Sorafenib

Catalog No.S7397 Synonyms: BAY 43-9006

Sorafenib Chemical Structure

Molecular Weight(MW): 464.82

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.

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Cited by 60 Publications

7 Customer Reviews

  • Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.

    J Invest Dermatol 2011 131, 1886–1895. Sorafenib purchased from Selleck.

    (A) were exposed to 200 uM gentamicin for various time periods. Immunoreactivity for phosphorylated JNK (green) and c-Jun (blue) in hair cells increased in a time-dependent manner. B. Hair cells from explants pre-treated with 500 nM sorafenib displayed a near complete inhibition of JNK activation at all time points analyzed.

    J Neurosci 2013 33(7), 3079-93. Sorafenib purchased from Selleck.

  • Sorafenib in combination with metformin or the AMPK activator salicylate enhances AMPK activation. a, b, AMPK activation with the combination of sorafenib and metformin in LKB1 mutant KRAS mutant (A549 and H460) NSCLC cells (a), LKB1 wild-type KRAS mutant (H358) (b, left panel) or LKB1 mutant KRAS wild-type (H838) NSCLC cells (b, right panel). Cells were treated for 48 hr with sorafenib (1-3 uM), metformin (1–1.5 mM) or the combination of sorafenib and metformin with the same concentrations as were used for the individual treatments. c, AMPK activation with the combination of sorafenib and salicylate in LKB1 mutant KRAS mutant (A549 and H460) or LKB1 mutant KRAS wild-type (H838) NSCLC cells. Cells were treated for 48 hr with sorafenib (1–3 uM), salicylate (1–1.5 mM) or the combination of sorafenib and salicylate with the same concentrations as were used for the individual treatments. Cell lysates were harvested for western blot analysis and probed with the indicated antibodies.

    Int J Cancer 2012 10.1002/ijc.29113.. Sorafenib purchased from Selleck.

    Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.

    Mol Cancer Res 2014 12(10), 1377-87. Sorafenib purchased from Selleck.

  • Sorafenib and PX-866 interact to suppress tumor growth in vivo. Mice were PO administered vehicle diluent, sorafenib (25 mg/kg), PX-866 (2 mg/kg), or the drug combination QD for 3 days. Animals were monitored daily and tumor volume determined every fifth day. Tumors from animals were isolated at day 15 and fixed, sectioned (10-um), and stained against proliferation (Ki67 staining), phospho-ERK1/2 and phospho-AKT staining, the levels of tumor cell apoptosis/cleaved caspase 3, as well as with H&E and 4′,6-diamidino-2-phenylindole (DAPI).

    Mol Pharmacol 2013 84(4), 562-71. Sorafenib purchased from Selleck.

    Effects of sorafenib or sunitinib on LicA-induced cell death, ER stress responses, PLCc1, Ca2+, and ROS in HepG2 cells. HepG2 cells were pretreated with sorafenib or sunitinib for 1 h, then treated with LicA or TG for 1 h (for P-eIF2a and P-PLCc1) or 24 h (for CHOP, ATF6a(p90), and caspase-4). The cell lysates were subjected to Western blot analyses using antibodies against CHOP, ATF6a(p90), caspase-4(C), P-eIF2a, and b-actin.

    Apoptosis 2014 19(4), 682-97. Sorafenib purchased from Selleck.

  • PLoS One 2013 8(1), e54595. Sorafenib purchased from Selleck.

Purity & Quality Control

Choose Selective Raf Inhibitors

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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 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.
Targets
Raf-1 [1]
(Cell-free assay)
mVEGFR2(Flk1) [1]
(Cell-free assay)
mVEGFR3 [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
B-Raf (V599E) [1]
(Cell-free assay)
6 nM 15 nM 20 nM 22 nM 38 nM
In vitro

Sorafenib inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. Sorafenib inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. [1] In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sorafenib significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\kV3hPUUN3ME2wMlAxODByM{CzJO69VQ>? NU\4cWhZW0GQR1XS
MONO-MAC-6 M1rz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4G3NmlEPTB;MD6wNFQyQCEQvF2= M3;wWnNCVkeHUh?=
ALL-PO NIe4OHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTBwMEOxPFQh|ryP MmHyV2FPT0WU
NKM-1 MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPjNWZKSzVyPUCuNFc1OTZizszN NHn0U5hUSU6JRWK=
CGTH-W-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7hWXpxUUN3ME2wMlI2ODJ{IN88US=> MXXTRW5ITVJ?
BB65-RCC MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPyUGxKSzVyPUCuOFcxPzNizszN MUHTRW5ITVJ?
NOS-1 MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLmSoFKSzVyPUCuOVY{PiEQvF2= NYDlRWNGW0GQR1XS
SH-4 M2TZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwNkW2NVMh|ryP NHXnNIlUSU6JRWK=
HOP-62 NEjSNJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33zZWlEPTB;MD64OVA5QCEQvF2= MWTTRW5ITVJ?
HCC2998 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETIT25KSzVyPUCuPFg5OThizszN MVPTRW5ITVJ?
GDM-1 NFHjbZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTVO2NJUUN3ME2wMlkxPjl6IN88US=> MlH1V2FPT0WU
KM12 NHTQPGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrNSlY3UUN3ME2xMlAzODl6IN88US=> NX;je3JrW0GQR1XS
LB2518-MEL M2TkfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnpTWM2OD1zLkKwPFA6KM7:TR?= NX3vemhSW0GQR1XS
NCI-H1436 NEjzU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwMkG2O|gh|ryP MnrmV2FPT0WU
EM-2 M3HIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\aXHFKSzVyPUGuN|U2PzhizszN MlLWV2FPT0WU
LAMA-84 MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwM{e2OFgh|ryP NGfabGxUSU6JRWK=
KG-1 NF\s[JJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LIeGlEPTB;MT60O|k{PSEQvF2= Mm\XV2FPT0WU
A388 NULlOolHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfiXZFKSzVyPUGuOVkyPjVizszN M1TNU3NCVkeHUh?=
no-10 M3PIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml36TWM2OD1zLk[xO|I3KM7:TR?= NFjL[mJUSU6JRWK=
SF126 NWLIfGpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLTTpBnUUN3ME2xMlY{QDF{IN88US=> MULTRW5ITVJ?
MEG-01 NHLiOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DEOGlEPTB;MT64NFk5KM7:TR?= MWDTRW5ITVJ?
A3-KAW MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFwOEi0NkDPxE1? MoX2V2FPT0WU
D-247MG NH7TUnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PDV2lEPTB;Mj6xOFQ5KM7:TR?= MY\TRW5ITVJ?
OVCAR-4 NFLmOpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDHVItKSzVyPUKuNlE{QTNizszN M1;rWnNCVkeHUh?=
NCI-SNU-1 MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DpcWlEPTB;Mj6zNVYzKM7:TR?= MkD5V2FPT0WU
NCI-H2171 M37PSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PoOGlEPTB;Mj6zPVc3PCEQvF2= MU\TRW5ITVJ?
SIG-M5 MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPSUYxKSzVyPUKuOFIzPDJizszN NEP6W29USU6JRWK=
BE-13 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLrTWM2OD1{Lk[5OlA6KM7:TR?= NGnMO5dUSU6JRWK=
K052 NVHuR45QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHhOWxUUUN3ME2yMlc1PjF4IN88US=> M36yeHNCVkeHUh?=
L-540 NILjPHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:xWYxXUUN3ME2yMlc2Pzh7IN88US=> NIr2S49USU6JRWK=
KMOE-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\OTWM2OD1{LkixN|Uh|ryP M2HI[XNCVkeHUh?=
MFH-ino NWWxfItCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJwOUKxPFUh|ryP NVezUJpzW0GQR1XS
HL-60 M4W5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrQRnZiUUN3ME2zMlA3Ojl7IN88US=> NYLWRWkzW0GQR1XS
HCC2218 NF\KVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfRTWM2OD1|LkGyNFA{KM7:TR?= MWjTRW5ITVJ?
TE-5 NU\zXXZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXlTWM2OD1|LkGzNVYzKM7:TR?= NILjUHJUSU6JRWK=
MZ1-PC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fOU2lEPTB;Mz60O|UxQSEQvF2= NFTCSVlUSU6JRWK=
MRK-nu-1 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTNwNkG0Olgh|ryP NFLxNXhUSU6JRWK=
MZ7-mel MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[wTWM2OD1|Lk[2NFk6KM7:TR?= Ml7zV2FPT0WU
BC-1 NVK5OIR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK4b2Z[UUN3ME2zMlc1ODJizszN NUTkUWU1W0GQR1XS
ST486 MoDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4exZ2lEPTB;Mz64N|Y4OyEQvF2= MYHTRW5ITVJ?
KS-1 NIXC[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3uTWM2OD1|Lki4NVk5KM7:TR?= MnTwV2FPT0WU
SK-NEP-1 M3LVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO1TWM2OD12LkG2PFE2KM7:TR?= MVXTRW5ITVJ?
BC-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrrXo5KSzVyPUSuNlM{QTFizszN MoPhV2FPT0WU
NCI-H1581 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DJd2lEPTB;ND6yPFc6QCEQvF2= NXPMOXhuW0GQR1XS
MHH-PREB-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XHRWlEPTB;ND60NFQ5PCEQvF2= MkL6V2FPT0WU
NOMO-1 NImyOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrsS3JKSzVyPUSuOFg6ODVizszN M3nOTXNCVkeHUh?=
QIMR-WIL Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPpbItZUUN3ME21MlA4Ojl2IN88US=> MU\TRW5ITVJ?
SF539 NV;EVmFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjBOJNKSzVyPUWuNVMzOjdizszN MVzTRW5ITVJ?
TE-12 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2zb2pzUUN3ME21MlI1QTJ7IN88US=> NUTSTY92W0GQR1XS
NCI-H510A MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHGTWM2OD13LkSxOlg2KM7:TR?= MYTTRW5ITVJ?
JAR NEHMXHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPFTXhKSzVyPUWuOVA5OjRizszN MX;TRW5ITVJ?
no-11 NES0XlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTVwN{O1Olgh|ryP MmHOV2FPT0WU
BV-173 M4njPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXsXnNGUUN3ME21Mlk2Pjh{IN88US=> NEj4UVZUSU6JRWK=
SR NInVU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPoTWM2OD14LkCwOlc5KM7:TR?= NGHMfpBUSU6JRWK=
MOLT-16 M4\uUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXxTWM2OD14LkK1NlY3KM7:TR?= NIm5TFNUSU6JRWK=
MZ2-MEL NGDORnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vHTmlEPTB;Nj6zNVg{QSEQvF2= MnvVV2FPT0WU
SW954 NInUWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nPPWlEPTB;Nj60OVg3PiEQvF2= MXzTRW5ITVJ?
ML-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnUTWM2OD14LkWyPFQ6KM7:TR?= NFLWdWVUSU6JRWK=
OCI-AML2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPLTWM2OD14Lk[xNFYzKM7:TR?= MmntV2FPT0WU
SIMA NHK4TYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfEOpRyUUN3ME23MlAxOTBzIN88US=> MVXTRW5ITVJ?
DOHH-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPVTWM2OD15LkC1Olc3KM7:TR?= MV;TRW5ITVJ?
697 NG\UWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTdwMEW5PFkh|ryP NVHM[lFrW0GQR1XS
NB1 NEHLWG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLVO3dKSzVyPUeuOFA1ODdizszN MYjTRW5ITVJ?
D-392MG MnjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXacXJKSzVyPUeuOlI3PjNizszN MnHBV2FPT0WU
ES8 M2TE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnzWY1KSzVyPUeuO|Y2ODNizszN NF;oXJJUSU6JRWK=
RPMI-8226 NFryZolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTdwOES1NVEh|ryP Mly4V2FPT0WU
IST-MEL1 MlK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHETWM2OD16LkSwNFAzKM7:TR?= M33MPHNCVkeHUh?=
NB14 NV3vV|FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjqZYhKSzVyPUiuOlMyOzNizszN NFnjUJNUSU6JRWK=
HD-MY-Z NEW2OnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXXTWM2OD16Lk[zO|Q3KM7:TR?= NIrJcohUSU6JRWK=
TE-10 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DDV2lEPTB;OD63OlM2OyEQvF2= NEflNndUSU6JRWK=
LC-1F M3fLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljOTWM2OD17LkGwPFM1KM7:TR?= MlvNV2FPT0WU
OS-RC-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorRTWM2OD17LkGxNlQ{KM7:TR?= M4LiUHNCVkeHUh?=
NCI-SNU-16 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS2TWM2OD17LkKxNFI3KM7:TR?= MUHTRW5ITVJ?
SHP-77 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEH1XGVKSzVyPUmuO|E3PjJizszN NFPUS21USU6JRWK=
A4-Fuk MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TwfmlEPTB;OT63OVYyKM7:TR?= MVnTRW5ITVJ?
NB6 MlTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\UTWM2OD17Lke2NFI6KM7:TR?= M3nSV3NCVkeHUh?=
JiyoyeP-2003 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnISYtKSzVyPUGwMlQ4PDVizszN NYnWVZFKW0GQR1XS
DMS-114 M3ntSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XnPGlEPTB;MUCuOVQ1OSEQvF2= NUHTdYM4W0GQR1XS
NB7 M1jDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL1TWM2OD1zMD63OVI3KM7:TR?= MVXTRW5ITVJ?
NCI-H747 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq2SphKSzVyPUGxMlEzOTZizszN Mn[wV2FPT0WU
HH M{Dzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFzLkO4O|Yh|ryP MYfTRW5ITVJ?
EW-18 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFzLkmwOFQh|ryP M2[4fHNCVkeHUh?=
CHP-126 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFzLkm3N|gh|ryP MojSV2FPT0WU
NTERA-S-cl-D1 NVnBeHpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XBc2lEPTB;MUKuNFI4QCEQvF2= Ml7pV2FPT0WU
DEL M{XjU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrVXGpKSzVyPUGyMlA6QDVizszN NYnafY9FW0GQR1XS
LU-139 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYmzVY9rUUN3ME2xNk42PDF|IN88US=> M2PkWnNCVkeHUh?=
P30-OHK NInmT3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2La[GlEPTB;MUKuOVQ4QSEQvF2= MnjqV2FPT0WU
NCI-H1522 NFu4XZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXXc|VlUUN3ME2xNk44PDZizszN NVTZeWxSW0GQR1XS
NCI-H1299 NHf0S3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIj3OmhKSzVyPUGzMlI6OTFizszN MVXTRW5ITVJ?
UACC-257 NUfGNmd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjCTWM2OD1zMz61NVI3KM7:TR?= M4nscHNCVkeHUh?=
Calu-6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL3TWM2OD1zMz62NFQ3KM7:TR?= M1;3SXNCVkeHUh?=
NCI-H1882 Ml3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTF|Lki1OVUh|ryP M1\BXnNCVkeHUh?=
BB30-HNC NV2xdFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHDPXlKSzVyPUG0MlA3ODlizszN MUTTRW5ITVJ?
ES1 NGXyN5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF2LkG1OVEh|ryP NHLDXJZUSU6JRWK=
NCI-H1694 NVLoSXdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvUXm1sUUN3ME2xOE41QDFzIN88US=> MoDRV2FPT0WU
IST-SL1 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Tj[WlEPTB;MUSuPVYyPiEQvF2= MYPTRW5ITVJ?
ECC4 NU[5VVk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF3LkC1OVgh|ryP M3Pr[HNCVkeHUh?=
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Ramos-2G6-4C10 M3nxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvRTWM2OD1zNj6xNlk4KM7:TR?= NGn3dolUSU6JRWK=
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NCI-H2141 NV20NI81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPlTWM2OD1zNj6xPFkh|ryP NGnGb|ZUSU6JRWK=
LC4-1 MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF4Lk[xNVkh|ryP MljRV2FPT0WU
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C8166 MmnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTF5Lk[4N|Mh|ryP M3jTOXNCVkeHUh?=
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K-562 NVXaNIVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1joPGlEPTB;MUiuO|E1OyEQvF2= MVfTRW5ITVJ?
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LU-165 M{jYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Gyc2lEPTB;MUmuO|AxQCEQvF2= NVHQUoNLW0GQR1XS
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A101D MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T6SGlEPTB;MkGuN|c2OiEQvF2= MmLRV2FPT0WU
HUTU-80 NF3IdplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnPOIZxUUN3ME2yNU4{QTR4IN88US=> NUDNUXVkW0GQR1XS
NCI-H23 MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXje|dVUUN3ME2yNU4{QTl{IN88US=> M33OTHNCVkeHUh?=
PF-382 NGTKfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzzTWM2OD1{MT60OFA{KM7:TR?= NYHtZ5NQW0GQR1XS
LB373-MEL-D NIL2N3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJzLkW2NVUh|ryP MYHTRW5ITVJ?
TE-8 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz4N4ZXUUN3ME2yNU43Ozl2IN88US=> MmH4V2FPT0WU
TE-9 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJzLki1NVMh|ryP M1q4bHNCVkeHUh?=
Daudi Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIGydpdKSzVyPUKxMlk{ODRizszN NHixPVdUSU6JRWK=
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U-698-M M4W0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ{LkS2NFMh|ryP M3zk[XNCVkeHUh?=
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DU-4475 MmD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7MNVNrUUN3ME2yN{45QDl5IN88US=> M37RZ3NCVkeHUh?=
ECC12 NFPUTYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDoO49FUUN3ME2yOE4zQDB|IN88US=> MXHTRW5ITVJ?
C2BBe1 NHnBU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXZO|VNUUN3ME2yOE4{OjN7IN88US=> MoHFV2FPT0WU
IST-SL2 M2T3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T2fWlEPTB;MkSuOFM3OiEQvF2= MYnTRW5ITVJ?
DJM-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfrUI5vUUN3ME2yOE42OjJzIN88US=> MoTOV2FPT0WU
DMS-153 M3LHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvSWYRKSzVyPUK0Mlg3OTRizszN NED0S2pUSU6JRWK=
NB13 M4L5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T4ZmlEPTB;MkWuNFI3PSEQvF2= NHXCbGdUSU6JRWK=
SK-N-DZ Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\2PWlEPTB;Mk[uN|QyPCEQvF2= MoGxV2FPT0WU
COR-L88 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq2SlhKSzVyPUK2MlU4QTZizszN MUjTRW5ITVJ?
LU-65 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTuTWM2OD1{Nj64OVM2KM7:TR?= NYC5fo5PW0GQR1XS
TGBC1TKB NYniWYdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfTTWM2OD1{Nj65PFI5KM7:TR?= NYfJNVB[W0GQR1XS
THP-1 MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTDdGszUUN3ME2yO{4zOTRzIN88US=> NF3xbYlUSU6JRWK=
ONS-76 NYKyeYRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7TTWM2OD1{Nz6zN|Ih|ryP MmHBV2FPT0WU
LC-2-ad NHiwNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnVWJVHUUN3ME2yO{43OjNzIN88US=> NYLUZnlwW0GQR1XS
EW-13 NES5Um5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvvZ29KSzVyPUK5MlE4PDZizszN NFO2Om5USU6JRWK=
MS-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfsZ|hrUUN3ME2zNE44Ojd6IN88US=> NUPYO3pWW0GQR1XS
NCI-H2227 NXvpW3k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrvZ2pKSzVyPUOwMlk5ODZizszN Mkn0V2FPT0WU
LXF-289 M{e2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTNzLkS0PVIh|ryP MVjTRW5ITVJ?
MC116 NUW1OZM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\aTWM2OD1|Mj6wPFI3KM7:TR?= M1vMVnNCVkeHUh?=
EVSA-T MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3aTWM2OD1|Mj6yOVg2KM7:TR?= MVnTRW5ITVJ?
CTB-1 M3P4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofOTWM2OD1|Mz6xNVAyKM7:TR?= M3GxdXNCVkeHUh?=
COLO-320-HSR MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLwd2VQUUN3ME2zN{4yPjB|IN88US=> NV\TZlh2W0GQR1XS
NCI-H2196 M33uUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjsTWM2OD1|Mz6yOVU4KM7:TR?= M1q3bXNCVkeHUh?=
LB2241-RCC NIS1NndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDYTWM2OD1|Mz6zNVM2KM7:TR?= MUnTRW5ITVJ?
LS-513 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTN|Lki2N|gh|ryP MVzTRW5ITVJ?
LP-1 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonUTWM2OD1|Mz65PVU3KM7:TR?= MmDUV2FPT0WU
A253 M3jHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1iyfGlEPTB;M{SuNlI6PiEQvF2= MVLTRW5ITVJ?
SK-MM-2 NFrGboFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN2Lkm0OVEh|ryP MUjTRW5ITVJ?
NCI-H1963 NXrYRWpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHiTFNKSzVyPUO1MlMxPzJizszN MmL0V2FPT0WU
MMAC-SF NW\XdHpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHVO|J{UUN3ME2zOU45Pzh3IN88US=> MXfTRW5ITVJ?
LB831-BLC M3mwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG3NWdKSzVyPUO2MlA3PTRizszN NIHpR|RUSU6JRWK=
WSU-NHL NHzGNJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXwTWM2OD1|Nj6xOlQh|ryP NYPidpg3W0GQR1XS
CESS M2DINmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u3fWlEPTB;M{[uNlg1QCEQvF2= MkLoV2FPT0WU
NEC8 MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojkTWM2OD1|Nj61PFM2KM7:TR?= MUDTRW5ITVJ?
KNS-42 NHfjXHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN5LkGyN|ch|ryP M1\KWnNCVkeHUh?=
MHH-CALL-2 NHnuNYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGD1do5KSzVyPUO3MlE5OjFizszN NG\JRm1USU6JRWK=
K5 NVXnXVU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTN6LkSzJO69VQ>? MnXuV2FPT0WU
CP66-MEL M{fhdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN7LkC3N|Mh|ryP NIC0UppUSU6JRWK=
OPM-2 NUf2OY5uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXyNmpCUUN3ME2zPU45PDN{IN88US=> M2C4SXNCVkeHUh?=
IST-MES1 Mlz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTRyLkOwPVYh|ryP NW\wNGF{W0GQR1XS
EC-GI-10 NEOzOm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHiw[m9KSzVyPUSxMlU5ODVizszN M{\oXXNCVkeHUh?=
CTV-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR{Lki0NFYh|ryP NFvBPFJUSU6JRWK=
DG-75 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR|Lke1PVUh|ryP MULTRW5ITVJ?
KNS-81-FD M2fxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrUWm5XUUN3ME20OU41ODV6IN88US=> NXuwUoZpW0GQR1XS
NCI-H82 Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLr[Vh3UUN3ME20OU42PzV6IN88US=> NUPoSHB5W0GQR1XS
RPMI-8866 M2jGUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPVTWM2OD12Nj6xPFc{KM7:TR?= NVnGSpFyW0GQR1XS
ACN NEPOS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHldotkUUN3ME20Ok41OzRizszN MmP6V2FPT0WU
NCI-H1395 NG\kWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTR4LkS3OVYh|ryP MVXTRW5ITVJ?
NCI-H209 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoGyTWM2OD12Nz6xOFA2KM7:TR?= NUDYboRxW0GQR1XS
TGW MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nwZWlEPTB;NEmuNFc6OSEQvF2= NXeycFdiW0GQR1XS
NCI-H748 M4LMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Dtd2lEPTB;NEmuOFc2OyEQvF2= MVzTRW5ITVJ?
EKVX M4Lsd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu0OnA1UUN3ME20PU43PjJ6IN88US=> NFfEflRUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo Oral administration of Sorafenib (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, Sorafenib treatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. [1] Sorafenib treatment produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis. [2] Sorafenib sensitizes bax-/- cells to TRAIL in a dose-dependent manner, through a mechanism involving down-regulating NF-κB mediated Mcl-1 and cIAP2 expression. Combining Sorafenib (30-60 mg/kg) with TRAIL (5 mg/kg) show dramatic efficacy in TRAIL-resistant HCT116 bax-/- and HT29 tumor xenografts. [3]

Protocol

Kinase Assay
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Biochemical assays:

Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[33P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, Sorafenib tosylate is added before the enzyme initiation. A 50-fold stock plate is made with Sorafenib tosylate serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final Sorafenib tosylate concentrations range from 10 μM to 4.56 nM in 1% DMSO.
Cell Research
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  • Cell lines: MDA-MB-231, and HAoSMC
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to increasing concentrations of Sorafenib tosylate for 72 hours. Cell number is quantitated using the Cell TiterGlo ATP Luminescent assay kit. This assay measures the number of viable cells per well by measurement of luminescent signal based on amount of cellular ATP.


    (Only for Reference)
Animal Research
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  • Animal Models: Female NCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells
  • Formulation: Dissolved in Cremophor EL/ethanol (50:50) as 4-fold (4 × stock solution, and diluted to 1 × with water
  • Dosages: ~60 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (135.53 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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 464.82
Formula

C21H16ClF3N4O3

CAS No. 284461-73-0
Storage powder
in solvent
Synonyms BAY 43-9006

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / 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:

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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02834546 Not yet recruiting Hepatocellular Carcinoma (HCC) University Hospital, Bordeaux September 2016 --
NCT02836847 Recruiting Cholangiocarcinoma of the Extrahepatic Bile Duct|Gallbladder Cancer Shanghai Jiao Tong University School of Medicine|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Ruijin Hospital|RenJi Hospital|Eastern Hepatobiliary Surgery Hospital|Huashan Hospital July 2016 Phase 2
NCT02575339 Recruiting Hepatocellular Carcinoma|Liver Cancer|HCC Bert ONeil, MD|Hoosier Cancer Research Network|Millennium Pharmaceuticals, Inc.|Big Ten Cancer Research Consortium July 2016 Phase 1|Phase 2
NCT02747537 Not yet recruiting Pediatric Solid Tumors Washington University School of Medicine July 2016 Phase 2
NCT02774187 Recruiting Hepatocellular Carcinoma Sun Yat-sen University May 2016 Phase 3
NCT02616692 Recruiting Hepatocellular Cancer Bayer May 2016 --

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

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID