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

文献中の使用例(62)

カスタマーフィードバック(9)

  • 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.

  • 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 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHFTWM2OD1yLkCwNFAxOzB|IN88US=> NGG1[oVUSU6JRWK=
MONO-MAC-6 M{nXNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O1NGlEPTB;MD6wNFQyQCEQvF2= MXLTRW5ITVJ?
ALL-PO NEXpd5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwMEOxPFQh|ryP MXXTRW5ITVJ?
NKM-1 M{XKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMEe0NVYh|ryP MmPhV2FPT0WU
CGTH-W-1 MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwMkWwNlIh|ryP NYLLNGV{W0GQR1XS
BB65-RCC NHHEVXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DqSmlEPTB;MD60O|A4OyEQvF2= NULEU5VCW0GQR1XS
NOS-1 NUPaUoNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2POdmlEPTB;MD61OlM3KM7:TR?= M1fSV3NCVkeHUh?=
SH-4 M4LrdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXBbIpYUUN3ME2wMlY2PjF|IN88US=> NX\SOJpiW0GQR1XS
HOP-62 M2\keWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XSc2lEPTB;MD64OVA5QCEQvF2= NHXhVFdUSU6JRWK=
HCC2998 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwOEi4NVgh|ryP M1O2W3NCVkeHUh?=
GDM-1 NGT4NoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\tR3FHUUN3ME2wMlkxPjl6IN88US=> M4G2[HNCVkeHUh?=
KM12 NUDF[4VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXMRZp2UUN3ME2xMlAzODl6IN88US=> NIHLV2dUSU6JRWK=
LB2518-MEL M3KzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPCW3N5UUN3ME2xMlIxQDB7IN88US=> M2rtW3NCVkeHUh?=
NCI-H1436 NGe2WmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2W0O2lEPTB;MT6yNVY4QCEQvF2= M3e5[HNCVkeHUh?=
EM-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO1d5kzUUN3ME2xMlM2PTd6IN88US=> NYfJSHVUW0GQR1XS
LAMA-84 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLVTWM2OD1zLkO3OlQ5KM7:TR?= NIjyUGFUSU6JRWK=
KG-1 NYHTVmkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInwSIlKSzVyPUGuOFc6OzVizszN NV\2NYJ[W0GQR1XS
A388 NVXuOG9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNUmxOlUh|ryP MUnTRW5ITVJ?
no-10 MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfsPFhiUUN3ME2xMlYyPzJ4IN88US=> MkHxV2FPT0WU
SF126 NFjPUIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\lTWM2OD1zLk[zPFEzKM7:TR?= MY\TRW5ITVJ?
MEG-01 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\2PZFyUUN3ME2xMlgxQThizszN Mmj0V2FPT0WU
A3-KAW MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXq2RVY2UUN3ME2xMlg5PDJizszN MWTTRW5ITVJ?
D-247MG M3j6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnPN4FKSzVyPUKuNVQ1QCEQvF2= MY\TRW5ITVJ?
OVCAR-4 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XF[mlEPTB;Mj6yNVM6OyEQvF2= MkjvV2FPT0WU
NCI-SNU-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\UeHRKSzVyPUKuN|E3OiEQvF2= NV:2XZhyW0GQR1XS
NCI-H2171 M2rDfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq2VVlKSzVyPUKuN|k4PjRizszN NHnWRnVUSU6JRWK=
SIG-M5 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nHe2lEPTB;Mj60NlI1OiEQvF2= NF;wNoRUSU6JRWK=
BE-13 M1nsWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFf6XoFKSzVyPUKuOlk3ODlizszN MlW5V2FPT0WU
K052 NUPTOnZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrTbVNsUUN3ME2yMlc1PjF4IN88US=> NIfSU2FUSU6JRWK=
L-540 NVvjRWlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwN{W3PFkh|ryP NWKxNYNMW0GQR1XS
KMOE-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyxTWM2OD1{LkixN|Uh|ryP NInlTpZUSU6JRWK=
MFH-ino MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJwOUKxPFUh|ryP MXfTRW5ITVJ?
HL-60 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK0TWM2OD1|LkC2Nlk6KM7:TR?= M3X4NnNCVkeHUh?=
HCC2218 M1Ts[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T6emlEPTB;Mz6xNlAxOyEQvF2= NHvCe2FUSU6JRWK=
TE-5 NIXv[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNwMUOxOlIh|ryP NVjXR2tSW0GQR1XS
MZ1-PC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LKZmlEPTB;Mz60O|UxQSEQvF2= MX\TRW5ITVJ?
MRK-nu-1 NXP3S5JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHqTWM2OD1|Lk[xOFY5KM7:TR?= NVzoO|VXW0GQR1XS
MZ7-mel Ml\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LXemlEPTB;Mz62OlA6QSEQvF2= M{HGU3NCVkeHUh?=
BC-1 NV3ZV3B1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTNwN{SwNkDPxE1? M1nVWXNCVkeHUh?=
ST486 NVzR[4VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33NPWlEPTB;Mz64N|Y4OyEQvF2= MoP5V2FPT0WU
KS-1 NYCwW5BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCwV|c3UUN3ME2zMlg5OTl6IN88US=> NHGye45USU6JRWK=
SK-NEP-1 M1LkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTRwMU[4NVUh|ryP M3nLfXNCVkeHUh?=
BC-3 MknWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PTbGlEPTB;ND6yN|M6OSEQvF2= M{\OWXNCVkeHUh?=
NCI-H1581 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW0TWM2OD12LkK4O|k5KM7:TR?= NH7zUmRUSU6JRWK=
MHH-PREB-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTRwNEC0PFQh|ryP NHjkPIlUSU6JRWK=
NOMO-1 M1XLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoCyTWM2OD12LkS4PVA2KM7:TR?= MWLTRW5ITVJ?
QIMR-WIL MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTGTWM2OD13LkC3Nlk1KM7:TR?= M1\WVXNCVkeHUh?=
SF539 NHjETIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTVwMUOyNlch|ryP M{L6THNCVkeHUh?=
TE-12 NU[welBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnaWHg{UUN3ME21MlI1QTJ7IN88US=> MnHKV2FPT0WU
NCI-H510A MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTVwNEG2PFUh|ryP NVnmPYpkW0GQR1XS
JAR NHv6WWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvW[oczUUN3ME21MlUxQDJ2IN88US=> MUjTRW5ITVJ?
no-11 M2fCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPZSVdYUUN3ME21Mlc{PTZ6IN88US=> NG\HR2pUSU6JRWK=
BV-173 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX1TWM2OD13Lkm1OlgzKM7:TR?= MUPTRW5ITVJ?
SR NXTlRZdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjnclhQUUN3ME22MlAxPjd6IN88US=> NYrVPGFNW0GQR1XS
MOLT-16 NX\5copTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDFTYF3UUN3ME22MlI2OjZ4IN88US=> M1jES3NCVkeHUh?=
MZ2-MEL NIDjNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DBUmlEPTB;Nj6zNVg{QSEQvF2= MorBV2FPT0WU
SW954 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\SUZBKSzVyPU[uOFU5PjZizszN M1jTTnNCVkeHUh?=
ML-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OzUWlEPTB;Nj61Nlg1QSEQvF2= NYXSW255W0GQR1XS
OCI-AML2 M{[zNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXETWM2OD14Lk[xNFYzKM7:TR?= M3mzdXNCVkeHUh?=
SIMA M1zEcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHkS2tKSzVyPUeuNFAyODFizszN Mn7EV2FPT0WU
DOHH-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTdwMEW2O|Yh|ryP NYXC[W9GW0GQR1XS
697 NIXmNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPzfYhKSzVyPUeuNFU6QDlizszN MYrTRW5ITVJ?
NB1 NVjwW|ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M374WGlEPTB;Nz60NFQxPyEQvF2= NHPhPXhUSU6JRWK=
D-392MG MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW2TWM2OD15Lk[yOlY{KM7:TR?= Moi4V2FPT0WU
ES8 M1nUV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW0TWM2OD15Lke2OVA{KM7:TR?= MmjjV2FPT0WU
RPMI-8226 NUjmWmtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP2TWM2OD15Lki0OVEyKM7:TR?= NUCx[JZ[W0GQR1XS
IST-MEL1 NFjQWJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRThwNECwNFIh|ryP Mkn6V2FPT0WU
NB14 NF3vTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRThwNkOxN|Mh|ryP M{\uZXNCVkeHUh?=
HD-MY-Z MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW3fVh7UUN3ME24MlY{PzR4IN88US=> M3nwOnNCVkeHUh?=
TE-10 M3jSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G1dGlEPTB;OD63OlM2OyEQvF2= M1vH[nNCVkeHUh?=
LC-1F M2\oWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm0fJJKSzVyPUmuNVA5OzRizszN MVvTRW5ITVJ?
OS-RC-2 NFH5dohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTlwMUGyOFMh|ryP MoHMV2FPT0WU
NCI-SNU-16 NF\DcJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrPTWM2OD17LkKxNFI3KM7:TR?= MYTTRW5ITVJ?
SHP-77 NH7CUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvBTWM2OD17LkexOlYzKM7:TR?= M2nJcnNCVkeHUh?=
A4-Fuk NF33b2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTITWM2OD17Lke1OlEh|ryP NGDrdYRUSU6JRWK=
NB6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTlwN{[wNlkh|ryP NEDDc5hUSU6JRWK=
JiyoyeP-2003 M1;PWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfI[VBKSzVyPUGwMlQ4PDVizszN M4TvVnNCVkeHUh?=
DMS-114 NUX6[HB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzNNpJlUUN3ME2xNE42PDRzIN88US=> NYjWZ3J3W0GQR1XS
NB7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfiTWM2OD1zMD63OVI3KM7:TR?= NID5fpZUSU6JRWK=
NCI-H747 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXRTWM2OD1zMT6xNlE3KM7:TR?= NUjPdGYyW0GQR1XS
HH MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETxSnRKSzVyPUGxMlM5PzZizszN MlP4V2FPT0WU
EW-18 M2K1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTzc5dIUUN3ME2xNU46ODR2IN88US=> NY\wVGhTW0GQR1XS
CHP-126 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XJcWlEPTB;MUGuPVc{QCEQvF2= NYn2UlBJW0GQR1XS
NTERA-S-cl-D1 MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnhTWM2OD1zMj6wNlc5KM7:TR?= NIHh[IFUSU6JRWK=
DEL NUDHNIJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:5TWM2OD1zMj6wPVg2KM7:TR?= NEHEd5pUSU6JRWK=
LU-139 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIKwVmtKSzVyPUGyMlU1OTNizszN NFPtVVFUSU6JRWK=
P30-OHK NWS3bIhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF{LkW0O|kh|ryP NV;HTZlXW0GQR1XS
NCI-H1522 MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF{Lke0OkDPxE1? MV\TRW5ITVJ?
NCI-H1299 NX[5VHBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTF|LkK5NVEh|ryP M1fFZXNCVkeHUh?=
UACC-257 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjqWYpKSzVyPUGzMlUyOjZizszN MoqxV2FPT0WU
Calu-6 M{DGdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF|Lk[wOFYh|ryP Mn\iV2FPT0WU
NCI-H1882 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;yTWM2OD1zMz64OVU2KM7:TR?= NW\LWIlvW0GQR1XS
BB30-HNC M4TKbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCxZ3pKSzVyPUG0MlA3ODlizszN MVXTRW5ITVJ?
ES1 NIrPT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DRfGlEPTB;MUSuNVU2OSEQvF2= M{\UOXNCVkeHUh?=
NCI-H1694 NXTQUYVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTF2LkS4NVEh|ryP NFXvR2NUSU6JRWK=
IST-SL1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTVV4s3UUN3ME2xOE46PjF4IN88US=> MX\TRW5ITVJ?
ECC4 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF3LkC1OVgh|ryP MX;TRW5ITVJ?
MDA-MB-134-VI M3jXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[3OmlEPTB;MUWuOFE{OSEQvF2= NUXlPWVKW0GQR1XS
SCH MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TFN2lEPTB;MUWuOFczQCEQvF2= MVHTRW5ITVJ?
SK-N-FI M2\NWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF3Lk[1N|Qh|ryP MYPTRW5ITVJ?
HDLM-2 MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37Qd2lEPTB;MU[uNFcyPCEQvF2= NYq2R45iW0GQR1XS
Ramos-2G6-4C10 NIfwUJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFKzTIZKSzVyPUG2MlEzQTdizszN NWCxSXJOW0GQR1XS
EW-24 NHHk[IlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj6Wos{UUN3ME2xOk4yPjZzIN88US=> MmLHV2FPT0WU
NCI-H2141 NELje|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPJOWd1UUN3ME2xOk4yQDlizszN MWLTRW5ITVJ?
LC4-1 NXnsXFJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTJN4pmUUN3ME2xOk43OTF7IN88US=> MUnTRW5ITVJ?
HT-144 M33heGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\hXWlEPTB;MUeuNFA3KM7:TR?= NWLYeYs5W0GQR1XS
SK-MEL-1 NXj3doxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnCTWM2OD1zNz6wNFczKM7:TR?= Ml;tV2FPT0WU
SCC-15 M4r6VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G3RWlEPTB;MUeuNVY{QCEQvF2= MkiwV2FPT0WU
C8166 MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TydGlEPTB;MUeuOlg{OyEQvF2= NFHqSJVUSU6JRWK=
GOTO NWPWOopCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjBTGNKSzVyPUG3Mlg{PDRizszN M3zFSnNCVkeHUh?=
COR-L279 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF6LkGzOlIh|ryP NGjlVIhUSU6JRWK=
K-562 NEDxTZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DsWGlEPTB;MUiuO|E1OyEQvF2= NIPuXXFUSU6JRWK=
ES3 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HDSWlEPTB;MUiuPFA1OSEQvF2= NYrKNmxYW0GQR1XS
LU-165 NETVc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLTe2F4UUN3ME2xPU44ODB6IN88US=> MX7TRW5ITVJ?
KM-H2 M372Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnMVXFYUUN3ME2yNE4{OTh2IN88US=> MmGzV2FPT0WU
RL MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LMRmlEPTB;MkCuPVY6OiEQvF2= NXvJfJlpW0GQR1XS
EW-3 M2HEUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXENZVKSzVyPUKxMlE5QDlizszN MW\TRW5ITVJ?
A101D NVnsRo51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJzLkO3OVIh|ryP MVPTRW5ITVJ?
HUTU-80 M33WXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ToNmlEPTB;MkGuN|k1PiEQvF2= NH3XfGhUSU6JRWK=
NCI-H23 NFm4[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LYbmlEPTB;MkGuN|k6OiEQvF2= MknmV2FPT0WU
PF-382 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXCXmVzUUN3ME2yNU41PDB|IN88US=> NVPMcphMW0GQR1XS
LB373-MEL-D MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PzRWlEPTB;MkGuOVYyPSEQvF2= M4\ncHNCVkeHUh?=
TE-8 NVTCUYVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJzLk[zPVQh|ryP M3fHUXNCVkeHUh?=
TE-9 NUXDS2E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO0R3NKSzVyPUKxMlg2OTNizszN M3;sZnNCVkeHUh?=
Daudi M3rSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJzLkmzNFQh|ryP NWrCRVNHW0GQR1XS
D-542MG MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\CTWM2OD1{Mj6wNlU3KM7:TR?= MXXTRW5ITVJ?
U-698-M MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHLbmVKSzVyPUKyMlQ3ODNizszN MYjTRW5ITVJ?
ES6 MoTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS2TWM2OD1{Mj63N|Y3KM7:TR?= MnzvV2FPT0WU
DU-4475 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jZNGlEPTB;MkOuPFg6PyEQvF2= MYfTRW5ITVJ?
ECC12 M{m4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nWRWlEPTB;MkSuNlgxOyEQvF2= NWnD[I1IW0GQR1XS
C2BBe1 NUGxSYRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJ2LkOyN|kh|ryP NIPNOFFUSU6JRWK=
IST-SL2 NXXqd4o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ2LkSzOlIh|ryP M3zl[HNCVkeHUh?=
DJM-1 M1ntVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PKU2lEPTB;MkSuOVIzOSEQvF2= M3jwe3NCVkeHUh?=
DMS-153 NHf6[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkSzTWM2OD1{ND64OlE1KM7:TR?= M1rEPHNCVkeHUh?=
NB13 NYXESo5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjmTWM2OD1{NT6wNlY2KM7:TR?= MVXTRW5ITVJ?
SK-N-DZ M1u3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnjTWM2OD1{Nj6zOFE1KM7:TR?= NEnSdm5USU6JRWK=
COR-L88 NUPwN|k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLx[Y5KSzVyPUK2MlU4QTZizszN MmXhV2FPT0WU
LU-65 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJ4Lki1N|Uh|ryP NVf0PW1FW0GQR1XS
TGBC1TKB MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjkU3h2UUN3ME2yOk46QDJ6IN88US=> NU\WOIRZW0GQR1XS
THP-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX74OYk{UUN3ME2yO{4zOTRzIN88US=> M2L3UnNCVkeHUh?=
ONS-76 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TnfmlEPTB;MkeuN|MzKM7:TR?= MmXqV2FPT0WU
LC-2-ad MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzKepNKSzVyPUK3MlYzOzFizszN NHHCSpZUSU6JRWK=
EW-13 MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\CRZc{UUN3ME2yPU4yPzR4IN88US=> MVHTRW5ITVJ?
MS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXp[5VKSzVyPUOwMlczPzhizszN NI[1TolUSU6JRWK=
NCI-H2227 M3fDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13OOmlEPTB;M{CuPVgxPiEQvF2= MXvTRW5ITVJ?
LXF-289 NYficWpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXldJRKSzVyPUOxMlQ1QTJizszN NEPrXYVUSU6JRWK=
MC116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PzW2lEPTB;M{KuNFgzPiEQvF2= M3;0[3NCVkeHUh?=
EVSA-T M4\5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP5TWM2OD1|Mj6yOVg2KM7:TR?= MnfuV2FPT0WU
CTB-1 NEDaTW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTN|LkGxNFEh|ryP MYrTRW5ITVJ?
COLO-320-HSR NGDrWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H4XWlEPTB;M{OuNVYxOyEQvF2= MX3TRW5ITVJ?
NCI-H2196 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13LemlEPTB;M{OuNlU2PyEQvF2= MmTKV2FPT0WU
LB2241-RCC M2rld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n5TWlEPTB;M{OuN|E{PSEQvF2= NULBb29qW0GQR1XS
LS-513 MmDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nqeGlEPTB;M{OuPFY{QCEQvF2= NID2[nhUSU6JRWK=
LP-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f1PWlEPTB;M{OuPVk2PiEQvF2= M3\G[nNCVkeHUh?=
A253 Mof1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LIVWlEPTB;M{SuNlI6PiEQvF2= NUK2eWpGW0GQR1XS
SK-MM-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTDVFVNUUN3ME2zOE46PDVzIN88US=> NWXFdGZ5W0GQR1XS
NCI-H1963 NWDBcFZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7EZlRXUUN3ME2zOU4{ODd{IN88US=> MWfTRW5ITVJ?
MMAC-SF NFTGVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWxTWM2OD1|NT64O|g2KM7:TR?= NGPJUlNUSU6JRWK=
LB831-BLC M{Tl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN4LkC2OVQh|ryP MnTiV2FPT0WU
WSU-NHL MmDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3OZYxKSzVyPUO2MlE3PCEQvF2= NHSyWW9USU6JRWK=
CESS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fGTWlEPTB;M{[uNlg1QCEQvF2= MoHjV2FPT0WU
NEC8 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjpNJdRUUN3ME2zOk42QDN3IN88US=> NIi0[2VUSU6JRWK=
KNS-42 Mm\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:zTWM2OD1|Nz6xNlM4KM7:TR?= NF7r[mFUSU6JRWK=
MHH-CALL-2 M{jkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInWXndKSzVyPUO3MlE5OjFizszN MmDFV2FPT0WU
K5 NGq4NXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4njfGlEPTB;M{iuOFMh|ryP M3yxOHNCVkeHUh?=
CP66-MEL MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO5TWM2OD1|OT6wO|M{KM7:TR?= M1vYWHNCVkeHUh?=
OPM-2 M2\qdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorzTWM2OD1|OT64OFMzKM7:TR?= MmOwV2FPT0WU
IST-MES1 Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H1VGlEPTB;NECuN|A6PiEQvF2= NXLQO5FkW0GQR1XS
EC-GI-10 M3i0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrzTWM2OD12MT61PFA2KM7:TR?= MUfTRW5ITVJ?
CTV-1 NHK2e2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkG1TWM2OD12Mj64OFA3KM7:TR?= MXHTRW5ITVJ?
DG-75 NEfsO2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jzbmlEPTB;NEOuO|U6PSEQvF2= MUXTRW5ITVJ?
KNS-81-FD M2DCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXlTWM2OD12NT60NFU5KM7:TR?= NYrnWGxNW0GQR1XS
NCI-H82 NVqz[3VWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF62OYJKSzVyPUS1MlU4PThizszN MVnTRW5ITVJ?
RPMI-8866 NXPDWVA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTR4LkG4O|Mh|ryP MV;TRW5ITVJ?
ACN MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\5NVhTUUN3ME20Ok41OzRizszN MVjTRW5ITVJ?
NCI-H1395 NWHHdVJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXq5fHB2UUN3ME20Ok41PzV4IN88US=> M1P6bHNCVkeHUh?=
NCI-H209 NX3pdXpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTR5LkG0NFUh|ryP Mn24V2FPT0WU
TGW M2fvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rWcWlEPTB;NEmuNFc6OSEQvF2= MmP2V2FPT0WU
NCI-H748 NV7xdpJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XaeWlEPTB;NEmuOFc2OyEQvF2= MVXTRW5ITVJ?
EKVX MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTR7Lk[2Nlgh|ryP MX;TRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

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:
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
別名 BAY 43-9006

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00727233 Completed Neurofibromatosis Type I|Plexiform Neurofibroma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 8, 2008 Phase 1
NCT02989870 Not yet recruiting HepatoCellular Carcinoma|Unresectable HepatoCellular Carcinoma|Liver Cancer H. Lee Moffitt Cancer Center and Research Institute|National Comprehensive Cancer Network April 30, 2017 Phase 1
NCT01445080 Completed Leukemia|With AML and FLT3-ITD Mutations National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 23, 2006 Phase 1
NCT01434602 Recruiting Brain Tumor|Glioblastoma|Anaplastic Glioma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 21, 2015 Phase 1|Phase 2
NCT02988440 Not yet recruiting Hepatocellular Carcinoma Novartis Pharmaceuticals|Novartis May 2017 Phase 1
NCT03037437 Not yet recruiting Hepatocellular Cancer The University of Texas Health Science Center at San Antonio January 2017 Phase 2

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID