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 NW\RcldZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDiTWM2OD1yLkCwNFAxOzB|IN88US=> NXf4d2lCW0GQR1XS
MONO-MAC-6 MmfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMEC0NVgh|ryP NX[1NnRnW0GQR1XS
ALL-PO MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[3TWM2OD1yLkCzNVg1KM7:TR?= NXnMPVVmW0GQR1XS
NKM-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\NVpNIUUN3ME2wMlA4PDF4IN88US=> M{jjc3NCVkeHUh?=
CGTH-W-1 NGf5NXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;HRo9KSzVyPUCuNlUxOjJizszN MVrTRW5ITVJ?
BB65-RCC NWDRVnRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHmTWM2OD1yLkS3NFc{KM7:TR?= NXe0dlFJW0GQR1XS
NOS-1 NFXsNYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwNU[zOkDPxE1? NWfjUJE2W0GQR1XS
SH-4 NYH0XotYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DxV2lEPTB;MD62OVYyOyEQvF2= MULTRW5ITVJ?
HOP-62 M2ixcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPtTWM2OD1yLki1NFg5KM7:TR?= MYDTRW5ITVJ?
HCC2998 NFexUY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwOEi4NVgh|ryP M4TnZXNCVkeHUh?=
GDM-1 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwOUC2PVgh|ryP M4G0[3NCVkeHUh?=
KM12 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLZTWM2OD1zLkCyNFk5KM7:TR?= NX7YTm8yW0GQR1XS
LB2518-MEL MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH3WI9UUUN3ME2xMlIxQDB7IN88US=> M1PEfXNCVkeHUh?=
NCI-H1436 NHvRfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;nNmlEPTB;MT6yNVY4QCEQvF2= MVXTRW5ITVJ?
EM-2 NXruVVQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFwM{W1O|gh|ryP NWjSbXVJW0GQR1XS
LAMA-84 NUjwXZNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2ybpJMUUN3ME2xMlM4PjR6IN88US=> MkfFV2FPT0WU
KG-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDxTWM2OD1zLkS3PVM2KM7:TR?= M{nGd3NCVkeHUh?=
A388 NEDsNXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;uXlRKSzVyPUGuOVkyPjVizszN NYK4SZVvW0GQR1XS
no-10 NGTmenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTFwNkG3NlYh|ryP MXnTRW5ITVJ?
SF126 MnH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn75TWM2OD1zLk[zPFEzKM7:TR?= NGXDbWdUSU6JRWK=
MEG-01 Mo\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPzZYxEUUN3ME2xMlgxQThizszN M3TlVHNCVkeHUh?=
A3-KAW NX\yOmVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwOEi0NkDPxE1? MlrlV2FPT0WU
D-247MG M33rbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvNXGNKSzVyPUKuNVQ1QCEQvF2= NFflbWFUSU6JRWK=
OVCAR-4 NW\TemVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJwMkGzPVMh|ryP NVTEbYg2W0GQR1XS
NCI-SNU-1 Mmi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjSVYFKSzVyPUKuN|E3OiEQvF2= NG\iWYpUSU6JRWK=
NCI-H2171 NInaVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH31fldKSzVyPUKuN|k4PjRizszN MkXQV2FPT0WU
SIG-M5 M3i0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnudFhKSzVyPUKuOFIzPDJizszN MkTRV2FPT0WU
BE-13 M4LVNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jLbGlEPTB;Mj62PVYxQSEQvF2= MmjOV2FPT0WU
K052 M4H4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfETWM2OD1{Lke0OlE3KM7:TR?= NVrBbZhyW0GQR1XS
L-540 M1nScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW0TWM2OD1{Lke1O|g6KM7:TR?= M3;JSHNCVkeHUh?=
KMOE-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2juWWlEPTB;Mj64NVM2KM7:TR?= M1nBVnNCVkeHUh?=
MFH-ino M1vUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HBXGlEPTB;Mj65NlE5PSEQvF2= M{\HWXNCVkeHUh?=
HL-60 NVHuVnRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XmeGlEPTB;Mz6wOlI6QSEQvF2= MnTJV2FPT0WU
HCC2218 M4\iVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTNwMUKwNFMh|ryP MmTHV2FPT0WU
TE-5 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLVTWM2OD1|LkGzNVYzKM7:TR?= M{TEd3NCVkeHUh?=
MZ1-PC NU\vZ2NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nVbWlEPTB;Mz60O|UxQSEQvF2= MXzTRW5ITVJ?
MRK-nu-1 NVHybHU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknRTWM2OD1|Lk[xOFY5KM7:TR?= MlmyV2FPT0WU
MZ7-mel NHfO[|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Hwc2lEPTB;Mz62OlA6QSEQvF2= NVvYWVdzW0GQR1XS
BC-1 NIjXNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTNwN{SwNkDPxE1? MnW1V2FPT0WU
ST486 NUL6NWJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYi1e49WUUN3ME2zMlg{Pjd|IN88US=> Ml72V2FPT0WU
KS-1 NF[1fWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vFcmlEPTB;Mz64PFE6QCEQvF2= MXHTRW5ITVJ?
SK-NEP-1 NGq3PYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XFWmlEPTB;ND6xOlgyPSEQvF2= MVHTRW5ITVJ?
BC-3 M1fNfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTRwMkOzPVEh|ryP MoWxV2FPT0WU
NCI-H1581 NHHEWJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i4NWlEPTB;ND6yPFc6QCEQvF2= MYjTRW5ITVJ?
MHH-PREB-1 NWCyRnBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm0bVRKSzVyPUSuOFA1QDRizszN MmD0V2FPT0WU
NOMO-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LaSmlEPTB;ND60PFkxPSEQvF2= M{LDUnNCVkeHUh?=
QIMR-WIL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnSOZRpUUN3ME21MlA4Ojl2IN88US=> M3PjdXNCVkeHUh?=
SF539 NUPCeW9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlv3TWM2OD13LkGzNlI4KM7:TR?= MUHTRW5ITVJ?
TE-12 M2fsU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTVwMkS5Nlkh|ryP M4joWnNCVkeHUh?=
NCI-H510A M1\Ud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXIcpFZUUN3ME21MlQyPjh3IN88US=> Mln6V2FPT0WU
JAR MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDrVXl1UUN3ME21MlUxQDJ2IN88US=> M17sdHNCVkeHUh?=
no-11 NEjMSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDPdllCUUN3ME21Mlc{PTZ6IN88US=> NVLDNmV4W0GQR1XS
BV-173 NELyNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITBPIFKSzVyPUWuPVU3QDJizszN M3ewXnNCVkeHUh?=
SR MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTZwMEC2O|gh|ryP MnnJV2FPT0WU
MOLT-16 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXSTWM2OD14LkK1NlY3KM7:TR?= NFjkbZZUSU6JRWK=
MZ2-MEL NW\I[nNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTZwM{G4N|kh|ryP MVfTRW5ITVJ?
SW954 NHnVXJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv0[4NKSzVyPU[uOFU5PjZizszN MlT2V2FPT0WU
ML-2 NVPuNnNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXFemtyUUN3ME22MlUzQDR7IN88US=> MnXoV2FPT0WU
OCI-AML2 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LadWlEPTB;Nj62NVA3OiEQvF2= M4LIVnNCVkeHUh?=
SIMA NGjTXXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq2TFMxUUN3ME23MlAxOTBzIN88US=> MoOxV2FPT0WU
DOHH-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GyPWlEPTB;Nz6wOVY4PiEQvF2= NXTBNndzW0GQR1XS
697 NFLTPIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy3VnplUUN3ME23MlA2QTh7IN88US=> M3fxbHNCVkeHUh?=
NB1 MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;zTWM2OD15LkSwOFA4KM7:TR?= NUP0N5pNW0GQR1XS
D-392MG MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\LTWM2OD15Lk[yOlY{KM7:TR?= M2XkTnNCVkeHUh?=
ES8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTdwN{[1NFMh|ryP NGfMe5NUSU6JRWK=
RPMI-8226 NXLQS4JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\SfoNKSzVyPUeuPFQ2OTFizszN NXyxcmpEW0GQR1XS
IST-MEL1 M2TDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHpUIxvUUN3ME24MlQxODB{IN88US=> MmGzV2FPT0WU
NB14 NEjGXohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRThwNkOxN|Mh|ryP M{nF[XNCVkeHUh?=
HD-MY-Z NGWxdo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHqzVFhKSzVyPUiuOlM4PDZizszN MoHPV2FPT0WU
TE-10 NIfwd2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTjRW91UUN3ME24Mlc3OzV|IN88US=> NFjEUopUSU6JRWK=
LC-1F MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrHdVhoUUN3ME25MlExQDN2IN88US=> NWfRVVdMW0GQR1XS
OS-RC-2 MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT3TXBHUUN3ME25MlEyOjR|IN88US=> NWfJ[2ZMW0GQR1XS
NCI-SNU-16 NVjIWnpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnoTWM2OD17LkKxNFI3KM7:TR?= Mly5V2FPT0WU
SHP-77 NXLwWplCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XxTWlEPTB;OT63NVY3OiEQvF2= MUTTRW5ITVJ?
A4-Fuk MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DTOmlEPTB;OT63OVYyKM7:TR?= NH20Z3RUSU6JRWK=
NB6 NWXLT2hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIntepJKSzVyPUmuO|YxOjlizszN NX;m[YNCW0GQR1XS
JiyoyeP-2003 NVz5fGRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFyLkS3OFUh|ryP M1X2XHNCVkeHUh?=
DMS-114 MlG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFyLkW0OFEh|ryP MmjHV2FPT0WU
NB7 M1X0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLUTWM2OD1zMD63OVI3KM7:TR?= MXvTRW5ITVJ?
NCI-H747 NUW3VlZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnSyTWM2OD1zMT6xNlE3KM7:TR?= MkGyV2FPT0WU
HH NYXmXnpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13weWlEPTB;MUGuN|g4PiEQvF2= M{KybHNCVkeHUh?=
EW-18 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFmwRmFKSzVyPUGxMlkxPDRizszN NW\YTm9ZW0GQR1XS
CHP-126 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Lad2lEPTB;MUGuPVc{QCEQvF2= NWHBPVVrW0GQR1XS
NTERA-S-cl-D1 M1TkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf6eVY5UUN3ME2xNk4xOjd6IN88US=> M3fDWHNCVkeHUh?=
DEL NYLZR2FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF{LkC5PFUh|ryP MWLTRW5ITVJ?
LU-139 M13v[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPLTWM2OD1zMj61OFE{KM7:TR?= NH20OoRUSU6JRWK=
P30-OHK MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF{LkW0O|kh|ryP NHvxR3ZUSU6JRWK=
NCI-H1522 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfnSGtKSzVyPUGyMlc1PiEQvF2= NGDyfFlUSU6JRWK=
NCI-H1299 NEjPN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXpUYZKSzVyPUGzMlI6OTFizszN Mnq1V2FPT0WU
UACC-257 M4XVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHFfWVKSzVyPUGzMlUyOjZizszN NH3Hb3pUSU6JRWK=
Calu-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF|Lk[wOFYh|ryP M{nOdXNCVkeHUh?=
NCI-H1882 NXLscWQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfNXm9KSzVyPUGzMlg2PTVizszN MXLTRW5ITVJ?
BB30-HNC NXHiboZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vHT2lEPTB;MUSuNFYxQSEQvF2= NVvEdYJzW0GQR1XS
ES1 NEHXVo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHHdG42UUN3ME2xOE4yPTVzIN88US=> MYTTRW5ITVJ?
NCI-H1694 NF30U|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrTTWM2OD1zND60PFEyKM7:TR?= MofmV2FPT0WU
IST-SL1 NEjPXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF2Lkm2NVYh|ryP MnPRV2FPT0WU
ECC4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF3LkC1OVgh|ryP NFnHRotUSU6JRWK=
MDA-MB-134-VI MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnRXWhKSzVyPUG1MlQyOzFizszN NHHGSGdUSU6JRWK=
SCH NW\jV|NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETnVVhKSzVyPUG1MlQ4OjhizszN NWXRVlZ4W0GQR1XS
SK-N-FI NF7ZNY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHBTWM2OD1zNT62OVM1KM7:TR?= MnrtV2FPT0WU
HDLM-2 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LWUWlEPTB;MU[uNFcyPCEQvF2= M3y4NnNCVkeHUh?=
Ramos-2G6-4C10 NX;a[nJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17seWlEPTB;MU[uNVI6PyEQvF2= NEft[|BUSU6JRWK=
EW-24 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXDWVVKSzVyPUG2MlE3PjFizszN NHHyUFlUSU6JRWK=
NCI-H2141 M1zIcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF4LkG4PUDPxE1? MWDTRW5ITVJ?
LC4-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:zeWlEPTB;MU[uOlEyQSEQvF2= NEfZPIpUSU6JRWK=
HT-144 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;BTWM2OD1zNz6wNFYh|ryP MkHEV2FPT0WU
SK-MEL-1 NFS4ZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrZZ2V6UUN3ME2xO{4xODd{IN88US=> MlfLV2FPT0WU
SCC-15 NGnZTGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TWRWlEPTB;MUeuNVY{QCEQvF2= NFTFW5pUSU6JRWK=
C8166 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq5dnY{UUN3ME2xO{43QDN|IN88US=> M2jvNHNCVkeHUh?=
GOTO MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTF5LkizOFQh|ryP MWDTRW5ITVJ?
COR-L279 NIfFVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV61V5dkUUN3ME2xPE4yOzZ{IN88US=> MX;TRW5ITVJ?
K-562 M2LROmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fQfWlEPTB;MUiuO|E1OyEQvF2= NWXPbFlZW0GQR1XS
ES3 MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXwN5ZKSzVyPUG4MlgxPDFizszN NHnFTmtUSU6JRWK=
LU-165 NYXjVVF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF7LkewNFgh|ryP M2\wOnNCVkeHUh?=
KM-H2 M1zZdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zYd2lEPTB;MkCuN|E5PCEQvF2= M4rIO3NCVkeHUh?=
RL M3zscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:0SHhzUUN3ME2yNE46Pjl{IN88US=> MXHTRW5ITVJ?
EW-3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETobmhKSzVyPUKxMlE5QDlizszN MmnaV2FPT0WU
A101D MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj4SZZKSzVyPUKxMlM4PTJizszN M4HRdHNCVkeHUh?=
HUTU-80 M1W2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3TPW9KSzVyPUKxMlM6PDZizszN MnzaV2FPT0WU
NCI-H23 M3;XcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCzNnhXUUN3ME2yNU4{QTl{IN88US=> NVf6dYlnW0GQR1XS
PF-382 MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjpTWM2OD1{MT60OFA{KM7:TR?= NWjOdXBIW0GQR1XS
LB373-MEL-D MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJzLkW2NVUh|ryP Mn65V2FPT0WU
TE-8 M4S5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHQSm5KSzVyPUKxMlY{QTRizszN MXXTRW5ITVJ?
TE-9 M4jzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJzLki1NVMh|ryP NXrhT2l[W0GQR1XS
Daudi NYW4NJhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKyenFKSzVyPUKxMlk{ODRizszN MX\TRW5ITVJ?
D-542MG Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPpTWM2OD1{Mj6wNlU3KM7:TR?= NIjid5VUSU6JRWK=
U-698-M M4niU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3oTWM2OD1{Mj60OlA{KM7:TR?= NXnRPYl2W0GQR1XS
ES6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjjTWM2OD1{Mj63N|Y3KM7:TR?= M3z0d3NCVkeHUh?=
DU-4475 NF2zVHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfhS3J1UUN3ME2yN{45QDl5IN88US=> Mny3V2FPT0WU
ECC12 NX7pV2pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJ2LkK4NFMh|ryP NFjmTYVUSU6JRWK=
C2BBe1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJ2LkOyN|kh|ryP MmfiV2FPT0WU
IST-SL2 NHL3OHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TzUGlEPTB;MkSuOFM3OiEQvF2= MoLhV2FPT0WU
DJM-1 M2HSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyzU4RxUUN3ME2yOE42OjJzIN88US=> NFXhU3FUSU6JRWK=
DMS-153 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;GZmVKSzVyPUK0Mlg3OTRizszN MULTRW5ITVJ?
NB13 NUfvZW9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJ3LkCyOlUh|ryP MV;TRW5ITVJ?
SK-N-DZ NYLvb5o{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrYNHhMUUN3ME2yOk4{PDF2IN88US=> M4\xfHNCVkeHUh?=
COR-L88 Ml\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LlNGlEPTB;Mk[uOVc6PiEQvF2= MmTPV2FPT0WU
LU-65 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f0eGlEPTB;Mk[uPFU{PSEQvF2= MlzlV2FPT0WU
TGBC1TKB NUfOeolzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\2UWlEPTB;Mk[uPVgzQCEQvF2= NFrQT3dUSU6JRWK=
THP-1 M1nNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrrN|hDUUN3ME2yO{4zOTRzIN88US=> M4jqenNCVkeHUh?=
ONS-76 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr6TXc3UUN3ME2yO{4{OzJizszN NUXnNopvW0GQR1XS
LC-2-ad MnT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnGW|ZMUUN3ME2yO{43OjNzIN88US=> M1vW[3NCVkeHUh?=
EW-13 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ7LkG3OFYh|ryP NXf1S4hTW0GQR1XS
MS-1 MknrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DqNWlEPTB;M{CuO|I4QCEQvF2= NGe3OHlUSU6JRWK=
NCI-H2227 M3jwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zwSWlEPTB;M{CuPVgxPiEQvF2= MVLTRW5ITVJ?
LXF-289 NEfuNVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHyTWM2OD1|MT60OFkzKM7:TR?= NVf3N45DW0GQR1XS
MC116 MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkToTWM2OD1|Mj6wPFI3KM7:TR?= NEXB[oxUSU6JRWK=
EVSA-T NYnsd3luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN{LkK1PFUh|ryP NEjINpVUSU6JRWK=
CTB-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkS4TWM2OD1|Mz6xNVAyKM7:TR?= NHT2TW5USU6JRWK=
COLO-320-HSR Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknFTWM2OD1|Mz6xOlA{KM7:TR?= NIG4TolUSU6JRWK=
NCI-H2196 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTnVGgzUUN3ME2zN{4zPTV5IN88US=> NFq2VnBUSU6JRWK=
LB2241-RCC NUPHUGpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTLTpZjUUN3ME2zN{4{OTN3IN88US=> NG\DOXVUSU6JRWK=
LS-513 NUe4PY9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPwdJVuUUN3ME2zN{45PjN6IN88US=> MnPiV2FPT0WU
LP-1 NFn0XG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\UdWlEPTB;M{OuPVk2PiEQvF2= MV\TRW5ITVJ?
A253 M4DZVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTFTWM2OD1|ND6yNlk3KM7:TR?= Mn3TV2FPT0WU
SK-MM-2 MnfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPHenFiUUN3ME2zOE46PDVzIN88US=> MknNV2FPT0WU
NCI-H1963 M1zxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPlbIVKSzVyPUO1MlMxPzJizszN NYTtdIVYW0GQR1XS
MMAC-SF M4\wTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HwNmlEPTB;M{WuPFc5PSEQvF2= NInyXWFUSU6JRWK=
LB831-BLC M3GxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnJ[HlSUUN3ME2zOk4xPjV2IN88US=> NVTydXJpW0GQR1XS
WSU-NHL NEPjbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvJTWM2OD1|Nj6xOlQh|ryP NUDJWFRLW0GQR1XS
CESS M1nIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\zWoFuUUN3ME2zOk4zQDR6IN88US=> MkfXV2FPT0WU
NEC8 MojvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nCRWlEPTB;M{[uOVg{PSEQvF2= NWi4TphUW0GQR1XS
KNS-42 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1faR2lEPTB;M{euNVI{PyEQvF2= MmPPV2FPT0WU
MHH-CALL-2 MlnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDUcFdQUUN3ME2zO{4yQDJzIN88US=> M3i0[nNCVkeHUh?=
K5 M3[wOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTN6LkSzJO69VQ>? NWq5PW1CW0GQR1XS
CP66-MEL NIK1S5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN7LkC3N|Mh|ryP NXXKUXR7W0GQR1XS
OPM-2 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e3O2lEPTB;M{muPFQ{OiEQvF2= NIDGWGNUSU6JRWK=
IST-MES1 NHLuWW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTRyLkOwPVYh|ryP M{S5UHNCVkeHUh?=
EC-GI-10 M1nCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Z[o1TUUN3ME20NU42QDB3IN88US=> M321e3NCVkeHUh?=
CTV-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTR{Lki0NFYh|ryP M2XOVnNCVkeHUh?=
DG-75 NGW1e2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7oWWJKSzVyPUSzMlc2QTVizszN MlvCV2FPT0WU
KNS-81-FD MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnGW2QyUUN3ME20OU41ODV6IN88US=> NGTBO5hUSU6JRWK=
NCI-H82 MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj5TWM2OD12NT61O|U5KM7:TR?= NYOyRVdIW0GQR1XS
RPMI-8866 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nB[mlEPTB;NE[uNVg4OyEQvF2= MmXpV2FPT0WU
ACN NFrGfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITQOHZKSzVyPUS2MlQ{PCEQvF2= NVT0TFkzW0GQR1XS
NCI-H1395 M{TzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rGZ2lEPTB;NE[uOFc2PiEQvF2= NIjJOFdUSU6JRWK=
NCI-H209 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2mzU2lEPTB;NEeuNVQxPSEQvF2= M1fBNHNCVkeHUh?=
TGW M4nKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn5ZYVKSzVyPUS5MlA4QTFizszN Mn3UV2FPT0WU
NCI-H748 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDiS3JKSzVyPUS5MlQ4PTNizszN Ml7EV2FPT0WU
EKVX NF;GcWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3P6R2lEPTB;NEmuOlYzQCEQvF2= NG\pVJRUSU6JRWK=

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