PLX-4720

目录号:S1152

PLX-4720 Chemical Structure

Molecular Weight(MW): 413.83

PLX-4720是一种有效的,选择性的B-RafV600E抑制剂,无细胞试验中IC50为13 nM,同样有效地作用于c-Raf-1(Y340D和Y341D突变型),作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。

规格 价格 库存 购买数量  
RMB 1266.55 现货
RMB 976.01 现货
RMB 2186.24 现货
RMB 5496.89 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck该产品发表文献49篇:

客户使用该产品的10个实验数据:

  • Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.

    Cancer Discov 2013 3, 350-62. PLX-4720 purchased from Selleck.

    Most of the resistant cells had higher levels of DCT compared with the parental cells. Cells were stained with a fluorescent-labeled DCT antibody (green) and counterstained with DAPI (blue).

    Genome Res, 2018, 28(9):1353-1363. PLX-4720 purchased from Selleck.

  • RAF inhibitors induce dimer formation between KSR and RAF, and activate KSR by CRAF. (A) GDC0879 but not PLX4720 induces BRAF/CRAF dimers. Cells overexpressing myc-CRAF and BRAF were treated with drug for 1 h and CRAF immunoprecipitates were immunoblotted for BRAF and CRAF (epitope tagged with myc). (B) GDC0879 but not PLX4720 enhances KSR/BRAF complexes. KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and BRAF after treatment with the indicated drug for 1 h and immunoblotted using antibodies to BRAF. (C) Both GDC0879 and PLX4720 induce KSR/CRAF complexes.KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and myc-CRAF after treatment with the indicated drug for 1 h and immunoblotted for CRAF using myc antibodies. (D and E) Requirement of KSR for drug-induced ERK activation. Lysates fromwild-type and KSR deficient fibroblasts, transfected with RASV12, were treated with the indicated doses of either GDC-0879 (D) or PLX4720 (E) for 1 h. Lysates were immunoblotted for phospho-ERK1 and 2, ERK2, and RASV12. (F) KSR and CRAF cooperate to activate MEK. Cells expressing the indicated constructs were treated with a 50 μM PLX4720 for 2 h before cell lysates were prepared and analyzed for pMEK by immunoblotting. CRAF(TM) refers to the T421M gatekeeper mutant that cannot bind to the drug(4). (G) KSR in vitro kinase reactions. Cells were cotransfected with WT or ATP binding deficient KSR and CRAF and immunoprecipitates prepared after cells were treated with an activating dose of PLX (10 μM) for 1 h. KSR immunoprecipitates were prepared, pretreated with 50 uM PLX4720 to inhibit coprecipitating RAF activity, and then tested for kinase activity using purified MEK. MEK phosphorylation was detected using a pMEK specific antibody.

    Proc Natl Acad Sci USA 2011 108, 6067-6072. PLX-4720 purchased from Selleck.

    (D)Melanoma cell lines were treated with 0.5 uM Pi-103 and/or 2 uM PLX4720 for 4 h. Samples were analyzed by Western blotting for the indicated proteins. β-Actin served as a loading control. (E) Melanoma cell lines were treated with a dilution series of Pi-103 either alone or in combination with the BRAFV600E inhibitor PLX4720 at a concentration of 3 uM (D10) or 1 uM (453A0) for 3 d. Total cell numbers were determined with a cell titer blue assay. The Y-axis represents the percentage of living cells.

    Genes Dev 2012 26, 1055-69. PLX-4720 purchased from Selleck.

  • PTEN predicts for PLX4720-induced apoptosis. A, basal PTEN and phospho-AKT(pAKT; S473, T308) expression in PTENt (WM164, 451Lu, SK-mel-28, WM983A, WM35, WM51) and PTEN (WM239A, WM266-4, WM793, M233, WM9, 1205Lu) melanoma cell lines. B, MTT assay of PTENt (gray)-expressing versus PTEN (black) cell lines. C, PTENt cells are more sensitive than PTEN cells to PLX4720-mediated apoptosis. Cells treated for 48 hours with 3 or 10 μmol/L PLX4720 before being stained for TMRM and Annexin-V. Apoptosis was measured by flow cytometry. Data shows mean SE mean of 3 independent experiments.*, PTENt cohort significantly different from PTEN cohort(P < 0.05).

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    Loss of PTEN is associated with PI3K/AKT signaling following BRAF inhibition. A, PTENt (WM35, WM164, WM983A) and PTEN (M233, WM9,WM793, 1205Lu) cells were treated with PLX4720 (24 hours: 0.03-3 μmol/L) and probed for phospho-PDK1 (pPDK1), total PDK1, phospho-AKT (pAKT), total AKT (tAKT), phospho-S6 (pS6), and total S6. Numbers indicate relative intensity of pPDK1 normalized to PDK1 and pAKT normalized to tAKT. B, PLX4720 increases pAKT following PTEN knockdown. WM35 cells were incubated with nontargeting siRNA (NT) or 2 different PTEN-specific siRNA's (PTEN) before treatment with either vehicle or PLX4720 (3 μmol/L). C, siRNA knockdown of BRAF increases pAKT in melanoma cell lines that are PTEN. WM164 (PTENt) and WM793 (PTEN) cells were incubated with lipofectamine alone (L), nontargeting siRNA (NT), or BRAF-specific siRNA (BRAF). Protein was extracted, resolved, and probed for BRAF, pAKT, total AKT, and GAPDH.

     

     

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • Dual PI3K/BRAF inhibition upregulates BIM and enhances apoptosis in PTEN cells. A, left, Western blot of 1205Lu cells treated with PLX4720 (3 μmol/L, 48 hours), the PI3K inhibitor GDC-0941 (3 μmol/L, 48 hours), or both drugs in combination (PtG); right, immunofluorescence staining of BIM (green) and DAPI (blue) in PTEN cells following PLX4720 treatment (3 μmol/L, 48 hours), the PI3K inhibitor LY294002 (10 μmol/L, 48 hours), or both drugs in combination (PLXtLY). B, left, immunofluorescence staining of PTEN 1205Lu following combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48hours) increases nuclear localization of FOXO3a (green). DAPI is shown in blue. Magnification 40. Right, combined inhibition (3 μmol/L PLX4720 t 10 μmol/L LY294002, 48 hours) increases PTEN WM793 BIM mRNA levels to those observed with single BRAF inhibition (3 μmol/L PLX4720, 48 hours) in the PTENt WM35. C, PTEN cells were treated with PLX4720 (3 μmol/L, 48 hours), GDC-0941 (3 μmol/L, 48hours), or a combination of the 2 drugs (3Pt3G) before Annexin-V staining was analyzed by flow cytometry (*, P < 0.05 between the drug combination and each inhibitor alone). D, combined BRAF/PI3K inhibitor treatment blocks the escape of 1205Lu cells (PTEN) from therapy. Spheroids of 1205Lu cells were treated with either PLX4720 alone (3 and 10 μmol/L: data shows 3 μmol/L), LY294002 (10 μmol/L) alone or a combination of the 2 drugs for 72 hours. In other studies, spheroids were treated with drugs for 72 hours and then allowed to recover for 120 hours. Micrograph shows viability staining (green ?live cells, red ?dead cells). Magnification 10.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

    LC-MRM identifies differential regulation of BIM in PTENt and PTEN cell lines following PLX4720 treatment. A, representative LC-MRM data showing the fold changes in the expression of Bak, Bax, Bcl-2, Bcl-w, Bcl-xL, BID, BIM, Bok, and Mcl-1 over internal standard in the WM164 (PTENt) and 1205Lu (PTEN) cell lines following treatment with PLX4720 (10 μmol/L, 0-48 hours). Statistical analysis of BIM fold change in PTEN versus PTENt. *, P < 0.05. B, Western blot showing BIM expression following PLX4720 treatment (10 μmol/L, 0-48 hours) in PTEN (WM793, 1205Lu) and WM164 cell lines (PTENt). C, immunofluorescence staining, showing expression of BIM and DAPI staining of PTEN (M233, WM9, WM793, 1205Lu) and PTENt (WM35, WM164, WM983A) cells following PLX4720 treatment (3 μmol/L, 48 hours).D, Western blot showing BAD phosphorylation following treatment with PLX4720 (0-48 hours) in PTEN (WM793,1205Lu) and PTENt WM164. Annexin V binding following treatment with 3 or 10 μmol/L PLX4720 (48 hours) showing increased apoptosis in WM793 stably overexpressing WT BAD. *, P < 0.05.

    Cancer Res 2011 71, 2750-2760. PLX-4720 purchased from Selleck.

  • B-RafV600E mutated melanoma line, SK-MEL-28, was treated with different doses of PLX-4720 for 4 h or 22 h.  Cell lysates were analyzed by Western blotting to determine the levels of phosphorylated MEK1/2 (pMEK1/2) and phosphorylated ERK1/2 (pERK1/2). MEK1/2 is the substrate of B-Raf while ERK1/2 is the substrate of MEK1/2.  Data show that phosphorylation of MEK1/2 and ERK1/2 was significantly inhibited by PLX-4720 treatment although total MEK1/2 or ERK1/2 protein levels were not affected. No pMEK1/2 or pERK1/2 signal was detected even after prolonged exposure, indicating that the inhibitor at 1 μM is very effective in blocking the constitutive kinase activity of B-RafV600E.  This data is consistent with the previous result demonstrating the effect of PLX-4720 in the B-RafV600E mutated melanoma line, A375 – Fig. 2A, Nature 464:431 (2010)

     

     

    Dr. Jong-In Park of Medical College of Wisconsin. PLX-4720 purchased from Selleck.

    A dose titration of PLX-4720 in A375 melanoma cells which possess a V600E B-Raf mutation.Effects of  increasing PLX-4720 dose on Erk phosphorylation and on tumor cell proliferation as determined by MTT  assay are shown.

     

     

    Dr. Daniel C.Cho of Harvard Medical School. PLX-4720 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 PLX-4720是一种有效的,选择性的B-RafV600E抑制剂,无细胞试验中IC50为13 nM,同样有效地作用于c-Raf-1(Y340D和Y341D突变型),作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。
靶点
C-Raf-1 (Y340D/Y341D) [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
BRK [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
6.7 nM 13 nM 130 nM 160 nM
体外研究

PLX-4720高亲和力与活性B-RafV600E和c-Raf-1Y340D/Y341D结合,作用于野生型B-Raf选择性>10倍,作用于其他激酶如Frk, Src, Fak, FGFR, 和Aurora A 选择性>100倍,IC50为1.3-3.4 μM。与有效的选择性相一致, PLX-4720作用于携带B-RafV600E的细胞系,显著抑制ERK磷酸化,IC50为14-46 nM, 但是对携带野生型B-Raf的细胞没有作用效果。PLX-4720 作用于携带B-RafV600E致癌基因(如COLO205, A375, WM2664, 和 COLO829)的肿瘤细胞系,显著抑制细胞生长,GI50 分别为 0.31 μM, 0.50 μM, 1.5 μM, 和 1.7 μM。此外, 1 μM PLX-4720 只有作用于B-RafV600E-阳性1205Lu细胞, 诱导细胞周期停滞和凋亡,而作用于B-Raf 野生型C8161细胞则无此效果。[1]10 μM PLX-4720 处理PTEN+细胞,诱导BIM表达,比PTEN-细胞系(4倍-fold)高14倍,说明PTEN-细胞系抗PLX-4720诱导的凋亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-4475 M2DERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMEe0OVch|ryP M4H1eXNCVkeHUh?=
EoL-1-cell M1fFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwMUSxOlYh|ryP M4D4XHNCVkeHUh?=
C32 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfnfo5KSzVyPUCuNVUyOzFizszN MUPTRW5ITVJ?
M14 MoDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnDU3pKSzVyPUCuNlE4PTdizszN NFPaU5BUSU6JRWK=
CP50-MEL-B NXvLcWVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMkm3PFQh|ryP M1rvNXNCVkeHUh?=
A101D NWrYb2NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;kVWlKSzVyPUCuN|I2QDlizszN MojmV2FPT0WU
G-361 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDqR5ZKSzVyPUCuN|Q3OzdizszN MlmxV2FPT0WU
HT-144 M4HuXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEiySmZKSzVyPUCuN|Y{OjlizszN Mn\UV2FPT0WU
ACN M1\5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rpXWlEPTB;MD6zPFQ4PyEQvF2= MX3TRW5ITVJ?
COLO-829 M3XEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj6PZlKSzVyPUCuN|g6PjhizszN MmjWV2FPT0WU
MEL-HO MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwNEGxO|kh|ryP M3TIZ3NCVkeHUh?=
SH-4 Mkm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K3UmlEPTB;MD60NVQzOiEQvF2= M1\0R3NCVkeHUh?=
SK-MEL-3 NYD0SGk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fsR2lEPTB;MD61NVU3QCEQvF2= NWLuRphPW0GQR1XS
A375 MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHmTWM2OD1yLk[3N|U6KM7:TR?= NWjqfo5MW0GQR1XS
MMAC-SF M2j6XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;UTWM2OD1yLk[4OlE1KM7:TR?= MWHTRW5ITVJ?
BHT-101 NUTi[WlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTkfFlEUUN3ME2wMlcxPzB{IN88US=> NYTjR|JGW0GQR1XS
K5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn24TWM2OD1yLke2NVQ5KM7:TR?= M2PVSnNCVkeHUh?=
BV-173 NUTEfnM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TCTmlEPTB;MD63PVY1PCEQvF2= M1ntPXNCVkeHUh?=
RVH-421 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jWcGlEPTB;MD64Olc6PiEQvF2= MnfCV2FPT0WU
HCC2218 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLuTWM2OD1yLki3PFQ1KM7:TR?= M2fBTHNCVkeHUh?=
WM-115 NXrMTpR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrDO4xKSzVyPUCuPFg3QTJizszN Mor1V2FPT0WU
SK-MEL-28 NHnjWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\RTWM2OD1zLkC0OVY6KM7:TR?= M2XQUXNCVkeHUh?=
COLO-679 M2LVRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\jTWM2OD1zLkGwOFY1KM7:TR?= NHPp[YJUSU6JRWK=
MZ7-mel M4SwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjVdGNKSzVyPUGuNVQ6PjNizszN M2TZZnNCVkeHUh?=
SK-MEL-30 NGXlfWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvmSnpKSzVyPUGuN|M{QDZizszN NFW3RZBUSU6JRWK=
NCI-H209 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHUelhKSzVyPUGuOlA5PiEQvF2= MX;TRW5ITVJ?
HTC-C3 M4CxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXZblZKSzVyPUGuOlYzQTRizszN MkLmV2FPT0WU
KARPAS-45 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy3RZpJUUN3ME2yMlA1QTd6IN88US=> NFvDUVdUSU6JRWK=
NCI-SNU-5 M33Gfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTqTWM2OD1{LkGxPVY6KM7:TR?= NWfrZYJxW0GQR1XS
KP-4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LQfGlEPTB;Mj6zNFc5PyEQvF2= NIrmUWtUSU6JRWK=
PA-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WyemlEPTB;Mj63NlY4OyEQvF2= MkW2V2FPT0WU
HuO-3N1 NEXE[IdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwOEe5OFYh|ryP NVzOWlV4W0GQR1XS
NCI-H358 NVHLVYF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{T3[2lEPTB;Mj65NlI{OiEQvF2= NWXnXnVsW0GQR1XS
CTB-1 NVHvXWx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjoeIxKSzVyPUOuOFAyPzZizszN NEGwOphUSU6JRWK=
697 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHaTWM2OD1|LkW1NlY3KM7:TR?= M2f0T3NCVkeHUh?=
CP66-MEL NYHZeI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTRwMUW5Nlch|ryP M1vLXnNCVkeHUh?=
NB13 MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LmVGlEPTB;ND60PVE4QSEQvF2= MnjsV2FPT0WU
DBTRG-05MG NUPGVItXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTRwNUOzNlUh|ryP M{XjO3NCVkeHUh?=
A2058 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny1TWM2OD12LkeyNVY1KM7:TR?= MUPTRW5ITVJ?
KG-1 NYnNeWlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jtSWlEPTB;ND63N|kxQCEQvF2= NFPHOlNUSU6JRWK=
8305C MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofuTWM2OD13LkG4O|Mh|ryP M{PMVXNCVkeHUh?=
RPMI-7951 MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS5ToxKSzVyPUWuPFAzQDNizszN NHHwZoRUSU6JRWK=
CHL-1 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn2R|llUUN3ME21Mlk4PjB|IN88US=> NHHGUmNUSU6JRWK=
TI-73 NFLaXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH6xZ|RKSzVyPU[uNFA6ODJizszN NV7Yb3h2W0GQR1XS
HT-1080 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjWRnRoUUN3ME22MlExQTR4IN88US=> NXqwflU4W0GQR1XS
ES5 NXLQU41TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\h[o5ZUUN3ME22MlE1QTJ2IN88US=> MkjKV2FPT0WU
8-MG-BA M1rORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTZwMUixNlkh|ryP M2HjPXNCVkeHUh?=
NB7 M1HSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLtNm42UUN3ME22MlIyOzd|IN88US=> MnP3V2FPT0WU
H4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTZwMkK0PVMh|ryP MUfTRW5ITVJ?
CAL-72 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4G0PGlEPTB;Nj60OVQzOyEQvF2= NV\W[XpEW0GQR1XS
HCC1806 M1nQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PxOmlEPTB;Nj64NVk{OSEQvF2= M1v4UnNCVkeHUh?=
BCPAP MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTdwMkG3OlQh|ryP MXXTRW5ITVJ?
LB2241-RCC Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTdwM{[5NFch|ryP NHrwUlVUSU6JRWK=
COLO-741 M2L5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T2fmlEPTB;OD6wNVY4QSEQvF2= MkL5V2FPT0WU
HSC-3 Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRThwMEewOlgh|ryP M1XlWnNCVkeHUh?=
SW982 NF7RbHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRThwNEG1NVYh|ryP M{X5[HNCVkeHUh?=
GCT NIfmfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRThwN{WzNVQh|ryP NFfzXWFUSU6JRWK=
KY821 M3zQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnHeppKSzVyPUmuNFUyPzhizszN MmrlV2FPT0WU
JVM-3 NH[5Z5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTlwNU[5PVkh|ryP M{WyN3NCVkeHUh?=
RS4-11 M3XTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fUeGlEPTB;OT62NFQ5KM7:TR?= NVnhcY97W0GQR1XS
VA-ES-BJ NYXxTYg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS4TWM2OD1zMD6wNVQ6KM7:TR?= NIXBXmpUSU6JRWK=
A431 NV\zZldVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFyLkSyNVIh|ryP MlfzV2FPT0WU
LXF-289 MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFyLkS1PEDPxE1? NFn1b|BUSU6JRWK=
SK-MEL-24 NF;xWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrwZWRCUUN3ME2xNE45Ojd2IN88US=> MULTRW5ITVJ?
NOS-1 MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\2VWlEPTB;MUCuPFQ4OiEQvF2= NGTTXo5USU6JRWK=
KNS-62 M32xdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\UWGlEPTB;MUGuNlQxPCEQvF2= NVf0WVNVW0GQR1XS
SK-HEP-1 NH3BfWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jVbmlEPTB;MUGuN|UzPyEQvF2= MoHsV2FPT0WU
A3-KAW MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFzLkexO|gh|ryP MnXnV2FPT0WU
SK-LU-1 NHzsS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF{LkK2OVUh|ryP MULTRW5ITVJ?
TYK-nu MoPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33TW2lEPTB;MUKuN|k{OiEQvF2= M13Gc3NCVkeHUh?=
NMC-G1 M4niS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfp[4VxUUN3ME2xNk43ODZ{IN88US=> MlPUV2FPT0WU
BB65-RCC MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF{LkexOlkh|ryP MWjTRW5ITVJ?
QIMR-WIL NFP5eodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF{Lki4N|Mh|ryP M2HKb3NCVkeHUh?=
D-566MG NYHFVVBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33TNmlEPTB;MUOuPVU4PiEQvF2= MkLaV2FPT0WU
KYSE-140 Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF2LkC3OVMh|ryP Moj3V2FPT0WU
SCC-4 NXzYUpJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF2LkOzOVkh|ryP Mnn1V2FPT0WU
U251 NGnpbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj0fIN[UUN3ME2xOE45PDl{IN88US=> NUK1R5UzW0GQR1XS
D-542MG M4e3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjuU2VKSzVyPUG0MlkzOjJizszN MYfTRW5ITVJ?
LAMA-84 M4rGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTwbnJKSzVyPUG0Mlk6OzJizszN Mmj0V2FPT0WU
NCI-H720 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTF3LkK2PFQh|ryP Ml7UV2FPT0WU
DEL NF3tSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXie4FKSzVyPUG1MlQzQTNizszN NVu4[INkW0GQR1XS
SBC-1 NF3rbWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7S[VBKSzVyPUG1MlQ{ODVizszN MnW0V2FPT0WU
ECC10 NH[5VXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnJXZVKSzVyPUG1MlQ1PThizszN NHrjVXJUSU6JRWK=
Daoy MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7rXm43UUN3ME2xOU44PjF4IN88US=> MmjMV2FPT0WU
SCH NH7u[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTF3Lke4N|Uh|ryP MYTTRW5ITVJ?
MZ2-MEL NWPPdYV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\afI5tUUN3ME2xOk4xPjR4IN88US=> M2LyZ3NCVkeHUh?=
CAL-12T NIrkPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFX3ZndKSzVyPUG2MlQ5PjJizszN M3f6TnNCVkeHUh?=
KE-37 NIjLfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTF4LkixNFch|ryP MoP2V2FPT0WU
LS-411N NYH6[JcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO2emJKSzVyPUG3MlEyQCEQvF2= NV3OS5BkW0GQR1XS
NCI-H2228 NHrQ[lNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13mTWlEPTB;MUeuN|A4OSEQvF2= M1fsWnNCVkeHUh?=
SK-MEL-2 NH;GNYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\pTHFKSzVyPUG3MlQ6PjVizszN M1vZUHNCVkeHUh?=
HN Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrmSJBKSzVyPUG3MlczPDhizszN M4jXTnNCVkeHUh?=
NCI-H1648 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXvR4FKSzVyPUG3MlgyQCEQvF2= NFO2bZlUSU6JRWK=
IA-LM NYG4[HBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzlUINxUUN3ME2xPE4{OTd{IN88US=> NVrxeldZW0GQR1XS
EW-13 NUnSVXV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPyTWM2OD1zOD61O|A5KM7:TR?= NV7WSI5iW0GQR1XS
YKG-1 NXfkcGN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfmTWM2OD1zOT61O|EyKM7:TR?= NFLUUJJUSU6JRWK=
KNS-81-FD NGr3eWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXxTWM2OD1zOT61PFU5KM7:TR?= NXHVfnVXW0GQR1XS
23132-87 NG\LO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nwTGlEPTB;MUmuO|Y1OiEQvF2= M3PlTnNCVkeHUh?=
NUGC-3 NW\jcIY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPlO2xqUUN3ME2xPU46QDh5IN88US=> MWnTRW5ITVJ?
5637 NHnsRnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITF[G1KSzVyPUKwMlA1PzhizszN MWrTRW5ITVJ?
NCI-H1755 NV7TSGt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nCUWlEPTB;MkCuOFc3PCEQvF2= MnvZV2FPT0WU
RH-18 NIrIbVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTLTWM2OD1{MD61O|Q5KM7:TR?= NGDP[IlUSU6JRWK=
RXF393 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJyLk[3OVYh|ryP MWTTRW5ITVJ?
LU-134-A M1PLcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PlU2lEPTB;MkCuO|A2PiEQvF2= MmDOV2FPT0WU
TE-12 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nXdWlEPTB;MkCuO|IxOSEQvF2= MVnTRW5ITVJ?
MOLT-4 NGrVbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj4bnFKSzVyPUKxMlE6OTVizszN NH3jcndUSU6JRWK=
IGR-1 NGT4dppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXNTWM2OD1{MT6zO|k3KM7:TR?= M1ruWXNCVkeHUh?=
HOP-92 Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TxNmlEPTB;MkGuOFk5PyEQvF2= MofaV2FPT0WU
SK-MES-1 M{XwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PXbWlEPTB;MkGuO|M5OSEQvF2= M13jVXNCVkeHUh?=
LU-65 NGHOb5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPoTWM2OD1{MT64OlI1KM7:TR?= NULoVJlzW0GQR1XS
MS-1 M3LNRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjsOoZKSzVyPUKyMlEzODNizszN NUT5[HJvW0GQR1XS
LoVo MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHP[o5KSzVyPUKyMlI1PCEQvF2= NFfESI1USU6JRWK=
A704 NYLOd4RqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDjeVNHUUN3ME2yNk42OTV3IN88US=> M3TvdXNCVkeHUh?=
HT-1376 M{Lod2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXPTWM2OD1{Mj62NFU6KM7:TR?= MYPTRW5ITVJ?
IST-MEL1 MmDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nlPWlEPTB;MkKuOlc2OSEQvF2= MlTKV2FPT0WU
Ramos-2G6-4C10 NGi2PZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nLbmlEPTB;MkKuO|M3PiEQvF2= NFXVc4RUSU6JRWK=
T47D NIrjN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[1eGlEPTB;MkKuO|k4QSEQvF2= MlrtV2FPT0WU
HT-1197 NVvIWG1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\tbnk1UUN3ME2yN{4xQDF5IN88US=> M2rMdHNCVkeHUh?=
LB2518-MEL M17TS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7GNm1KSzVyPUKzMlY1OTJizszN NIXqN5ZUSU6JRWK=
J-RT3-T3-5 M{C4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnNTpFKSzVyPUK0Mlc2QTVizszN Mnj2V2FPT0WU
SK-NEP-1 MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnaTWM2OD1{ND64O|Q1KM7:TR?= MWHTRW5ITVJ?
NCI-H526 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzvWooxUUN3ME2yOU4xODJ|IN88US=> MoPEV2FPT0WU
IST-SL1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ3LkK3OVEh|ryP M{XWO3NCVkeHUh?=
HH NYnk[FhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPl[W5[UUN3ME2yOU4{OTl{IN88US=> MnnCV2FPT0WU
NCI-H82 MmDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TXemlEPTB;MkWuPVM5KM7:TR?= MYHTRW5ITVJ?
SNU-449 M2PKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ5LkKwNVgh|ryP NGSxfJNUSU6JRWK=
COR-L23 MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJ5LkK4NVMh|ryP NELX[lNUSU6JRWK=
LOXIMVI MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPIe|hKSzVyPUK3MlM3QCEQvF2= MkDSV2FPT0WU
GR-ST NEC2TlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ5Lk[3NFYh|ryP NVjkW5ZIW0GQR1XS
NCI-SNU-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvHTWM2OD1{Nz65OFQh|ryP M{PsXnNCVkeHUh?=
ALL-PO NXT6fFlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnPRZZKSzVyPUK4MlE3ODRizszN NWjrcXBDW0GQR1XS
ML-2 NHe0V5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJ6LkK4NVQh|ryP M2PUWHNCVkeHUh?=
HOP-62 M1PJTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ6LkexN{DPxE1? MUjTRW5ITVJ?
EGI-1 NIHpUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJ6Lki4OFUh|ryP NYjVWlFDW0GQR1XS
TCCSUP M4XzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j5TWlEPTB;MkiuPVI4OiEQvF2= MlTiV2FPT0WU
LB996-RCC Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke4TWM2OD1{OT61OlgzKM7:TR?= M2nRN3NCVkeHUh?=
LCLC-97TM1 NEP0NJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnDW5BPUUN3ME2zNk4yQTZ2IN88US=> NWq4R2dMW0GQR1XS
NCI-H1304 M1;3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[4XZBHUUN3ME2zNk4{OzBzIN88US=> M2\UNXNCVkeHUh?=
KP-N-YS NFi1TmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN{LkW5O|Mh|ryP NIH2Vm9USU6JRWK=
NCI-H1770 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTYe5FpUUN3ME2zN{4yPjR6IN88US=> MW\TRW5ITVJ?
EM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzWNVZKSzVyPUOzMlY2ODRizszN M2[3T3NCVkeHUh?=
ChaGo-K-1 NH3tbIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2npWWlEPTB;M{OuO|I{PiEQvF2= NIXIcnNUSU6JRWK=
ACHN MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TTcmlEPTB;M{OuPFM5PSEQvF2= Mmf0V2FPT0WU
MN-60 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn6[XlTUUN3ME2zN{45PTR2IN88US=> MkP1V2FPT0WU
EW-18 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml2xTWM2OD1|Mz64PVcyKM7:TR?= M17iVXNCVkeHUh?=
KGN M3;MVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN3LkeyPVIh|ryP MVnTRW5ITVJ?
U031 NYnCRoRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnxSFBqUUN3ME2zOU45OTN{IN88US=> MlXnV2FPT0WU
HMV-II MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT0WVVKSzVyPUO2MlA4PzRizszN M4nl[nNCVkeHUh?=
L-363 M3q2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n1fmlEPTB;M{euOlQ2PSEQvF2= M1G2ZXNCVkeHUh?=
NCI-H1155 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN6LkCwNVUh|ryP Ml\SV2FPT0WU
NCI-H1793 NILZ[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfaTpVKSzVyPUO4MlExOjZizszN MV7TRW5ITVJ?
P30-OHK NIDWbplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnIXWhHUUN3ME2zPE4yOzN{IN88US=> NHm1RVdUSU6JRWK=
AN3-CA Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUW4d3hiUUN3ME2zPE4yPjF3IN88US=> MXvTRW5ITVJ?
UACC-257 NWroVJF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTzTWM2OD1|OD63PUDPxE1? NGi3VFdUSU6JRWK=
MCF7 NH\NfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG2U4ViUUN3ME2zPU45PjJ7IN88US=> M2fWW3NCVkeHUh?=
KP-N-YN MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIT4cG9KSzVyPUSwMlQzQDVizszN Mk\wV2FPT0WU
T98G MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[xXmlEPTB;NECuOFk2PyEQvF2= NWPGeWtGW0GQR1XS
HGC-27 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj0eXJlUUN3ME20N{4zPzRizszN NXLMd5lIW0GQR1XS
NCI-H1092 M2r6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\a[nFKSzVyPUSzMlI5QTVizszN NEDydWRUSU6JRWK=
KARPAS-299 M3m1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTR|LkOwO|Eh|ryP M3f6[XNCVkeHUh?=
LB1047-RCC M{LuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX6dpZKSzVyPUS0Mlk6PTlizszN NF3ZbFBUSU6JRWK=
786-0 NW\nZ3c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;YTmNEUUN3ME20OU43PSEQvF2= NGjSXmlUSU6JRWK=
HCC2157 NWn3SnRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTR4LkCzOVkh|ryP NFG4bYtUSU6JRWK=
NY NWTMWYlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nNWmlEPTB;NE[uNVc4QCEQvF2= MnfmV2FPT0WU
EFM-19 NUHPbWFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELuRYFKSzVyPUS2Mlc2OzNizszN NWHoVlE2W0GQR1XS
EW-16 M4DqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTR4Lke4NFYh|ryP NEe3cmhUSU6JRWK=
UM-UC-3 NGqwVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XHemlEPTB;NE[uPFA2QSEQvF2= NFWwNVlUSU6JRWK=
HT-29 M4LUN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXYSm5LUUN3ME20O{45Pzl{IN88US=> NXnnVXJQW0GQR1XS
LN-405 M{TBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHwTWM2OD12OD6wPFI4KM7:TR?= MmDkV2FPT0WU
NCI-H727 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR6Lke3NlYh|ryP NGHqVXRUSU6JRWK=
D-502MG MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTR6Lkm2O|Yh|ryP M1;5Z3NCVkeHUh?=
GMS-10 M3nURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTR7LkK5O|Qh|ryP NXvkXo5ZW0GQR1XS
MEL-JUSO NGPrN3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTR7LkO0O{DPxE1? M3vXN3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

体内研究 PLX-4720每天按20 mg/kg剂量口服给药依赖B-RafV600E的COLO205移植瘤,显著延迟肿瘤生长,且引起肿瘤衰退, 即使按1 g/kg剂量处理也不会对小鼠造成明显的不利影响。PLX-4720按 100 mg/kg剂量处理 携带B-RafV600E的1205Lu 移植瘤,每天两次,几乎完全消除肿瘤, 而对携带野生型B-Raf的C8161 移植瘤则没有作用活性。PLX-4720 作用于含V600E突变细胞的抗癌效果与阻断MAPK通路相关。[1] PLX-4720每天按30 mg/kg剂量处理8505c肿瘤,显著抑制肿瘤生长,抑制达90%以上,也显著降低远处肺转移。[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]
+ 展开

体外Raf激酶活性实验:

通过测量生物素-MEK蛋白,使用Perkin-Elmer's AlphaScreen 技术测定体外野生型和突变型Raf的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM 生物素-MEK 蛋白,多种ATP浓度,及浓度不断增高的PLX-4720混合物中在室温下进行每组酶(0.1 ng)反应,反应体积为20-μL。 在 2, 5, 8, 10, 20,和 30分钟加入5 μL含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 和 0.3% BSA的溶液终止反应。终止液包括磷酸-MEK抗体, 链霉亲和素包被的供体珠,和AlphaScreen蛋白 A检测试剂盒中的蛋白A受体珠。抗体和小株在终止液中在室温下黑暗温育30分钟。抗体最终按 1:2,000稀释,每个小珠终浓度为 10 μg/mL。实验板在室温下温育1小时,然后在 PerkinElmer AlphaQuest 读数器上读数。
细胞实验:[1]
+ 展开
  • Cell lines: COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, 和C8161
  • Concentrations: 溶于DMSO, 终浓度为~1 mM
  • Incubation Time: 24, 48, 和 72小时
  • Method: 使用不同浓度PLX-4720 for处理细胞 24, 48,和72小时通过 CellTiter-GLO荧光细胞活性检测或MTT实验测定细胞增殖。为了分析细胞周期, 收集上清液和细胞, 制成颗粒,与70%乙醇混合。在使用碘化丙啶 (10 μg/mL)染色前,细胞在0.5 mg/mL RNase I 中37oC下温育1小时,除去残留RNA污染样本。使用EPICS XL仪分析样本。为了测定凋亡, 获得培养基和细胞,制成颗粒,然后使用膜联蛋白-FITC和碘化丙啶染色。然后再使用EPICS XL仪分析样本。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 皮下移植 COLO205 细胞的雌性无胸腺NCr nu/nu小鼠, 携带1205Lu或C8161 细胞的SCID小鼠
  • Formulation: 悬浮于5% DMSO, 1% 甲基纤维素中
  • Dosages: 5, 20, 或100 mg/kg
  • Administration: 口服饲喂,每天一次或两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 83 mg/mL (200.56 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(数据来自Selleck实验检测而非文献):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/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 413.83
化学式

C17H14ClF2N3O3S

CAS号 918505-84-7
稳定性 powder
in solvent
别名 N/A

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

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

常见问题及建议解决方法

  • 问题 1:

    What would you recommend to make working solution for intraperitoneal injection into mice?

  • 回答:

    PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品

Tags: 购买PLX-4720 | PLX-4720供应商 | 采购PLX-4720 | PLX-4720价格 | PLX-4720生产 | 订购PLX-4720 | PLX-4720代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID