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 M3vjUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LNd2lEPTB;MD6wNFAxODNyMzFOwG0> NGXHWHBUSU6JRWK=
MONO-MAC-6 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7kNnFYUUN3ME2wMlAxPDF6IN88US=> MWPTRW5ITVJ?
ALL-PO NF2xVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq1N5NsUUN3ME2wMlA{OTh2IN88US=> NF7xfmtUSU6JRWK=
NKM-1 MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPlTWM2OD1yLkC3OFE3KM7:TR?= M2jnZnNCVkeHUh?=
CGTH-W-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fCXWlEPTB;MD6yOVAzOiEQvF2= MnvrV2FPT0WU
BB65-RCC NXi1cnN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPpTWM2OD1yLkS3NFc{KM7:TR?= NV[4N3VXW0GQR1XS
NOS-1 M3nnSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL4OJlwUUN3ME2wMlU3OzZizszN MmroV2FPT0WU
SH-4 M1u4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\F[IQ6UUN3ME2wMlY2PjF|IN88US=> Ml73V2FPT0WU
HOP-62 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwOEWwPFgh|ryP MlzHV2FPT0WU
HCC2998 M3L1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M330dWlEPTB;MD64PFgyQCEQvF2= M37UT3NCVkeHUh?=
GDM-1 MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jmdGlEPTB;MD65NFY6QCEQvF2= M{j6fHNCVkeHUh?=
KM12 NFu1cmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\tc3JKSzVyPUGuNFIxQThizszN MoLBV2FPT0WU
LB2518-MEL MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1exeGlEPTB;MT6yNFgxQSEQvF2= MoH2V2FPT0WU
NCI-H1436 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTFwMkG2O|gh|ryP NV\5VItZW0GQR1XS
EM-2 NVjFNZd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rjWGlEPTB;MT6zOVU4QCEQvF2= NWH1OJNnW0GQR1XS
LAMA-84 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7CTWM2OD1zLkO3OlQ5KM7:TR?= MoHOV2FPT0WU
KG-1 NFOxco9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTFwNEe5N|Uh|ryP MkS3V2FPT0WU
A388 NYrCbWtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M372WmlEPTB;MT61PVE3PSEQvF2= NXe0W49tW0GQR1XS
no-10 NHi4WVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHKRYxXUUN3ME2xMlYyPzJ4IN88US=> M1XDPHNCVkeHUh?=
SF126 M3[5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD5[VAyUUN3ME2xMlY{QDF{IN88US=> M1q4TnNCVkeHUh?=
MEG-01 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf3TWM2OD1zLkiwPVgh|ryP NHrSclRUSU6JRWK=
A3-KAW MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfJTWM2OD1zLki4OFIh|ryP MoTaV2FPT0WU
D-247MG NGO0dmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zCUGlEPTB;Mj6xOFQ5KM7:TR?= NWPqZXBnW0GQR1XS
OVCAR-4 M2TSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;vdWlEPTB;Mj6yNVM6OyEQvF2= Mnf5V2FPT0WU
NCI-SNU-1 M2Wwd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDN[IlxUUN3ME2yMlMyPjJizszN NYXBfZJ7W0GQR1XS
NCI-H2171 MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJwM{m3OlQh|ryP MWXTRW5ITVJ?
SIG-M5 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK1N2JKSzVyPUKuOFIzPDJizszN NX22OoNRW0GQR1XS
BE-13 NYfsUJZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17vTWlEPTB;Mj62PVYxQSEQvF2= MlfsV2FPT0WU
K052 NGPZOWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH0TGV1UUN3ME2yMlc1PjF4IN88US=> MV;TRW5ITVJ?
L-540 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NICyXHBKSzVyPUKuO|U4QDlizszN NFflZmpUSU6JRWK=
KMOE-2 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJwOEGzOUDPxE1? M4DRN3NCVkeHUh?=
MFH-ino M1\iT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LmVmlEPTB;Mj65NlE5PSEQvF2= NWTCV2lxW0GQR1XS
HL-60 NULyOXlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;FTWM2OD1|LkC2Nlk6KM7:TR?= M3v3RXNCVkeHUh?=
HCC2218 NGj2O4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPOTWM2OD1|LkGyNFA{KM7:TR?= M3rpfXNCVkeHUh?=
TE-5 Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fNc2lEPTB;Mz6xN|E3OiEQvF2= MUfTRW5ITVJ?
MZ1-PC MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKxTIZKSzVyPUOuOFc2ODlizszN NYDnXXo5W0GQR1XS
MRK-nu-1 NUO4NmMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XRVWlEPTB;Mz62NVQ3QCEQvF2= NF\pUHFUSU6JRWK=
MZ7-mel M2XESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHj2V5ZKSzVyPUOuOlYxQTlizszN NFHNfVhUSU6JRWK=
BC-1 NHXQV2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnITWM2OD1|Lke0NFIh|ryP MWLTRW5ITVJ?
ST486 MkOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3TTWM2OD1|LkizOlc{KM7:TR?= M1TrdXNCVkeHUh?=
KS-1 NF7xO5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zzfWlEPTB;Mz64PFE6QCEQvF2= MWXTRW5ITVJ?
SK-NEP-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zucWlEPTB;ND6xOlgyPSEQvF2= NGTtNYZUSU6JRWK=
BC-3 M{LsV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fqUWlEPTB;ND6yN|M6OSEQvF2= NY[1dW56W0GQR1XS
NCI-H1581 NVv0eoNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHKZnBNUUN3ME20MlI5Pzl6IN88US=> NV\hboZFW0GQR1XS
MHH-PREB-1 NX7yNphyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ztN2lEPTB;ND60NFQ5PCEQvF2= M{j2Z3NCVkeHUh?=
NOMO-1 NYrMd|dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jFb2lEPTB;ND60PFkxPSEQvF2= MYHTRW5ITVJ?
QIMR-WIL Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT1TWM2OD13LkC3Nlk1KM7:TR?= MXHTRW5ITVJ?
SF539 MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4X3WmlEPTB;NT6xN|IzPyEQvF2= MlvsV2FPT0WU
TE-12 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTVwMkS5Nlkh|ryP NGXUT21USU6JRWK=
NCI-H510A MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPwU4RxUUN3ME21MlQyPjh3IN88US=> MnXJV2FPT0WU
JAR M{DrRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDNRVBoUUN3ME21MlUxQDJ2IN88US=> M4L0b3NCVkeHUh?=
no-11 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDiTWM2OD13LkezOVY5KM7:TR?= M1rtVnNCVkeHUh?=
BV-173 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTWTWM2OD13Lkm1OlgzKM7:TR?= MWPTRW5ITVJ?
SR NFvFSWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTjOll[UUN3ME22MlAxPjd6IN88US=> NGTlSG9USU6JRWK=
MOLT-16 NFXsVmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP3dWZKSzVyPU[uNlUzPjZizszN NE\UUotUSU6JRWK=
MZ2-MEL M3fhTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;HTWlEPTB;Nj6zNVg{QSEQvF2= NH\U[WlUSU6JRWK=
SW954 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zxTmlEPTB;Nj60OVg3PiEQvF2= MV;TRW5ITVJ?
ML-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XZdWlEPTB;Nj61Nlg1QSEQvF2= NXm3ToloW0GQR1XS
OCI-AML2 NEfxe|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL0TWM2OD14Lk[xNFYzKM7:TR?= MlrHV2FPT0WU
SIMA NHyxOY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL4PYVKSzVyPUeuNFAyODFizszN NUTsO2F3W0GQR1XS
DOHH-2 MlvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7tW|ZKSzVyPUeuNFU3PzZizszN MWnTRW5ITVJ?
697 NVHP[2c2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjFWYpbUUN3ME23MlA2QTh7IN88US=> Mlz2V2FPT0WU
NB1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3CTJBbUUN3ME23MlQxPDB5IN88US=> NWWyXI1SW0GQR1XS
D-392MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLTU4NVUUN3ME23MlYzPjZ|IN88US=> NFfiS4ZUSU6JRWK=
ES8 NX;wWVUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4mxbWlEPTB;Nz63OlUxOyEQvF2= MlnFV2FPT0WU
RPMI-8226 M4D1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL5eG9KSzVyPUeuPFQ2OTFizszN MWXTRW5ITVJ?
IST-MEL1 M2W0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRThwNECwNFIh|ryP NUjNfopTW0GQR1XS
NB14 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\3O2lEPTB;OD62N|E{OyEQvF2= MmPlV2FPT0WU
HD-MY-Z M4rT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTISHZMUUN3ME24MlY{PzR4IN88US=> NH3mSHNUSU6JRWK=
TE-10 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rOeWlEPTB;OD63OlM2OyEQvF2= NFH6TVNUSU6JRWK=
LC-1F NXzPR2pyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33SOWlEPTB;OT6xNFg{PCEQvF2= MmjaV2FPT0WU
OS-RC-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn4V5dKSzVyPUmuNVEzPDNizszN MWnTRW5ITVJ?
NCI-SNU-16 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnmzTWM2OD17LkKxNFI3KM7:TR?= NFL1[pBUSU6JRWK=
SHP-77 MnXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTlwN{G2OlIh|ryP MWHTRW5ITVJ?
A4-Fuk NHzweppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\UTY5JUUN3ME25Mlc2PjFizszN NUDzNGJ5W0GQR1XS
NB6 M1HBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILsRXNKSzVyPUmuO|YxOjlizszN NE[w[FhUSU6JRWK=
JiyoyeP-2003 NEHSXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHJeG1KSzVyPUGwMlQ4PDVizszN NEnTSYFUSU6JRWK=
DMS-114 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TTc2lEPTB;MUCuOVQ1OSEQvF2= Ml61V2FPT0WU
NB7 NWK2VVB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrYTWM2OD1zMD63OVI3KM7:TR?= NX:4VYZxW0GQR1XS
NCI-H747 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFzLkGyNVYh|ryP NVLYdmxKW0GQR1XS
HH M4T3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULLbZlZUUN3ME2xNU4{QDd4IN88US=> MnTqV2FPT0WU
EW-18 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFzLkmwOFQh|ryP NV21PFJxW0GQR1XS
CHP-126 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFzLkm3N|gh|ryP NGnQNmlUSU6JRWK=
NTERA-S-cl-D1 M2K3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF{LkCyO|gh|ryP NWPTOXJJW0GQR1XS
DEL NGnQVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\JZWQ5UUN3ME2xNk4xQTh3IN88US=> NVq4ZmxZW0GQR1XS
LU-139 MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H0ZmlEPTB;MUKuOVQyOyEQvF2= M4DmT3NCVkeHUh?=
P30-OHK MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIizNY1KSzVyPUGyMlU1PzlizszN M2HiVnNCVkeHUh?=
NCI-H1522 NFjjZ|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\SRVZKSzVyPUGyMlc1PiEQvF2= NYnUfG1xW0GQR1XS
NCI-H1299 NWHybmlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PyT2lEPTB;MUOuNlkyOSEQvF2= M3\Fd3NCVkeHUh?=
UACC-257 NHfLOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfEdppKSzVyPUGzMlUyOjZizszN MorUV2FPT0WU
Calu-6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInuOJFKSzVyPUGzMlYxPDZizszN MX7TRW5ITVJ?
NCI-H1882 NXXncm14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rMOGlEPTB;MUOuPFU2PSEQvF2= MYDTRW5ITVJ?
BB30-HNC NHTWTVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXUTWM2OD1zND6wOlA6KM7:TR?= MVXTRW5ITVJ?
ES1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfzbWhKSzVyPUG0MlE2PTFizszN NF;VbZlUSU6JRWK=
NCI-H1694 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[wTWM2OD1zND60PFEyKM7:TR?= NXryVnExW0GQR1XS
IST-SL1 MoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHTWXJKSzVyPUG0Mlk3OTZizszN NWm5TnV[W0GQR1XS
ECC4 NVHiZZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF3LkC1OVgh|ryP M1PlNnNCVkeHUh?=
MDA-MB-134-VI NXXaU2pIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfkTWM2OD1zNT60NVMyKM7:TR?= MkP4V2FPT0WU
SCH NFvKTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTF3LkS3Nlgh|ryP NF3TXWJUSU6JRWK=
SK-N-FI Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PVXmlEPTB;MUWuOlU{PCEQvF2= MXHTRW5ITVJ?
HDLM-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXpTWM2OD1zNj6wO|E1KM7:TR?= M1;xOXNCVkeHUh?=
Ramos-2G6-4C10 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjZW5lKSzVyPUG2MlEzQTdizszN MkCwV2FPT0WU
EW-24 MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnTN5FKSzVyPUG2MlE3PjFizszN MlnTV2FPT0WU
NCI-H2141 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF4LkG4PUDPxE1? MXTTRW5ITVJ?
LC4-1 NGG0fFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjPeJdEUUN3ME2xOk43OTF7IN88US=> NF7vOIVUSU6JRWK=
HT-144 M1PW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nqOGlEPTB;MUeuNFA3KM7:TR?= Ml3FV2FPT0WU
SK-MEL-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXMe2RKSzVyPUG3MlAxPzJizszN NHnMc4lUSU6JRWK=
SCC-15 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWyOYhKSzVyPUG3MlE3OzhizszN M{DmcXNCVkeHUh?=
C8166 NFfWd2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED1N4FKSzVyPUG3MlY5OzNizszN NVjUWVlRW0GQR1XS
GOTO MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVztUYtWUUN3ME2xO{45OzR2IN88US=> M2Dhe3NCVkeHUh?=
COR-L279 MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zE[mlEPTB;MUiuNVM3OiEQvF2= MnHDV2FPT0WU
K-562 M4i4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G5PGlEPTB;MUiuO|E1OyEQvF2= NHzvS25USU6JRWK=
ES3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\FTWM2OD1zOD64NFQyKM7:TR?= M2rifnNCVkeHUh?=
LU-165 NHXQ[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm0e3BRUUN3ME2xPU44ODB6IN88US=> NXniWo9TW0GQR1XS
KM-H2 NYK3N3BkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXZTWM2OD1{MD6zNVg1KM7:TR?= MnjMV2FPT0WU
RL NX7YSVRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvPTWM2OD1{MD65OlkzKM7:TR?= NF3yflVUSU6JRWK=
EW-3 M1fJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDiTWM2OD1{MT6xPFg6KM7:TR?= M4ri[XNCVkeHUh?=
A101D NXfpcVNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn2UJlKSzVyPUKxMlM4PTJizszN M3zwXHNCVkeHUh?=
HUTU-80 NGDnSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\OVoFKSzVyPUKxMlM6PDZizszN NUL6e|JrW0GQR1XS
NCI-H23 Mn3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TXVWlEPTB;MkGuN|k6OiEQvF2= MmPlV2FPT0WU
PF-382 M{nrdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTLTWM2OD1{MT60OFA{KM7:TR?= NX\lOGpQW0GQR1XS
LB373-MEL-D MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJzLkW2NVUh|ryP M1XvXXNCVkeHUh?=
TE-8 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfZTWM2OD1{MT62N|k1KM7:TR?= NUPNbJB2W0GQR1XS
TE-9 M4n6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP1TWM2OD1{MT64OVE{KM7:TR?= M4DwTnNCVkeHUh?=
Daudi MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qxbmlEPTB;MkGuPVMxPCEQvF2= NHz4fFlUSU6JRWK=
D-542MG NYjlfJFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;2e3VKSzVyPUKyMlAzPTZizszN M{fGc3NCVkeHUh?=
U-698-M NHf4bWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHO1dFBKSzVyPUKyMlQ3ODNizszN NGf5eJFUSU6JRWK=
ES6 M3PYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{e0fWlEPTB;MkKuO|M3PiEQvF2= M3rhdnNCVkeHUh?=
DU-4475 M37IUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7vRVJKSzVyPUKzMlg5QTdizszN NYDVOnF[W0GQR1XS
ECC12 NXryfm5uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJ2LkK4NFMh|ryP M2rze3NCVkeHUh?=
C2BBe1 NWHIeo54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe2VYxvUUN3ME2yOE4{OjN7IN88US=> Mn60V2FPT0WU
IST-SL2 M13SbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJ2LkSzOlIh|ryP NGX3WYJUSU6JRWK=
DJM-1 NEPZOm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rZNGlEPTB;MkSuOVIzOSEQvF2= MXfTRW5ITVJ?
DMS-153 NEm2TXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLiXVFKSzVyPUK0Mlg3OTRizszN Mnq2V2FPT0WU
NB13 NXfGXmlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETDZ4xKSzVyPUK1MlAzPjVizszN MYXTRW5ITVJ?
SK-N-DZ MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPJOWlKSzVyPUK2MlM1OTRizszN MYLTRW5ITVJ?
COR-L88 NIHjdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJ4LkW3PVYh|ryP NHnE[HZUSU6JRWK=
LU-65 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{La[mlEPTB;Mk[uPFU{PSEQvF2= NWHrR3R2W0GQR1XS
TGBC1TKB MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJ4Lkm4Nlgh|ryP M3P4c3NCVkeHUh?=
THP-1 M2Pldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy0N4hKSzVyPUK3MlIyPDFizszN MUDTRW5ITVJ?
ONS-76 NHHTXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvPTWM2OD1{Nz6zN|Ih|ryP M3TpcHNCVkeHUh?=
LC-2-ad MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O3PWlEPTB;MkeuOlI{OSEQvF2= MUTTRW5ITVJ?
EW-13 M4HFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu1NXpKSzVyPUK5MlE4PDZizszN MkfvV2FPT0WU
MS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3BTWM2OD1|MD63Nlc5KM7:TR?= Ml;sV2FPT0WU
NCI-H2227 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHaNnR2UUN3ME2zNE46QDB4IN88US=> M{mxPHNCVkeHUh?=
LXF-289 NYPOZ5E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1WyXmlEPTB;M{GuOFQ6OiEQvF2= MVvTRW5ITVJ?
MC116 M1HIdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXGOmlIUUN3ME2zNk4xQDJ4IN88US=> NYn2dpNFW0GQR1XS
EVSA-T MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[5[GI6UUN3ME2zNk4zPTh3IN88US=> MnXVV2FPT0WU
CTB-1 NGDTcZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\U[YZKSzVyPUOzMlEyODFizszN MUDTRW5ITVJ?
COLO-320-HSR Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoewTWM2OD1|Mz6xOlA{KM7:TR?= NV7yeI5yW0GQR1XS
NCI-H2196 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnmxTWM2OD1|Mz6yOVU4KM7:TR?= NWnpRm1IW0GQR1XS
LB2241-RCC NVrC[3NGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPwTWM2OD1|Mz6zNVM2KM7:TR?= MULTRW5ITVJ?
LS-513 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jDZmlEPTB;M{OuPFY{QCEQvF2= NELOUotUSU6JRWK=
LP-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPGPXVWUUN3ME2zN{46QTV4IN88US=> MWXTRW5ITVJ?
A253 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX5NGtHUUN3ME2zOE4zOjl4IN88US=> NFHRZXhUSU6JRWK=
SK-MM-2 Ml;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz4TWM2OD1|ND65OFUyKM7:TR?= NYnDeJVSW0GQR1XS
NCI-H1963 M3TycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTRTWM2OD1|NT6zNFczKM7:TR?= MV\TRW5ITVJ?
MMAC-SF NF\HXJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\4TWM2OD1|NT64O|g2KM7:TR?= MmXmV2FPT0WU
LB831-BLC M13IbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jCbWlEPTB;M{[uNFY2PCEQvF2= M4XyfHNCVkeHUh?=
WSU-NHL MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7MXlJKSzVyPUO2MlE3PCEQvF2= M3G4NnNCVkeHUh?=
CESS MlXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPRRZpKSzVyPUO2MlI5PDhizszN NUjLd2pJW0GQR1XS
NEC8 MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTN4LkW4N|Uh|ryP Mn[xV2FPT0WU
KNS-42 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LIR2lEPTB;M{euNVI{PyEQvF2= MXvTRW5ITVJ?
MHH-CALL-2 NVm1Z2F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknxTWM2OD1|Nz6xPFIyKM7:TR?= M{DJenNCVkeHUh?=
K5 NGr5WmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN6LkSzJO69VQ>? NFLMVlFUSU6JRWK=
CP66-MEL NIn1cohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X6eGlEPTB;M{muNFc{OyEQvF2= NGn6W4dUSU6JRWK=
OPM-2 MnnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLHU5hLUUN3ME2zPU45PDN{IN88US=> NGO1NYJUSU6JRWK=
IST-MES1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTRyLkOwPVYh|ryP M3XiXHNCVkeHUh?=
EC-GI-10 NEjRTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLOTWM2OD12MT61PFA2KM7:TR?= NYPPbGFnW0GQR1XS
CTV-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjTcJhKSzVyPUSyMlg1ODZizszN NHLIN2VUSU6JRWK=
DG-75 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzRTWM2OD12Mz63OVk2KM7:TR?= Ml3DV2FPT0WU
KNS-81-FD MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m4O2lEPTB;NEWuOFA2QCEQvF2= M{DWOXNCVkeHUh?=
NCI-H82 M{LEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7CWm9KSzVyPUS1MlU4PThizszN MUXTRW5ITVJ?
RPMI-8866 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR4LkG4O|Mh|ryP NX7Z[mY1W0GQR1XS
ACN M{TtRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\YUHpCUUN3ME20Ok41OzRizszN MWrTRW5ITVJ?
NCI-H1395 NIO1S5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTXRVlKSzVyPUS2MlQ4PTZizszN NXT4fYJxW0GQR1XS
NCI-H209 M1LDSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS1TWM2OD12Nz6xOFA2KM7:TR?= NWHONlJCW0GQR1XS
TGW NFjpOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTxfoNjUUN3ME20PU4xPzlzIN88US=> MnLLV2FPT0WU
NCI-H748 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[2W2xKSzVyPUS5MlQ4PTNizszN NVv2W3RGW0GQR1XS
EKVX NIe5XmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vidmlEPTB;NEmuOlYzQCEQvF2= MX7TRW5ITVJ?

... 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 从左到右依次加入纯溶剂:
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。

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