Sorafenib

製品コードS7397 別名:BAY 43-9006

Sorafenib化学構造

分子量(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.

サイズ 価格(税別)  
JPY 24402.00
JPY 44820.00
JPY 111220.00

文献中Selleckの製品使用例(71)

カスタマーフィードバック(12)

  • (A) and (C) qPCR showing the levels of HMGA2 and SOX9 mRNA in Hep3B and Huh7 human HCC cells treated for 48 hours with 1 μM AZD6244, or 7.5 μM sorafenib relative to control-treated cells (Ctrl). (B) and (D) qPCR showing Hmga2 and Sox9 expression in p53−/−; HRAS(G12V) and p53−/−; Myc; Cas9; sgNf1 mouse liver cells. Drug treatment was the same as in (A). Error bars are s.d. of mean (n = 3). ***, P < .001.

    Gastroenterology, 2017, 152(5):1161-1173. Sorafenib purchased from Selleck.

    E-G, Shown are H&E, Ki67, and Tunel-stained representative sections from a vehicle or OTX015+panobinostat+sorafenib-treated GBM12 tumor

    Clin Cancer Res, 2018, 24(16):3941-3954. Sorafenib purchased from Selleck.

  • Western blotting of Mcl-1 in HCT116 cells treated with indicated agents for 24 hours. ABT-263, 5 μmol/L; ABT-737, 5 μmol/L; SAHA, 4 μmol/L; MS-275, 5 μmol/L; regorafenib, 40 μmol/L; sorafenib, 20 μmol/L; UCN-01, 1 μmol/L; sunitinib, 15 μmol/L.

    Cancer Res, 2018, 78(16):4704-4715. 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.

  • 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.

  • 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.

    HCC cell-derived exosomes reverse sorafenib-induced apoptosis in hepatoma carcinoma cells in vivo. a Tumors from mice treated with PBS (Control), sorafenib (Sora), sorafenib + LO2-exosomes (Sora + LO2 exo), sorafenib + MHCC-97 L-exosomes (Sora + 97 L exo), and sorafenib + MHCC-97H-exosomes (Sora + 97H exo) were paraffin-embedded and sectioned, followed by staining of apoptotic cell by using TUNEL assays.

    J Exp Clin Cancer Res, 2016, 35(1):159. 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.

    (C) Western blotting revealed the expression levels of p-AKT, p-ERK1/2 and cleaved PARP in HUH-7 and R-HUH-7 HCC cell lines, these cell lines were treated with three different concentrations of sorafenib (0, 5, and 10 μM) for 24 h. (D) Western blotting revealed the expression levels of p-AKT, p-ERK1/2 and cleaved PARP in SK-HEP-1 and R-SK-HEP-1 HCC cell lines, these cell lines were treated with three different concentrations of sorafenib (0, 5, and 10 μM) for 24 h. (E) HUH-7 hepatoma cells treated with three different concentrations of sorafenib (0, 5, and 10 μM) for 24 h; proportions of apoptotic cells were calculated after cell cytotoxicity assay. (F) SK-HEP-1 hepatoma cells treated with three different concentrations of sorafenib (0, 5, and 10 μM) for 24 h; proportions of apoptotic cells were calculated after cell cytotoxicity assay. Data were expressed as mean ± standard deviation of each experiment in triplicate. (*P < 0.05, HUH-7, SK-HEP-1 are control groups, R-HUH-7, R-SK-HEP-1 are resistant groups).

    J Surg Res, 2016, 206(2):371-379. Sorafenib purchased from Selleck.

製品安全説明書

Raf阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 M{Sx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMECwNFA{ODNizszN MV;TRW5ITVJ?
MONO-MAC-6 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTWTWM2OD1yLkCwOFE5KM7:TR?= MYjTRW5ITVJ?
ALL-PO MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\GTWM2OD1yLkCzNVg1KM7:TR?= M1PlZ3NCVkeHUh?=
NKM-1 MnLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMEe0NVYh|ryP MoDtV2FPT0WU
CGTH-W-1 M1LOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HGRWlEPTB;MD6yOVAzOiEQvF2= MXvTRW5ITVJ?
BB65-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPaNWhKSzVyPUCuOFcxPzNizszN NWfKfoxmW0GQR1XS
NOS-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK5bXF6UUN3ME2wMlU3OzZizszN M3XDT3NCVkeHUh?=
SH-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzTXXpKSzVyPUCuOlU3OTNizszN MnTSV2FPT0WU
HOP-62 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL0TWM2OD1yLki1NFg5KM7:TR?= Mn;sV2FPT0WU
HCC2998 NHu0WnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH0[WZKSzVyPUCuPFg5OThizszN NX3uW29DW0GQR1XS
GDM-1 NUPNS41CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwOUC2PVgh|ryP NGnJS3lUSU6JRWK=
KM12 NHXtNVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFm2WXhKSzVyPUGuNFIxQThizszN MXvTRW5ITVJ?
LB2518-MEL M1LITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe5V2dJUUN3ME2xMlIxQDB7IN88US=> M3XSO3NCVkeHUh?=
NCI-H1436 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr4bGNHUUN3ME2xMlIyPjd6IN88US=> M4Tw[nNCVkeHUh?=
EM-2 M{\2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\4fYp7UUN3ME2xMlM2PTd6IN88US=> M1X4eXNCVkeHUh?=
LAMA-84 Mon1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnzU4ZKSzVyPUGuN|c3PDhizszN MnftV2FPT0WU
KG-1 NHq0bW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\KTWM2OD1zLkS3PVM2KM7:TR?= MoPCV2FPT0WU
A388 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7jeHRKSzVyPUGuOVkyPjVizszN NYPNOZdCW0GQR1XS
no-10 MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVS2S5hxUUN3ME2xMlYyPzJ4IN88US=> M4r3bXNCVkeHUh?=
SF126 M3TjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDwTWM2OD1zLk[zPFEzKM7:TR?= NFPnTIpUSU6JRWK=
MEG-01 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv1TWM2OD1zLkiwPVgh|ryP M2HrW3NCVkeHUh?=
A3-KAW M4rx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4q3NGlEPTB;MT64PFQzKM7:TR?= MmiwV2FPT0WU
D-247MG MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLpS2oxUUN3ME2yMlE1PDhizszN NIO0W4lUSU6JRWK=
OVCAR-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TTWWlEPTB;Mj6yNVM6OyEQvF2= NWHVOoZIW0GQR1XS
NCI-SNU-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojGTWM2OD1{LkOxOlIh|ryP M4j1OHNCVkeHUh?=
NCI-H2171 NGLjZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvGTWM2OD1{LkO5O|Y1KM7:TR?= MoLGV2FPT0WU
SIG-M5 NVTIS|V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxPGdKSzVyPUKuOFIzPDJizszN NF3pUoZUSU6JRWK=
BE-13 NULVVVZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJwNkm2NFkh|ryP NGrQdWtUSU6JRWK=
K052 NFXhe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjLV3lrUUN3ME2yMlc1PjF4IN88US=> NXvh[ZpjW0GQR1XS
L-540 M37YTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwN{W3PFkh|ryP M1P1dHNCVkeHUh?=
KMOE-2 NYjqWIZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17DVWlEPTB;Mj64NVM2KM7:TR?= M33xOHNCVkeHUh?=
MFH-ino NVrmfVlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W4dmlEPTB;Mj65NlE5PSEQvF2= NHL3W3ZUSU6JRWK=
HL-60 M4HQRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTSTWM2OD1|LkC2Nlk6KM7:TR?= MUXTRW5ITVJ?
HCC2218 NXS0fW0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLqTWM2OD1|LkGyNFA{KM7:TR?= M3HkU3NCVkeHUh?=
TE-5 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPPOndKSzVyPUOuNVMyPjJizszN MoLSV2FPT0WU
MZ1-PC NFHxdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLTTWM2OD1|LkS3OVA6KM7:TR?= MUTTRW5ITVJ?
MRK-nu-1 MlTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTNwNkG0Olgh|ryP MWnTRW5ITVJ?
MZ7-mel NX72V2JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DRR2lEPTB;Mz62OlA6QSEQvF2= NIiwWmlUSU6JRWK=
BC-1 M37ze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS2PW8{UUN3ME2zMlc1ODJizszN NWDCWG4{W0GQR1XS
ST486 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn71TWM2OD1|LkizOlc{KM7:TR?= NGjqWItUSU6JRWK=
KS-1 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\L[2JKSzVyPUOuPFgyQThizszN NFTlS2pUSU6JRWK=
SK-NEP-1 M2HhXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTRwMU[4NVUh|ryP MUfTRW5ITVJ?
BC-3 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzhcFFKSzVyPUSuNlM{QTFizszN MmrMV2FPT0WU
NCI-H1581 M2\3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwMki3PVgh|ryP MWnTRW5ITVJ?
MHH-PREB-1 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljBTWM2OD12LkSwOFg1KM7:TR?= M37RNHNCVkeHUh?=
NOMO-1 NWTVT2F{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTRwNEi5NFUh|ryP NV32ZnduW0GQR1XS
QIMR-WIL M3ux[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPYTWM2OD13LkC3Nlk1KM7:TR?= M1n3NHNCVkeHUh?=
SF539 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rKdWlEPTB;NT6xN|IzPyEQvF2= NXTtNY45W0GQR1XS
TE-12 NYnQfGJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfEd5NKSzVyPUWuNlQ6OjlizszN M2LOUHNCVkeHUh?=
NCI-H510A NIruVnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLYPYtKSzVyPUWuOFE3QDVizszN NX;PUoo5W0GQR1XS
JAR NWm4fVRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXBfGRKSzVyPUWuOVA5OjRizszN NV\TV3V3W0GQR1XS
no-11 MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf6eG9KSzVyPUWuO|M2PjhizszN M3q1Z3NCVkeHUh?=
BV-173 NET2Z2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrYTWM2OD13Lkm1OlgzKM7:TR?= M1TlV3NCVkeHUh?=
SR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jTcWlEPTB;Nj6wNFY4QCEQvF2= NH\iWIFUSU6JRWK=
MOLT-16 NIrkSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjSdHZKSzVyPU[uNlUzPjZizszN MXfTRW5ITVJ?
MZ2-MEL NHHsUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjERml[UUN3ME22MlMyQDN7IN88US=> MkXIV2FPT0WU
SW954 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPuTWM2OD14LkS1PFY3KM7:TR?= NXmyNHVQW0GQR1XS
ML-2 NWH1W2pDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnuyTWM2OD14LkWyPFQ6KM7:TR?= NUnLfVRiW0GQR1XS
OCI-AML2 MnPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK0TWM2OD14Lk[xNFYzKM7:TR?= M{nNRnNCVkeHUh?=
SIMA NEG0RZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzPZohZUUN3ME23MlAxOTBzIN88US=> Ml6wV2FPT0WU
DOHH-2 M1fEd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL4RYtKSzVyPUeuNFU3PzZizszN MlrMV2FPT0WU
697 NFiyfYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;BbGlEPTB;Nz6wOVk5QSEQvF2= NHLiNY9USU6JRWK=
NB1 MofmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGmzfmlKSzVyPUeuOFA1ODdizszN MWHTRW5ITVJ?
D-392MG M{DIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17vSGlEPTB;Nz62NlY3OyEQvF2= NFvVdVlUSU6JRWK=
ES8 NWfLe5dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfXeGJwUUN3ME23Mlc3PTB|IN88US=> MWrTRW5ITVJ?
RPMI-8226 Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\pWXZKSzVyPUeuPFQ2OTFizszN NYnNV4dqW0GQR1XS
IST-MEL1 M33FTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zoUWlEPTB;OD60NFAxOiEQvF2= NH[3b2FUSU6JRWK=
NB14 NYXFe3dXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHQemJKSzVyPUiuOlMyOzNizszN MmK4V2FPT0WU
HD-MY-Z NHu1cmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf2UIVKSzVyPUiuOlM4PDZizszN NUXVSJFRW0GQR1XS
TE-10 M1ewdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HGcWlEPTB;OD63OlM2OyEQvF2= MoPzV2FPT0WU
LC-1F MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfKTWM2OD17LkGwPFM1KM7:TR?= MofWV2FPT0WU
OS-RC-2 NIfLVmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\RVGlEPTB;OT6xNVI1OyEQvF2= NWHzd2tiW0GQR1XS
NCI-SNU-16 MlH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTlwMkGwNlYh|ryP MWTTRW5ITVJ?
SHP-77 NVzpVJIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHCTWM2OD17LkexOlYzKM7:TR?= NUDiPGxiW0GQR1XS
A4-Fuk MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTlwN{W2NUDPxE1? MlXYV2FPT0WU
NB6 NE\afFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfSU3hKSzVyPUmuO|YxOjlizszN MXvTRW5ITVJ?
JiyoyeP-2003 NHfBUFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PURWlEPTB;MUCuOFc1PSEQvF2= NEfIUHVUSU6JRWK=
DMS-114 NFTWcXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFyLkW0OFEh|ryP MkPEV2FPT0WU
NB7 NIfFcHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHlbXJsUUN3ME2xNE44PTJ4IN88US=> M1n2cXNCVkeHUh?=
NCI-H747 NX:4[49PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfETWM2OD1zMT6xNlE3KM7:TR?= NEjzUZZUSU6JRWK=
HH M1uzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TQSGlEPTB;MUGuN|g4PiEQvF2= MlXEV2FPT0WU
EW-18 NVTUToU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj0dGpKSzVyPUGxMlkxPDRizszN MVjTRW5ITVJ?
CHP-126 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFzLkm3N|gh|ryP M{nodXNCVkeHUh?=
NTERA-S-cl-D1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfLWGl1UUN3ME2xNk4xOjd6IN88US=> NEXYfZFUSU6JRWK=
DEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL1TWM2OD1zMj6wPVg2KM7:TR?= MoTPV2FPT0WU
LU-139 M4XtZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvUVXRbUUN3ME2xNk42PDF|IN88US=> NI\ySWdUSU6JRWK=
P30-OHK NH;5eXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrYSVJxUUN3ME2xNk42PDd7IN88US=> NUK4RpJPW0GQR1XS
NCI-H1522 M4S5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLaTWM2OD1zMj63OFYh|ryP NH\WR2hUSU6JRWK=
NCI-H1299 NYriWZpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmxTWM2OD1zMz6yPVEyKM7:TR?= M2PCdXNCVkeHUh?=
UACC-257 NWfMfVVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnwTWM2OD1zMz61NVI3KM7:TR?= NWS4[nd4W0GQR1XS
Calu-6 M2HOTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37JTmlEPTB;MUOuOlA1PiEQvF2= NXf5fndkW0GQR1XS
NCI-H1882 NWrPWGlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojSTWM2OD1zMz64OVU2KM7:TR?= MlezV2FPT0WU
BB30-HNC NYHLN3BuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXXTWM2OD1zND6wOlA6KM7:TR?= MlP2V2FPT0WU
ES1 NY\oRoplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXUTWM2OD1zND6xOVUyKM7:TR?= MlXnV2FPT0WU
NCI-H1694 M{D0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF2LkS4NVEh|ryP Mm\KV2FPT0WU
IST-SL1 NEG3N5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF2Lkm2NVYh|ryP NFe1fFJUSU6JRWK=
ECC4 NFP1bFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHHdFRYUUN3ME2xOU4xPTV6IN88US=> MV;TRW5ITVJ?
MDA-MB-134-VI NXm1UYdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\MSm9SUUN3ME2xOU41OTNzIN88US=> NH7CRo1USU6JRWK=
SCH NYnh[XNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXVVnhKSzVyPUG1MlQ4OjhizszN NH2yT45USU6JRWK=
SK-N-FI NWDzcFd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDQU|NKSzVyPUG1MlY2OzRizszN MXXTRW5ITVJ?
HDLM-2 NGDKPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly0TWM2OD1zNj6wO|E1KM7:TR?= NVnjcnR6W0GQR1XS
Ramos-2G6-4C10 MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXxTWM2OD1zNj6xNlk4KM7:TR?= NFzJT2FUSU6JRWK=
EW-24 NHqxUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[3TWM2OD1zNj6xOlYyKM7:TR?= NFjVXHFUSU6JRWK=
NCI-H2141 M1HXOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNeGlEPTB;MU[uNVg6KM7:TR?= NULYVm4zW0GQR1XS
LC4-1 M1jGNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLPcJVKSzVyPUG2MlYyOTlizszN NWDMVJJQW0GQR1XS
HT-144 M13QU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\vTWM2OD1zNz6wNFYh|ryP MkTZV2FPT0WU
SK-MEL-1 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnjc25jUUN3ME2xO{4xODd{IN88US=> M4TCeHNCVkeHUh?=
SCC-15 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHFdINHUUN3ME2xO{4yPjN6IN88US=> Mlr4V2FPT0WU
C8166 MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvGTWM2OD1zNz62PFM{KM7:TR?= MnvhV2FPT0WU
GOTO NIDmfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTF5LkizOFQh|ryP Mn7kV2FPT0WU
COR-L279 NI\LcWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPYd|BQUUN3ME2xPE4yOzZ{IN88US=> NFK0PHVUSU6JRWK=
K-562 NV;oVGVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7vTWM2OD1zOD63NVQ{KM7:TR?= Ml;wV2FPT0WU
ES3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF6LkiwOFEh|ryP MYjTRW5ITVJ?
LU-165 M2jIZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r3UWlEPTB;MUmuO|AxQCEQvF2= NIrCUoxUSU6JRWK=
KM-H2 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHRXI5KSzVyPUKwMlMyQDRizszN M2L3[HNCVkeHUh?=
RL M4nxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPNSHVKSzVyPUKwMlk3QTJizszN M4\UOHNCVkeHUh?=
EW-3 M3HYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fP[WlEPTB;MkGuNVg5QSEQvF2= NEfCNVRUSU6JRWK=
A101D M4nxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJzLkO3OVIh|ryP MXTTRW5ITVJ?
HUTU-80 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jhVWlEPTB;MkGuN|k1PiEQvF2= NYS2ZYk4W0GQR1XS
NCI-H23 M1\kRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX2b5pKUUN3ME2yNU4{QTl{IN88US=> M3;WWXNCVkeHUh?=
PF-382 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjmRlhKSzVyPUKxMlQ1ODNizszN NYT4bIx3W0GQR1XS
LB373-MEL-D NXPFWFdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXiyc2o1UUN3ME2yNU42PjF3IN88US=> NWnJeGhqW0GQR1XS
TE-8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\6PHlKSzVyPUKxMlY{QTRizszN NIDoWYdUSU6JRWK=
TE-9 NHzmSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjaTWM2OD1{MT64OVE{KM7:TR?= Moe4V2FPT0WU
Daudi NYnDZ255T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nhXmlEPTB;MkGuPVMxPCEQvF2= MXXTRW5ITVJ?
D-542MG M4rw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHSb5NnUUN3ME2yNk4xOjV4IN88US=> MXnTRW5ITVJ?
U-698-M MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjoSIJTUUN3ME2yNk41PjB|IN88US=> M3;VXXNCVkeHUh?=
ES6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJ{LkezOlYh|ryP M2\TNXNCVkeHUh?=
DU-4475 MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHofVU6UUN3ME2yN{45QDl5IN88US=> NVWzbmc{W0GQR1XS
ECC12 NHfXcphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJ2LkK4NFMh|ryP MYrTRW5ITVJ?
C2BBe1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPDTWM2OD1{ND6zNlM6KM7:TR?= MljwV2FPT0WU
IST-SL2 NFvkc5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTnTWM2OD1{ND60N|YzKM7:TR?= MXnTRW5ITVJ?
DJM-1 NHOye4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ2LkWyNlEh|ryP M1LpdXNCVkeHUh?=
DMS-153 NIK2NVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PiXmlEPTB;MkSuPFYyPCEQvF2= M2\EfnNCVkeHUh?=
NB13 MlzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJ3LkCyOlUh|ryP NGrJNnRUSU6JRWK=
SK-N-DZ MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PpOGlEPTB;Mk[uN|QyPCEQvF2= M3TUeXNCVkeHUh?=
COR-L88 NWjHNGlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXkWVdRUUN3ME2yOk42Pzl4IN88US=> MX7TRW5ITVJ?
LU-65 NVXPZnZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof5TWM2OD1{Nj64OVM2KM7:TR?= NH3uNGlUSU6JRWK=
TGBC1TKB MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37afmlEPTB;Mk[uPVgzQCEQvF2= MnPpV2FPT0WU
THP-1 MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLqWHdKSzVyPUK3MlIyPDFizszN MX7TRW5ITVJ?
ONS-76 NHv6WmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjYe4hKSzVyPUK3MlM{OiEQvF2= MUTTRW5ITVJ?
LC-2-ad MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTaTWM2OD1{Nz62NlMyKM7:TR?= NHr0ZW9USU6JRWK=
EW-13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD1TnI3UUN3ME2yPU4yPzR4IN88US=> Ml7EV2FPT0WU
MS-1 NW\BPZE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHYbHp[UUN3ME2zNE44Ojd6IN88US=> Ml;qV2FPT0WU
NCI-H2227 M3HCb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HoUWlEPTB;M{CuPVgxPiEQvF2= NV:5W28{W0GQR1XS
LXF-289 M1nMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTNzLkS0PVIh|ryP MmHaV2FPT0WU
MC116 M3GxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\IXnlKSzVyPUOyMlA5OjZizszN MUnTRW5ITVJ?
EVSA-T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN{LkK1PFUh|ryP NX3lRVE5W0GQR1XS
CTB-1 NGrRfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN|LkGxNFEh|ryP NWL1b2I4W0GQR1XS
COLO-320-HSR NUXqZ3I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPaNlhxUUN3ME2zN{4yPjB|IN88US=> NWjWW3lqW0GQR1XS
NCI-H2196 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTN|LkK1OVch|ryP MWfTRW5ITVJ?
LB2241-RCC M363Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T5UmlEPTB;M{OuN|E{PSEQvF2= M{jWb3NCVkeHUh?=
LS-513 M{e3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT6cohEUUN3ME2zN{45PjN6IN88US=> M1K1S3NCVkeHUh?=
LP-1 MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnP[HJKSzVyPUOzMlk6PTZizszN NGjBTGxUSU6JRWK=
A253 MmH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTxSVQ6UUN3ME2zOE4zOjl4IN88US=> NV7ZfoxNW0GQR1XS
SK-MM-2 M2H3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\zRVVCUUN3ME2zOE46PDVzIN88US=> M1fZOXNCVkeHUh?=
NCI-H1963 NUT5PZd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H1XmlEPTB;M{WuN|A4OiEQvF2= MWLTRW5ITVJ?
MMAC-SF NWj2e21tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTN3Lki3PFUh|ryP NWD0W5B2W0GQR1XS
LB831-BLC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjyfnF7UUN3ME2zOk4xPjV2IN88US=> MmLuV2FPT0WU
WSU-NHL NFHidmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LjVGlEPTB;M{[uNVY1KM7:TR?= Mm\JV2FPT0WU
CESS NUfRVmx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN4LkK4OFgh|ryP NXnVfINvW0GQR1XS
NEC8 MkPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTN4LkW4N|Uh|ryP NIPyUnJUSU6JRWK=
KNS-42 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTN5LkGyN|ch|ryP NGDWN5ZUSU6JRWK=
MHH-CALL-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjnVGZKSzVyPUO3MlE5OjFizszN NF3TdoNUSU6JRWK=
K5 M{HERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu4ZW5KSzVyPUO4MlQ{KM7:TR?= MVfTRW5ITVJ?
CP66-MEL NUPjOWlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnhTnhKSzVyPUO5MlA4OzNizszN MVrTRW5ITVJ?
OPM-2 M{K1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu3TWM2OD1|OT64OFMzKM7:TR?= NHj3NXhUSU6JRWK=
IST-MES1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn22TWM2OD12MD6zNFk3KM7:TR?= NV7WXJd7W0GQR1XS
EC-GI-10 NF7NOGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTRzLkW4NFUh|ryP MlewV2FPT0WU
CTV-1 NWnRO5Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX3TnBCUUN3ME20Nk45PDB4IN88US=> MXzTRW5ITVJ?
DG-75 NYrSU3NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\n[WlEPTB;NEOuO|U6PSEQvF2= NFfDVYJUSU6JRWK=
KNS-81-FD MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTR3LkSwOVgh|ryP Ml[yV2FPT0WU
NCI-H82 MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TOemlEPTB;NEWuOVc2QCEQvF2= M1:zPXNCVkeHUh?=
RPMI-8866 NH\hcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR4LkG4O|Mh|ryP M{\ub3NCVkeHUh?=
ACN M3v0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGny[|hKSzVyPUS2MlQ{PCEQvF2= NF3Be5BUSU6JRWK=
NCI-H1395 NXq3[4l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3rZWNKSzVyPUS2MlQ4PTZizszN M33zUnNCVkeHUh?=
NCI-H209 NUT2fpJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe5SHlKSzVyPUS3MlE1ODVizszN NY\JR4pvW0GQR1XS
TGW NGK1UI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33LemlEPTB;NEmuNFc6OSEQvF2= NUfwO4VXW0GQR1XS
NCI-H748 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\y[GlEPTB;NEmuOFc2OyEQvF2= MYXTRW5ITVJ?
EKVX MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR7Lk[2Nlgh|ryP MVzTRW5ITVJ?

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 細胞株: MDA-MB-231, and HAoSMC
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 72 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Female NCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells
  • 製剤: Dissolved in Cremophor EL/ethanol (50:50) as 4-fold (4 × stock solution, and diluted to 1 × with water
  • 投薬量: ~60 mg/kg
  • 投与方法: Orally once daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 63 mg/mL (135.53 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+45% PEG 400+ddH2O
混合させたのち直ちに使用することを推奨します。
3mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 464.82
化学式

C21H16ClF3N4O3

CAS No. 284461-73-0
保管
in solvent
別名 BAY 43-9006

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03730675 Not yet recruiting Hepatocellular Carcinoma|Portal Vein Tumor Thrombosis Zhongda Hospital November 2018 Not Applicable
NCT03645980 Recruiting Hepatocellular Carcinoma Johannes Gutenberg University Mainz|Leap Therapeutics Inc. October 10 2018 Phase 1|Phase 2
NCT03644511 Not yet recruiting Hepatocellular Carcinoma Bayer October 30 2018 --
NCT03606590 Recruiting Hepatocellular Carcinoma NovoCure Ltd. September 2018 Phase 2
NCT03630120 Recruiting Thyroid Cancer|Thyroid Cancer Medullary|Differentiated Thyroid Cancer|Papillary Thyroid Cancer|Follicular Thyroid Cancer|Poorly Differentiated Thyroid Gland Carcinoma H. Lee Moffitt Cancer Center and Research Institute August 6 2018 Phase 2
NCT03582618 Recruiting Hepatocellular Carcinoma|Advanced Cancer TaiRx Inc. July 12 2018 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

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