the percentage of living cells.

    Genes Dev 2012 26, 1055-69. PLX-4720 purchased from Selleck.

  • RAF inhibitors induce dimer formation between KSR and RAF, and activate KSR by CRAF. (A) GDC0879 but not PLX4720 induces BRAF/CRAF dimers. Cells overexpressing myc-CRAF and BRAF were treated with drug for 1 h and CRAF immunoprecipitates were immunoblotted for BRAF and CRAF (epitope tagged with myc). (B) GDC0879 but not PLX4720 enhances KSR/BRAF complexes. KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and BRAF after treatment with the indicated drug for 1 h and immunoblotted using antibodies to BRAF. (C) Both GDC0879 and PLX4720 induce KSR/CRAF complexes.KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and myc-CRAF after treatment with the indicated drug for 1 h and immunoblotted for CRAF using myc antibodies. (D and E) Requirement of KSR for drug-induced ERK activation. Lysates fromwild-type and KSR deficient fibroblasts, transfected with RASV12, were treated with the indicated doses of either GDC-0879 (D) or PLX4720 (E) for 1 h. Lysates were immunoblotted for phospho-ERK1 and 2, ERK2, and RASV12. (F) KSR and CRAF cooperate to activate MEK. Cells expressing the indicated constructs were treated with a 50 μM PLX4720 for 2 h before cell lysates were prepared and analyzed for pMEK by immunoblotting. CRAF(TM) refers to the T421M gatekeeper mutant that cannot bind to the drug(4). (G) KSR in vitro kinase reactions. Cells were cotransfected with WT or ATP binding deficient KSR and CRAF and immunoprecipitates prepared after cells were treated with an activating dose of PLX (10 μM) for 1 h. KSR immunoprecipitates were prepared, pretreated with 50 uM PLX4720 to inhibit coprecipitating RAF activity, and then tested for kinase activity using purified MEK. MEK phosphorylation was detected using a pMEK specific antibody.

    Proc Natl Acad Sci USA 2011 108, 6067-6072. PLX-4720 purchased from Selleck.

    PTEN predicts for PLX4720-induced apoptosis. A, basal PTEN and phospho-AKT(pAKT; S473, T308) expression in PTENt (WM164, 451Lu, SK-mel-28, WM983A, WM35, WM51) and PTEN (WM239A, WM266-4, WM793, M233, WM9, 1205Lu) melanoma cell lines. B, MTT assay of PTENt (gray)-expressing versus PTEN (black) cell lines. C, PTENt cells are more sensitive than PTEN cells to PLX4720-mediated apoptosis. Cells treated for 48 hours with 3 or 10 μmol/L PLX4720 before being stained for TMRM and Annexin-V. Apoptosis was measured by flow cytometry. Data shows mean SE mean of 3 independent experiments.*, PTENt cohort significantly different from PTEN cohort(P < 0.05).

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • Loss of PTEN is associated with PI3K/AKT signaling following BRAF inhibition. A, PTENt (WM35, WM164, WM983A) and PTEN (M233, WM9,WM793, 1205Lu) cells were treated with PLX4720 (24 hours: 0.03-3 μmol/L) and probed for phospho-PDK1 (pPDK1), total PDK1, phospho-AKT (pAKT), total AKT (tAKT), phospho-S6 (pS6), and total S6. Numbers indicate relative intensity of pPDK1 normalized to PDK1 and pAKT normalized to tAKT. B, PLX4720 increases pAKT following PTEN knockdown. WM35 cells were incubated with nontargeting siRNA (NT) or 2 different PTEN-specific siRNA's (PTEN) before treatment with either vehicle or PLX4720 (3 μmol/L). C, siRNA knockdown of BRAF increases pAKT in melanoma cell lines that are PTEN. WM164 (PTENt) and WM793 (PTEN) cells were incubated with lipofectamine alone (L), nontargeting siRNA (NT), or BRAF-specific siRNA (BRAF). Protein was extracted, resolved, and probed for BRAF, pAKT, total AKT, and GAPDH.

     

     

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    Dual PI3K/BRAF inhibition upregulates BIM and enhances apoptosis in PTEN cells. A, left, Western blot of 1205Lu cells treated with PLX4720 (3 μmol/L, 48 hours), the PI3K inhibitor GDC-0941 (3 μmol/L, 48 hours), or both drugs in combination (PtG); right, immunofluorescence staining of BIM (green) and DAPI (blue) in PTEN cells following PLX4720 treatment (3 μmol/L, 48 hours), the PI3K inhibitor LY294002 (10 μmol/L, 48 hours), or both drugs in combination (PLXtLY). B, left, immunofluorescence staining of PTEN 1205Lu following combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48hours) increases nuclear localization of FOXO3a (green). DAPI is shown in blue. Magnification 40. Right, combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48 hours) increases PTEN WM793 BIM mRNA levels to those observed with single BRAF inhibition (3 μmol/L PLX4720, 48 hours) in the PTENt WM35. C, PTEN cells were treated with PLX4720 (3 μmol/L, 48 hours), GDC-0941 (3 μmol/L, 48hours), or a combination of the 2 drugs (3Pt3G) before Annexin-V staining was analyzed by flow cytometry (*, P < 0.05 between the drug combination and each inhibitor alone). D, combined BRAF/PI3K inhibitor treatment blocks the escape of 1205Lu cells (PTEN) from therapy. Spheroids of 1205Lu cells were treated with either PLX4720 alone (3 and 10 μmol/L: data shows 3 μmol/L), LY294002 (10 μmol/L) alone or a combination of the 2 drugs for 72 hours. In other studies, spheroids were treated with drugs for 72 hours and then allowed to recover for 120 hours. Micrograph shows viability staining (green ?live cells, red ?dead cells). Magnification 10.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • LC-MRM identifies differential regulation of BIM in PTENt and PTEN cell lines following PLX4720 treatment. A, representative LC-MRM data showing the fold changes in the expression of Bak, Bax, Bcl-2, Bcl-w, Bcl-xL, BID, BIM, Bok, and Mcl-1 over internal standard in the WM164 (PTENt) and 1205Lu (PTEN) cell lines following treatment with PLX4720 (10 μmol/L, 0-48 hours). Statistical analysis of BIM fold change in PTEN versus PTENt. *, P < 0.05. B, Western blot showing BIM expression following PLX4720 treatment (10 μmol/L, 0-48 hours) in PTEN (WM793, 1205Lu) and WM164 cell lines (PTENt). C, immunofluorescence staining, showing expression of BIM and DAPI staining of PTEN (M233, WM9, WM793, 1205Lu) and PTENt (WM35, WM164, WM983A) cells following PLX4720 treatment (3 μmol/L, 48 hours).D, Western blot showing BAD phosphorylation following treatment with PLX4720 (0-48 hours) in PTEN (WM793,1205Lu) and PTENt WM164. Annexin V binding following treatment with 3 or 10 μmol/L PLX4720 (48 hours) showing increased apoptosis in WM793 stably overexpressing WT BAD. *, P < 0.05.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    B-RafV600E mutated melanoma line, SK-MEL-28, was treated with different doses of PLX-4720 for 4 h or 22 h.  Cell lysates were analyzed by Western blotting to determine the levels of phosphorylated MEK1/2 (pMEK1/2) and phosphorylated ERK1/2 (pERK1/2). MEK1/2 is the substrate of B-Raf while ERK1/2 is the substrate of MEK1/2.  Data show that phosphorylation of MEK1/2 and ERK1/2 was significantly inhibited by PLX-4720 treatment although total MEK1/2 or ERK1/2 protein levels were not affected. No pMEK1/2 or pERK1/2 signal was detected even after prolonged exposure, indicating that the inhibitor at 1 μM is very effective in blocking the constitutive kinase activity of B-RafV600E.  This data is consistent with the previous result demonstrating the effect of PLX-4720 in the B-RafV600E mutated melanoma line, A375 – Fig. 2A, Nature 464:431 (2010)

     

     

    Dr. Jong-In Park of Medical College of Wisconsin. PLX-4720 purchased from Selleck.

  • A dose titration of PLX-4720 in A375 melanoma cells which possess a V600E B-Raf mutation.Effects of  increasing PLX-4720 dose on Erk phosphorylation and on tumor cell proliferation as determined by MTT  assay are shown.

     

     

    Dr. Daniel C.Cho of Harvard Medical School. PLX-4720 purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description PLX4720 is a potent and selective inhibitor of B-RafV600E 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.
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)
FRK [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM 1.3 μM
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-RafV600E 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-RafV600E 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-RafV600E-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 Concentration Incubation Time Formulation Activity Description PMID
DU-4475 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWflPItuUUN3ME2wMlA4PDV5IN88US=> MVvTRW5ITVJ?
EoL-1-cell MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMUSxOlYh|ryP MV3TRW5ITVJ?
C32 NHLFeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfqXI1KSzVyPUCuNVUyOzFizszN MmLCV2FPT0WU
M14 M33Fc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVuyOXQ5UUN3ME2wMlIyPzV5IN88US=> M4XDR3NCVkeHUh?=
CP50-MEL-B MkT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvCTWM2OD1yLkK5O|g1KM7:TR?= MljrV2FPT0WU
A101D MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDwfVZKSzVyPUCuN|I2QDlizszN MkezV2FPT0WU
G-361 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwM{S2N|ch|ryP M2e5O3NCVkeHUh?=
HT-144 M4DhS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofMTWM2OD1yLkO2N|I6KM7:TR?= MUXTRW5ITVJ?
ACN MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T5eGlEPTB;MD6zPFQ4PyEQvF2= M4GyXXNCVkeHUh?=
COLO-829 M{TS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwM{i5Olgh|ryP NGXPclZUSU6JRWK=
MEL-HO M2rhcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwNEGxO|kh|ryP M2XSTnNCVkeHUh?=
SH-4 M2HobGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwNEG0NlIh|ryP M2TNdXNCVkeHUh?=
SK-MEL-3 Moq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PHbWlEPTB;MD61NVU3QCEQvF2= MXXTRW5ITVJ?
A375 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT6UplKSzVyPUCuOlc{PTlizszN NUe0SXNLW0GQR1XS
MMAC-SF M2TsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\qTWM2OD1yLk[4OlE1KM7:TR?= MlG2V2FPT0WU
BHT-101 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X5fWlEPTB;MD63NFcxOiEQvF2= NWnnUmt4W0GQR1XS
K5 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjlbHdKSzVyPUCuO|YyPDhizszN MoW0V2FPT0WU
BV-173 M37pTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwN{m2OFQh|ryP M4TSfHNCVkeHUh?=
RVH-421 MlryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LZbGlEPTB;MD64Olc6PiEQvF2= NGHlUnhUSU6JRWK=
HCC2218 NHXXU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUKzeZVtUUN3ME2wMlg4QDR2IN88US=> MkP3V2FPT0WU
WM-115 M2\x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW5OoxKSzVyPUCuPFg3QTJizszN MWXTRW5ITVJ?
SK-MEL-28 M{DrbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HBUmlEPTB;MT6wOFU3QSEQvF2= M{XVNnNCVkeHUh?=
COLO-679 NXj5NnBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXBTWM2OD1zLkGwOFY1KM7:TR?= NX\IUlc3W0GQR1XS
MZ7-mel M3ThbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\LUGZKSzVyPUGuNVQ6PjNizszN M2\2Z3NCVkeHUh?=
SK-MEL-30 NXfJOnlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvSPXloUUN3ME2xMlM{Ozh4IN88US=> M1jJcHNCVkeHUh?=
NCI-H209 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDwRXlKSzVyPUGuOlA5PiEQvF2= M2DONHNCVkeHUh?=
HTC-C3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\kTWM2OD1zLk[2Nlk1KM7:TR?= M{DXUnNCVkeHUh?=
KARPAS-45 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILzXGdKSzVyPUKuNFQ6PzhizszN M4TqSHNCVkeHUh?=
NCI-SNU-5 NXzX[I1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L4fWlEPTB;Mj6xNVk3QSEQvF2= NYHRWWVFW0GQR1XS
KP-4 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KxSGlEPTB;Mj6zNFc5PyEQvF2= MUjTRW5ITVJ?
PA-1 NEHEVGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLBPVVFUUN3ME2yMlczPjd|IN88US=> Mmm0V2FPT0WU
HuO-3N1 NFOxZnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFW2dHlKSzVyPUKuPFc6PDZizszN MYDTRW5ITVJ?
NCI-H358 MkXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\rWZpMUUN3ME2yMlkzOjN{IN88US=> MnnIV2FPT0WU
CTB-1 M1jjeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PpTWlEPTB;Mz60NFE4PiEQvF2= NUPPTI5YW0GQR1XS
697 NYHEbIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnjeHZxUUN3ME2zMlU2OjZ4IN88US=> M17TXHNCVkeHUh?=
CP66-MEL NXj4RpNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrWN5FKSzVyPUSuNVU6OjdizszN NYjhPZd6W0GQR1XS
NB13 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTRwNEmxO|kh|ryP Mmn6V2FPT0WU
DBTRG-05MG M3KzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDmcWxiUUN3ME20MlU{OzJ3IN88US=> MYjTRW5ITVJ?
A2058 M17sW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTRwN{KxOlQh|ryP M1;6ZnNCVkeHUh?=
KG-1 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTRwN{O5NFgh|ryP NYHwbG1EW0GQR1XS
8305C NWD0WXhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnjO4V2UUN3ME21MlE5PzNizszN MnWzV2FPT0WU
RPMI-7951 NHfEXYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3xXZAzUUN3ME21MlgxOjh|IN88US=> MYHTRW5ITVJ?
CHL-1 NVTxNIJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPzeZpKSzVyPUWuPVc3ODNizszN Mm\qV2FPT0WU
TI-73 NHP2VWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTZwMEC5NFIh|ryP M{ToZ3NCVkeHUh?=
HT-1080 Mn\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjrTWM2OD14LkGwPVQ3KM7:TR?= MYXTRW5ITVJ?
ES5 NIDpWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jNUGlEPTB;Nj6xOFkzPCEQvF2= NIK4T2JUSU6JRWK=
8-MG-BA NXixOlZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\u[WhKSzVyPU[uNVgyOjlizszN NYG2Z5Z7W0GQR1XS
NB7 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGwTWM2OD14LkKxN|c{KM7:TR?= NFXF[HFUSU6JRWK=
H4 NV23RlBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjLTWM2OD14LkKyOFk{KM7:TR?= NV3HPWxNW0GQR1XS
CAL-72 NIHG[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTZwNEW0NlMh|ryP Mn7EV2FPT0WU
HCC1806 NFHXUFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:2RXFlUUN3ME22MlgyQTNzIN88US=> MVHTRW5ITVJ?
BCPAP NW\rUFVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorGTWM2OD15LkKxO|Y1KM7:TR?= MnzmV2FPT0WU
LB2241-RCC NVf5ZVJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTEe|E5UUN3ME23MlM3QTB5IN88US=> M{XlO3NCVkeHUh?=
COLO-741 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknwTWM2OD16LkCxOlc6KM7:TR?= NUf3XmNIW0GQR1XS
HSC-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ixNGlEPTB;OD6wO|A3QCEQvF2= M4CwOXNCVkeHUh?=
SW982 NYS0fJRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\IS2lEPTB;OD60NVUyPiEQvF2= NUTiT|dOW0GQR1XS
GCT NUHqT5B7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjVPJpKSzVyPUiuO|U{OTRizszN NISxUYlUSU6JRWK=
KY821 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLN[|R[UUN3ME25MlA2OTd6IN88US=> MXLTRW5ITVJ?
JVM-3 NELnT2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjkOJVnUUN3ME25MlU3QTl7IN88US=> NVvYbHZNW0GQR1XS
RS4-11 NGToW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD0TWM2OD17Lk[wOFgh|ryP NUDxWpBGW0GQR1XS
VA-ES-BJ M4nT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFyLkCxOFkh|ryP MkKzV2FPT0WU
A431 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTTWM2OD1zMD60NlEzKM7:TR?= NY[ySGxrW0GQR1XS
LXF-289 NIDD[XlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnOTWM2OD1zMD60OVgh|ryP NWi1WGlwW0GQR1XS
SK-MEL-24 M2XJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLTWM2OD1zMD64Nlc1KM7:TR?= MnPMV2FPT0WU
NOS-1 NEXOSFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz1dY1uUUN3ME2xNE45PDd{IN88US=> MkHtV2FPT0WU
KNS-62 NHzWbHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFzLkK0NFQh|ryP NV3OTndbW0GQR1XS
SK-HEP-1 NFL5[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrvZoVKSzVyPUGxMlM2OjdizszN MmmwV2FPT0WU
A3-KAW M2\vUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFzLkexO|gh|ryP NX;Eb|RMW0GQR1XS
SK-LU-1 MlTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTkT5EyUUN3ME2xNk4zPjV3IN88US=> NETsSI5USU6JRWK=
TYK-nu NFrWZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvnPI5WUUN3ME2xNk4{QTN{IN88US=> NYC2bI15W0GQR1XS
NMC-G1 Mke4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi3TWM2OD1zMj62NFYzKM7:TR?= MkPyV2FPT0WU
BB65-RCC NHmxU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHvXnd{UUN3ME2xNk44OTZ7IN88US=> MknpV2FPT0WU
QIMR-WIL NH[xRoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL0SpJKSzVyPUGyMlg5OzNizszN NV3VTlliW0GQR1XS
D-566MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3ITWM2OD1zMz65OVc3KM7:TR?= M1zUenNCVkeHUh?=
KYSE-140 NGLvdFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnXTWM2OD1zND6wO|U{KM7:TR?= NEjCS4lUSU6JRWK=
SCC-4 M2fXUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P4[mlEPTB;MUSuN|M2QSEQvF2= M{PsXHNCVkeHUh?=
U251 NIi3SGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPn[mxKSzVyPUG0Mlg1QTJizszN MWnTRW5ITVJ?
D-542MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjKPYI1UUN3ME2xOE46OjJ{IN88US=> MoT3V2FPT0WU
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ECC10 NV75[IVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ri[WlEPTB;MUWuOFQ2QCEQvF2= NGrpcJZUSU6JRWK=
Daoy MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWruXnZTUUN3ME2xOU44PjF4IN88US=> M3;vSHNCVkeHUh?=
SCH NELBO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF3Lke4N|Uh|ryP NE\KTohUSU6JRWK=
MZ2-MEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\JTWM2OD1zNj6wOlQ3KM7:TR?= M2D4T3NCVkeHUh?=
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KE-37 M3X5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFSxZoRKSzVyPUG2MlgyODdizszN NUHIRXd[W0GQR1XS
LS-411N MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF5LkGxPEDPxE1? M4\heHNCVkeHUh?=
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NCI-H1648 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3HcIdKSzVyPUG3MlgyQCEQvF2= M3HKNnNCVkeHUh?=
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5637 MnfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJyLkC0O|gh|ryP NVjsPHhYW0GQR1XS
NCI-H1755 NXr2Wll5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\BW2lEPTB;MkCuOFc3PCEQvF2= NIjsNnRUSU6JRWK=
RH-18 NXzTcXI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3CcVZOUUN3ME2yNE42PzR6IN88US=> MoDIV2FPT0WU
RXF393 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vyRWlEPTB;MkCuOlc2PiEQvF2= MUPTRW5ITVJ?
LU-134-A MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXETWM2OD1{MD63NFU3KM7:TR?= NV;UUFNrW0GQR1XS
TE-12 MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK5VVJLUUN3ME2yNE44OjBzIN88US=> NWj3dpg6W0GQR1XS
MOLT-4 NVHPT3h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJzLkG5NVUh|ryP MUfTRW5ITVJ?
IGR-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi5dHVKUUN3ME2yNU4{Pzl4IN88US=> M2X2RXNCVkeHUh?=
HOP-92 MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTjbGxNUUN3ME2yNU41QTh5IN88US=> MWTTRW5ITVJ?
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LU-65 NE\CcXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH35N3hKSzVyPUKxMlg3OjRizszN NFvOS3VUSU6JRWK=
MS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XGVWlEPTB;MkKuNVIxOyEQvF2= MX\TRW5ITVJ?
LoVo M4H4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHWzcnVKSzVyPUKyMlI1PCEQvF2= MkXsV2FPT0WU
A704 M3jhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjrdWJKSzVyPUKyMlUyPTVizszN M4PWfnNCVkeHUh?=
HT-1376 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPZS3pbUUN3ME2yNk43ODV7IN88US=> M{j4XXNCVkeHUh?=
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Ramos-2G6-4C10 M37oUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfUTWM2OD1{Mj63N|Y3KM7:TR?= NIPEb5JUSU6JRWK=
T47D NF;KUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjjTWM2OD1{Mj63PVc6KM7:TR?= MWfTRW5ITVJ?
HT-1197 M1zYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TxXWlEPTB;MkOuNFgyPyEQvF2= M1v0PHNCVkeHUh?=
LB2518-MEL M1HPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ|Lk[0NVIh|ryP M4ThcXNCVkeHUh?=
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SK-NEP-1 Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37qTWlEPTB;MkSuPFc1PCEQvF2= M3flR3NCVkeHUh?=
NCI-H526 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJ3LkCwNlMh|ryP NYnUTmloW0GQR1XS
IST-SL1 NVrVWnJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfRTWM2OD1{NT6yO|UyKM7:TR?= NEWyb3VUSU6JRWK=
HH NWfKOG46T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ3LkOxPVIh|ryP MY\TRW5ITVJ?
NCI-H82 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfpblJKSzVyPUK1Mlk{QCEQvF2= MnvpV2FPT0WU
SNU-449 MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJ5LkKwNVgh|ryP NF\QeFVUSU6JRWK=
COR-L23 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTqTWM2OD1{Nz6yPFE{KM7:TR?= NF3yTm1USU6JRWK=
LOXIMVI NVrWc|BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\HcGlEPTB;MkeuN|Y5KM7:TR?= M3LHN3NCVkeHUh?=
GR-ST NHfBZ2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C5bWlEPTB;MkeuOlcxPiEQvF2= NXGxblgzW0GQR1XS
NCI-SNU-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX1R3VKSzVyPUK3Mlk1PCEQvF2= MWTTRW5ITVJ?
ALL-PO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPfndKSzVyPUK4MlE3ODRizszN M4LRenNCVkeHUh?=
ML-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1yydGlEPTB;MkiuNlgyPCEQvF2= NXqwOIRMW0GQR1XS
HOP-62 NEC2fFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHrZXhKSzVyPUK4MlcyOyEQvF2= M1;hd3NCVkeHUh?=
EGI-1 M3joVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP2RoNFUUN3ME2yPE45QDR3IN88US=> M{PW[3NCVkeHUh?=
TCCSUP M1HJRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLrTWM2OD1{OD65NlczKM7:TR?= NIX1Z45USU6JRWK=
LB996-RCC NIfSSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfD[|BKSzVyPUK5MlU3QDJizszN NF;0SY9USU6JRWK=
LCLC-97TM1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjKWlg4UUN3ME2zNk4yQTZ2IN88US=> MX\TRW5ITVJ?
NCI-H1304 NXHGd3NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTQeGtKSzVyPUOyMlM{ODFizszN MUXTRW5ITVJ?
KP-N-YS Mmn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOybIxKUUN3ME2zNk42QTd|IN88US=> NVHFNW9kW0GQR1XS
NCI-H1770 M2DJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTN|LkG2OFgh|ryP MVLTRW5ITVJ?
EM-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITWUIxKSzVyPUOzMlY2ODRizszN NFfwN4FUSU6JRWK=
ChaGo-K-1 NXnCXVlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfJTWM2OD1|Mz63NlM3KM7:TR?= MWrTRW5ITVJ?
ACHN MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnNZm95UUN3ME2zN{45Ozh3IN88US=> NIHEe2VUSU6JRWK=
MN-60 M3zTPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7oVJVKSzVyPUOzMlg2PDRizszN MmftV2FPT0WU
EW-18 NFXGeodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzWTWM2OD1|Mz64PVcyKM7:TR?= NIj6VYlUSU6JRWK=
KGN NWHXdZNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfOTnhJUUN3ME2zOU44Ojl{IN88US=> MWrTRW5ITVJ?
U031 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTN3LkixN|Ih|ryP NIr1SYdUSU6JRWK=
HMV-II NG\rZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTN4LkC3O|Qh|ryP NFv1UplUSU6JRWK=
L-363 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HZWGlEPTB;M{euOlQ2PSEQvF2= NGG2WWpUSU6JRWK=
NCI-H1155 NY[yd4sxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fE[mlEPTB;M{iuNFAyPSEQvF2= M3fJRXNCVkeHUh?=
NCI-H1793 M1TJXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rRU2lEPTB;M{iuNVAzPiEQvF2= MWHTRW5ITVJ?
P30-OHK MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrCWXFKSzVyPUO4MlE{OzJizszN M2ixd3NCVkeHUh?=
AN3-CA NXjqTndRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fWU2lEPTB;M{iuNVYyPSEQvF2= MnfVV2FPT0WU
UACC-257 M17FZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3iUpVYUUN3ME2zPE44QSEQvF2= NWHST|NkW0GQR1XS
MCF7 M{TzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTN7Lki2Nlkh|ryP MkHNV2FPT0WU
KP-N-YN NIDm[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30enlKSzVyPUSwMlQzQDVizszN Ml7FV2FPT0WU
T98G NELBbpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDJTWM2OD12MD60PVU4KM7:TR?= NVjBfG9OW0GQR1XS
HGC-27 NWTpd3ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HPUWlEPTB;NEOuNlc1KM7:TR?= NV\ocHhjW0GQR1XS
NCI-H1092 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR|LkK4PVUh|ryP NFPhSlVUSU6JRWK=
KARPAS-299 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTlTWM2OD12Mz6zNFcyKM7:TR?= NHfWNZFUSU6JRWK=
LB1047-RCC NGHnUIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTR2Lkm5OVkh|ryP MXfTRW5ITVJ?
786-0 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnkNZlKSzVyPUS1MlY2KM7:TR?= MXjTRW5ITVJ?
HCC2157 NWrsT5VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\HRmZKSzVyPUS2MlA{PTlizszN MYnTRW5ITVJ?
NY NUXwdlhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfCTWM2OD12Nj6xO|c5KM7:TR?= M4PqVnNCVkeHUh?=
EFM-19 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrDXFZKSzVyPUS2Mlc2OzNizszN NFz2R3FUSU6JRWK=
EW-16 NHnQfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjwdItLUUN3ME20Ok44QDB4IN88US=> M3;wOHNCVkeHUh?=
UM-UC-3 NFPUZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTR4LkiwOVkh|ryP NH24O|BUSU6JRWK=
HT-29 NFX4d49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHFTWM2OD12Nz64O|kzKM7:TR?= NHfwcItUSU6JRWK=
LN-405 NInNbJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPuTWM2OD12OD6wPFI4KM7:TR?= M4rYd3NCVkeHUh?=
NCI-H727 NIXZRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIOwN29KSzVyPUS4Mlc4OjZizszN NVvGT2VrW0GQR1XS
D-502MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS4fVlKSzVyPUS4Mlk3PzZizszN NX;NUFFFW0GQR1XS
GMS-10 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDZVplKSzVyPUS5MlI6PzRizszN M4jOVXNCVkeHUh?=
MEL-JUSO NHGxN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTR7LkO0O{DPxE1? Mm\hV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-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-RafV600E, 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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)

Solubility (25°C)

In vitro DMSO 83 mg/mL (200.56 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 413.83
Formula

C17H14ClF2N3O3S

CAS No. 918505-84-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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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

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Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

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