Sorafenib

目录号:S7397 别名: BAY 43-9006

Sorafenib Chemical Structure

Molecular Weight(MW): 464.82

Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂,无细胞试验中IC50分别为6 nM, 22 nM和90 nM。

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RMB 1205.41 现货
RMB 2214.52 现货
RMB 5503.41 现货
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客户购买Selleck的此次产品后发表的文献62篇:

客户使用该产品的9个实验数据:

  • 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.

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂,无细胞试验中IC50分别为6 nM, 22 nM和90 nM。
靶点
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
体外研究

Sorafenib抑制野生型和V599E突变型B-Raf活性,IC50分别为22 nM 和 38 nM。Sorafenib也能有效抑制mVEGFR2 (Flk-1),mVEGFR3,mPDGFRβ,Flt3,和c-Kit,IC50分别为15 nM,20 nM,57 nM,58 nM,和68 nM。Sorafenib 能够较弱地抑制FGFR-1,IC50 为580 nM。Sorafenib对ERK-1,MEK-1,EGFR,HER-2,IGFR-1,c-Met,PKB,PKA,cdk1/cyclinB,PKCα,PKCγ,和pim-1没有活性。Sorafenib显著抑制NIH 3T3细胞中VEGFR2磷酸化,IC50 为 30 nM,也会抑制HEK-293细胞中Flt-3磷酸化,IC50 为20 nM。Sorafenib有效阻断大多数细胞中MEK 1/2 和 ERK 1/2磷酸化,但不阻断A549 或 H460细胞中该过程,同时不影响PKB通路的抑制。Sorafenib抑制HAoSMC 和 MDA-MB-231细胞的增殖,IC50分别为0.28 μM 和 2.6 μM。[1]除了抑制RAF/MEK/ERK信号通路,Sorafenib tosylate显著抑制eIF4E的磷酸化作用,并以MEK/ERK依赖的方式下调肝癌(HCC)细胞中Mcl-1水平。Sorafenib 抑制PLC/PRF/5 和HepG2细胞的增殖,IC50分别为6.3 μM 和 4.5 μM,并诱导显著的细胞凋亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 M1T6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjSdFlKSzVyPUCuNFAxODB|MEOg{txO Mlj0V2FPT0WU
MONO-MAC-6 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXuTWM2OD1yLkCwOFE5KM7:TR?= NH7DZXdUSU6JRWK=
ALL-PO NEL2OoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMEOxPFQh|ryP MXHTRW5ITVJ?
NKM-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;uUII2UUN3ME2wMlA4PDF4IN88US=> MXPTRW5ITVJ?
CGTH-W-1 M3;USWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIWxS5hKSzVyPUCuNlUxOjJizszN NWO3SXFoW0GQR1XS
BB65-RCC M1PmN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTkd5hKSzVyPUCuOFcxPzNizszN M2jrSXNCVkeHUh?=
NOS-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T5b2lEPTB;MD61OlM3KM7:TR?= MVPTRW5ITVJ?
SH-4 NUHlbXR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPKW21DUUN3ME2wMlY2PjF|IN88US=> NVTsZVhkW0GQR1XS
HOP-62 NHjjWmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fnbGlEPTB;MD64OVA5QCEQvF2= NV3weoo1W0GQR1XS
HCC2998 NIXDVGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjIWXN5UUN3ME2wMlg5QDF6IN88US=> MmXwV2FPT0WU
GDM-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwOUC2PVgh|ryP Mnf2V2FPT0WU
KM12 MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrRTWM2OD1zLkCyNFk5KM7:TR?= Mn3BV2FPT0WU
LB2518-MEL M3LSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnqN5k6UUN3ME2xMlIxQDB7IN88US=> MmL3V2FPT0WU
NCI-H1436 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHuzNJdKSzVyPUGuNlE3PzhizszN MmPxV2FPT0WU
EM-2 NUDOflQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HJTmlEPTB;MT6zOVU4QCEQvF2= NVzPVIpwW0GQR1XS
LAMA-84 NYHUZpkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXiTWM2OD1zLkO3OlQ5KM7:TR?= NFL5SohUSU6JRWK=
KG-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;vN3dpUUN3ME2xMlQ4QTN3IN88US=> M2jMTnNCVkeHUh?=
A388 M1zLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC0TWM2OD1zLkW5NVY2KM7:TR?= MWDTRW5ITVJ?
no-10 NEnWWG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTFwNkG3NlYh|ryP M1u0N3NCVkeHUh?=
SF126 NFfVRo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\5RmlEPTB;MT62N|gyOiEQvF2= MmjhV2FPT0WU
MEG-01 MnTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwOEC5PEDPxE1? MonUV2FPT0WU
A3-KAW NUH5fYV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwOEi0NkDPxE1? NHvPe4hUSU6JRWK=
D-247MG NHrUWmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7UTWM2OD1{LkG0OFgh|ryP NG\OUJhUSU6JRWK=
OVCAR-4 MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnK3TWM2OD1{LkKxN|k{KM7:TR?= MmjXV2FPT0WU
NCI-SNU-1 NF;2e45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LUdWlEPTB;Mj6zNVYzKM7:TR?= NHPHVZRUSU6JRWK=
NCI-H2171 NWrIOGd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\aTWM2OD1{LkO5O|Y1KM7:TR?= MVnTRW5ITVJ?
SIG-M5 M3\2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkmzTWM2OD1{LkSyNlQzKM7:TR?= Mn31V2FPT0WU
BE-13 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL2TWM2OD1{Lk[5OlA6KM7:TR?= M3LFWHNCVkeHUh?=
K052 NX7kTZA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoKxTWM2OD1{Lke0OlE3KM7:TR?= NH76OHdUSU6JRWK=
L-540 NYDTdHBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37WVmlEPTB;Mj63OVc5QSEQvF2= M1LsWnNCVkeHUh?=
KMOE-2 Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLq[pFKSzVyPUKuPFE{PSEQvF2= M3jrTXNCVkeHUh?=
MFH-ino NXfpUJFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XrO2lEPTB;Mj65NlE5PSEQvF2= NELwbFJUSU6JRWK=
HL-60 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\tTWM2OD1|LkC2Nlk6KM7:TR?= NEO1cXZUSU6JRWK=
HCC2218 NXKxUYIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HJNWlEPTB;Mz6xNlAxOyEQvF2= MorpV2FPT0WU
TE-5 M4SxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX0WXFKSzVyPUOuNVMyPjJizszN NEDGZZpUSU6JRWK=
MZ1-PC MojaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz1TWM2OD1|LkS3OVA6KM7:TR?= NVXWSJhPW0GQR1XS
MRK-nu-1 Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLZSGJoUUN3ME2zMlYyPDZ6IN88US=> M1TKcnNCVkeHUh?=
MZ7-mel NVPwWVI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCzOGlKSzVyPUOuOlYxQTlizszN MnHxV2FPT0WU
BC-1 M{ezOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjyTWM2OD1|Lke0NFIh|ryP NXq2O25uW0GQR1XS
ST486 M1XqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\2Xlh6UUN3ME2zMlg{Pjd|IN88US=> NIrvWYdUSU6JRWK=
KS-1 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli2TWM2OD1|Lki4NVk5KM7:TR?= NIrWOHVUSU6JRWK=
SK-NEP-1 NWPYNXlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPFTWM2OD12LkG2PFE2KM7:TR?= MmKyV2FPT0WU
BC-3 NYD5SIZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTRwMkOzPVEh|ryP NHiweodUSU6JRWK=
NCI-H1581 NVv5S4ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPOOWN4UUN3ME20MlI5Pzl6IN88US=> NXXibXJGW0GQR1XS
MHH-PREB-1 M3;FW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[5UWlEPTB;ND60NFQ5PCEQvF2= MkDaV2FPT0WU
NOMO-1 NFjQSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjiTWM2OD12LkS4PVA2KM7:TR?= NHq0SpdUSU6JRWK=
QIMR-WIL NFfscpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTVwMEeyPVQh|ryP NYPaSJd5W0GQR1XS
SF539 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTVwMUOyNlch|ryP MoXFV2FPT0WU
TE-12 NH7mSJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTUUHVKSzVyPUWuNlQ6OjlizszN MkDKV2FPT0WU
NCI-H510A M{T4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTVwNEG2PFUh|ryP MUfTRW5ITVJ?
JAR NV\PWotUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLyTWM2OD13LkWwPFI1KM7:TR?= NIDVRYFUSU6JRWK=
no-11 NITFXY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXDTWM2OD13LkezOVY5KM7:TR?= MUnTRW5ITVJ?
BV-173 NFX1TpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWmzUZFRUUN3ME21Mlk2Pjh{IN88US=> NHftXXVUSU6JRWK=
SR NUL5[|BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPrTWM2OD14LkCwOlc5KM7:TR?= MVLTRW5ITVJ?
MOLT-16 M{nPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDiS|JKSzVyPU[uNlUzPjZizszN MXHTRW5ITVJ?
MZ2-MEL MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;LTWM2OD14LkOxPFM6KM7:TR?= NIDjfVhUSU6JRWK=
SW954 NFPkXJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTZwNEW4OlYh|ryP MonuV2FPT0WU
ML-2 NVHIW5VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTZwNUK4OFkh|ryP M1vBSXNCVkeHUh?=
OCI-AML2 NVXpb5ZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnT0TWM2OD14Lk[xNFYzKM7:TR?= NILrNmpUSU6JRWK=
SIMA Ml\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTdwMECxNFEh|ryP NEPWOGhUSU6JRWK=
DOHH-2 M4fzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljETWM2OD15LkC1Olc3KM7:TR?= NInYTGdUSU6JRWK=
697 M1;oW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTdwMEW5PFkh|ryP NG[4bJBUSU6JRWK=
NB1 NWHne5Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\tfWlEPTB;Nz60NFQxPyEQvF2= NYDZdno6W0GQR1XS
D-392MG NGnKUWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M32zWmlEPTB;Nz62NlY3OyEQvF2= NV3FOJJJW0GQR1XS
ES8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\IcI53UUN3ME23Mlc3PTB|IN88US=> MWDTRW5ITVJ?
RPMI-8226 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu5cm1KSzVyPUeuPFQ2OTFizszN MV3TRW5ITVJ?
IST-MEL1 M3PTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPDeJBKSzVyPUiuOFAxODJizszN NWHidW9OW0GQR1XS
NB14 NF7lcGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRThwNkOxN|Mh|ryP NG\vTmFUSU6JRWK=
HD-MY-Z MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlToTWM2OD16Lk[zO|Q3KM7:TR?= M4fXV3NCVkeHUh?=
TE-10 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HnXmlEPTB;OD63OlM2OyEQvF2= Mon1V2FPT0WU
LC-1F MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfFbGlxUUN3ME25MlExQDN2IN88US=> MnjMV2FPT0WU
OS-RC-2 M3GwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTlwMUGyOFMh|ryP NXvyXpNIW0GQR1XS
NCI-SNU-16 NYK3fHpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;SfWlEPTB;OT6yNVAzPiEQvF2= M3nadnNCVkeHUh?=
SHP-77 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHlN2dKSzVyPUmuO|E3PjJizszN MlTOV2FPT0WU
A4-Fuk NIe4elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDLeI9KSzVyPUmuO|U3OSEQvF2= MmLUV2FPT0WU
NB6 NFOySnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXmTItKSzVyPUmuO|YxOjlizszN NEnLSG5USU6JRWK=
JiyoyeP-2003 NUTIUYxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFyLkS3OFUh|ryP MVTTRW5ITVJ?
DMS-114 NWrjSGdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3kTHVKSzVyPUGwMlU1PDFizszN MXfTRW5ITVJ?
NB7 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFyLke1NlYh|ryP MWTTRW5ITVJ?
NCI-H747 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfjPZpLUUN3ME2xNU4yOjF4IN88US=> MoXkV2FPT0WU
HH M1H2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjhUZpnUUN3ME2xNU4{QDd4IN88US=> M3HYcHNCVkeHUh?=
EW-18 M4G3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XrNWlEPTB;MUGuPVA1PCEQvF2= MV7TRW5ITVJ?
CHP-126 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjFRohKSzVyPUGxMlk4OzhizszN NXHsb5ZZW0GQR1XS
NTERA-S-cl-D1 NU\SUlJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzXOY5KSzVyPUGyMlAzPzhizszN M4\ZdXNCVkeHUh?=
DEL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e0cWlEPTB;MUKuNFk5PSEQvF2= NXjxc4tIW0GQR1XS
LU-139 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXBTWM2OD1zMj61OFE{KM7:TR?= Mlj6V2FPT0WU
P30-OHK NUPjfpNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF{LkW0O|kh|ryP NH;nUZRUSU6JRWK=
NCI-H1522 NY\0UYVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXkWGpKSzVyPUGyMlc1PiEQvF2= M4[xbHNCVkeHUh?=
NCI-H1299 NIXHTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF|LkK5NVEh|ryP MkCzV2FPT0WU
UACC-257 NH:yRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jqSGlEPTB;MUOuOVEzPiEQvF2= NH2xe4tUSU6JRWK=
Calu-6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\YN3JKSzVyPUGzMlYxPDZizszN M3TLT3NCVkeHUh?=
NCI-H1882 NX;lOJI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DiN2lEPTB;MUOuPFU2PSEQvF2= MYXTRW5ITVJ?
BB30-HNC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF2LkC2NFkh|ryP M1jRRnNCVkeHUh?=
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NCI-H1694 NFnp[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzTTWM2OD1zND60PFEyKM7:TR?= NYDkPZJMW0GQR1XS
IST-SL1 NF\tdIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF2Lkm2NVYh|ryP NGjrZWlUSU6JRWK=
ECC4 M1nZdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjKTWM2OD1zNT6wOVU5KM7:TR?= MWXTRW5ITVJ?
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HDLM-2 Mk[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jHeGlEPTB;MU[uNFcyPCEQvF2= M3vZU3NCVkeHUh?=
Ramos-2G6-4C10 Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF4LkGyPVch|ryP MUfTRW5ITVJ?
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HT-144 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljXTWM2OD1zNz6wNFYh|ryP MXHTRW5ITVJ?
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SCC-15 M{jkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf1Z2hiUUN3ME2xO{4yPjN6IN88US=> MnjWV2FPT0WU
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K-562 M3\HRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF6LkexOFMh|ryP MVrTRW5ITVJ?
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KM-H2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\jTWM2OD1{MD6zNVg1KM7:TR?= MWTTRW5ITVJ?
RL M1nkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Oz[WlEPTB;MkCuPVY6OiEQvF2= M2XkfHNCVkeHUh?=
EW-3 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT2TWM2OD1{MT6xPFg6KM7:TR?= MVnTRW5ITVJ?
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PF-382 NUPNXXBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJzLkS0NFMh|ryP NWLTZ2RuW0GQR1XS
LB373-MEL-D NWXTNJh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPFTWM2OD1{MT61OlE2KM7:TR?= M1faW3NCVkeHUh?=
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TE-9 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULndXJGUUN3ME2yNU45PTF|IN88US=> NH\odmJUSU6JRWK=
Daudi NVXaZ|A6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLKOpk5UUN3ME2yNU46OzB2IN88US=> MXzTRW5ITVJ?
D-542MG NVP2bHM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;0PGlEPTB;MkKuNFI2PiEQvF2= MmDDV2FPT0WU
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C2BBe1 Mnq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\pRWlEPTB;MkSuN|I{QSEQvF2= NVjET|d7W0GQR1XS
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DJM-1 NVvZR4E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmxTWM2OD1{ND61NlIyKM7:TR?= MVzTRW5ITVJ?
DMS-153 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fKWGlEPTB;MkSuPFYyPCEQvF2= MXPTRW5ITVJ?
NB13 M1zBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\1WYpKSzVyPUK1MlAzPjVizszN MkfDV2FPT0WU
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COR-L88 NI\RVppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLFXWlKSzVyPUK2MlU4QTZizszN MYjTRW5ITVJ?
LU-65 NFL4OmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;FTWM2OD1{Nj64OVM2KM7:TR?= NFvqVWNUSU6JRWK=
TGBC1TKB MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJ4Lkm4Nlgh|ryP M1TIUXNCVkeHUh?=
THP-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD0eGkyUUN3ME2yO{4zOTRzIN88US=> MkfEV2FPT0WU
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LC-2-ad M3H6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTOOZdKSzVyPUK3MlYzOzFizszN M1;BSXNCVkeHUh?=
EW-13 NVPEOGRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfMXFJKUUN3ME2yPU4yPzR4IN88US=> M2PvPXNCVkeHUh?=
MS-1 NV7hb4h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTNyLkeyO|gh|ryP Mn;KV2FPT0WU
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LXF-289 M1vrN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K1[mlEPTB;M{GuOFQ6OiEQvF2= NGPBW3ZUSU6JRWK=
MC116 NUXIZY1VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3CbmtKSzVyPUOyMlA5OjZizszN NHLGbXNUSU6JRWK=
EVSA-T M4r5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DKdWlEPTB;M{KuNlU5PSEQvF2= NF32bYNUSU6JRWK=
CTB-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTN|LkGxNFEh|ryP MnjLV2FPT0WU
COLO-320-HSR M2PvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG0TWM2OD1|Mz6xOlA{KM7:TR?= MWrTRW5ITVJ?
NCI-H2196 NI\CelFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2ycY5KSzVyPUOzMlI2PTdizszN NHPUcnJUSU6JRWK=
LB2241-RCC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC2c|R1UUN3ME2zN{4{OTN3IN88US=> NG\oeWhUSU6JRWK=
LS-513 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\OTWM2OD1|Mz64OlM5KM7:TR?= M3fIU3NCVkeHUh?=
LP-1 M1\pTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NISxT4lKSzVyPUOzMlk6PTZizszN MnnNV2FPT0WU
A253 NHXn[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3vTWM2OD1|ND6yNlk3KM7:TR?= NUixbnJwW0GQR1XS
SK-MM-2 NXq4ZmcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\hS21KSzVyPUO0Mlk1PTFizszN NHnNSmxUSU6JRWK=
NCI-H1963 NX2xfYl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzUbZFKSzVyPUO1MlMxPzJizszN NELOSFdUSU6JRWK=
MMAC-SF Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XpNWlEPTB;M{WuPFc5PSEQvF2= NGLKSZFUSU6JRWK=
LB831-BLC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml61TWM2OD1|Nj6wOlU1KM7:TR?= MljnV2FPT0WU
WSU-NHL MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m5N2lEPTB;M{[uNVY1KM7:TR?= M1zaW3NCVkeHUh?=
CESS M17JcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfC[ZdKSzVyPUO2MlI5PDhizszN Ml6wV2FPT0WU
NEC8 NWDRRVhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfrVHBUUUN3ME2zOk42QDN3IN88US=> MnmyV2FPT0WU
KNS-42 NX\rcYRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN5LkGyN|ch|ryP MWHTRW5ITVJ?
MHH-CALL-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPjXYQ1UUN3ME2zO{4yQDJzIN88US=> NIHEeYdUSU6JRWK=
K5 NV7QRlR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rIdGlEPTB;M{iuOFMh|ryP MYDTRW5ITVJ?
CP66-MEL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz0XFM{UUN3ME2zPU4xPzN|IN88US=> M{PicHNCVkeHUh?=
OPM-2 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jOSWlEPTB;M{muPFQ{OiEQvF2= MmjEV2FPT0WU
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EC-GI-10 Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj6O4ZSUUN3ME20NU42QDB3IN88US=> M3j0[HNCVkeHUh?=
CTV-1 NFrPV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXEO3pMUUN3ME20Nk45PDB4IN88US=> MmTGV2FPT0WU
DG-75 M1fFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z4NGlEPTB;NEOuO|U6PSEQvF2= M3r6NXNCVkeHUh?=
KNS-81-FD MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInHclFKSzVyPUS1MlQxPThizszN MYjTRW5ITVJ?
NCI-H82 Mnr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTR3LkW3OVgh|ryP NIfseHhUSU6JRWK=
RPMI-8866 M3fXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTR4LkG4O|Mh|ryP NHjOdnhUSU6JRWK=
ACN MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWxSGc5UUN3ME20Ok41OzRizszN MUDTRW5ITVJ?
NCI-H1395 M4jRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTR4LkS3OVYh|ryP NVTzTXU1W0GQR1XS
NCI-H209 NFzucmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi2d2FVUUN3ME20O{4yPDB3IN88US=> NEm2TmNUSU6JRWK=
TGW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPHUohxUUN3ME20PU4xPzlzIN88US=> MXHTRW5ITVJ?
NCI-H748 MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTR7LkS3OVMh|ryP NWHwNY02W0GQR1XS
EKVX NYfIPFFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PzPWlEPTB;NEmuOlYzQCEQvF2= NWPBS|ZpW0GQR1XS

... Click to View More Cell Line Experimental Data

体内研究 Sorafenib(~60 mg/kg)口服给药,对各种人肿瘤异种移植模型,包括MDA-MB-231,Colo-205,HT-29,DLD-1,NCI-H460,和A549表现出广谱的、剂量依赖性抗肿瘤活性,而没有毒性。与抗肿瘤功效相联系,Sorafenib 治疗有效抑制HT-29 和 MDA-MB-231异种移植物中MEK 1/2磷酸化和pERK 1/2水平,但对Colo-205异种移植物没有作用,并且也能显著抑制MDA MB-231,HT-29 和 Colo-205肿瘤异种移植物中肿瘤微血管面积(MVA)和微血管密度(MVD)。[1] 在SCID小鼠体内,Sorafenib治疗对PLC/PRF/5肿瘤异种移植产生剂量依赖性生长抑制,10 mg/kg和30 mg/kg剂量下,TGIs分别为49%和78%,与ERK 和 eIF4E磷酸化抑制,微血管面积减少,和肿瘤细胞凋亡的诱导相一致。[2] Sorafenib通过下调NF-κB介导的Mcl-1 和 cIAP2表达的作用机制使bax-/-细胞对TRAIL剂量依赖性敏感。 Sorafenib (30-60 mg/kg) 与 TRAIL (5 mg/kg)结合对TRAIL抗性HCT116 bax-/-和HT29肿瘤异种移植物表现出显著的功效。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
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生化检测:

重组杆状病毒表达的Raf-1 (残基305–648)和 B-Raf (残基 409–765)以融合蛋白纯化。全长人MEK-1由PCR产生,并以大肠杆菌裂解物中的融合蛋白纯化。将Sorafenib加入到含Raf-1 (80纳克),或B-Raf (80 纳克) 以及MEK-1 (1 微克) 混合物的实验缓冲液[20 mM Tris (pH 8.2),100 mM NaCl,5 mM MgCl2,和0.15% β-巯基乙醇]中,DMSO终浓度为1%。加入25微升10 μM γ[33P]ATP (400 Ci/mol)启动Raf激酶试验(终体积50微升),并在32 °C下培育25分钟。磷酸化的MEK-1通过过滤到磷酸纤维素板上采集,使用1%磷酸洗掉未结合的放射性。微波炉加热干燥后,使用β型板计数器量化过滤器结合放射性。人VEGFR2 (KDR)激酶域被表达,并从Sf9裂解物中纯化。VEGFR2的时间分辨荧光分析法能量转移测试在96孔不透明板中以时间分辨荧光分析法能量转移格式进行。最终反应条件如下:1 到10 μM ATP,25 nM poly GT生物素,2 nM 铕标记的磷酸(p)-酪氨酸抗体(PY20),10 nM APC,1% DMSO 终浓度的1 到 7 nM 细胞质激酶域,50 mM HEPES (pH 7.5),10 mM MgCl2,0.1 mM EDTA,0.015% Brij-35,0.1 毫克/毫升BSA,和0.1% β-巯基乙醇。反应体积为100微升,加入酶启动反应。反应启动~1.5 到 2.0小时后,板以615 和 665 nM在Perkin-Elmer VictorV多标记分析仪上读数。信号按如下比率计算:对每孔(665 nm/615 nM) × 10,000。对IC50的产生,在酶起始反应之前加入Sorafenib。50倍的库存板由Sorafenib在50% DMSO/50%蒸馏水溶液中连续稀释制得。最终Sorafenib在1% DMSO中的浓度范围为10 μM 到 4.56 nM。
细胞实验:[1]
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  • Cell lines: MDA-MB-231,和 HAoSMC
  • Concentrations: 溶解于DMSO,终浓度为~10 μM
  • Incubation Time: 72小时
  • Method: 细胞在逐渐增加浓度的Sorafenib下暴露72小时。细胞数通过Cell TiterGlo ATP发光测定试剂盒进行定量。该试验通过测定基于细胞中ATP量的发光信号,测量每孔中的活细胞。
    (Only for Reference)
动物实验:[1]
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  • Animal Models: 雌性 NCr-nu/nu 小鼠,皮下植入MDA-MB-231,Colo-205,HT-29,H460,或 A549 细胞
  • Formulation: 以4倍(4 ×储备溶液,稀释为1 ×)溶解于聚氧乙烯蓖麻油/乙醇(50:50)
  • Dosages: ~60 mg/kg
  • Administration: 口服,每天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 63 mg/mL warmed (135.53 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用:
5% DMSO+45% PEG 400+ddH2O
3mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 464.82
化学式

C21H16ClF3N4O3

CAS号 284461-73-0
稳定性 powder
别名 BAY 43-9006

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID