Vemurafenib (PLX4032)
别名: RG7204, RO5185426,PLX4032 中文名称：维罗非尼
Vemurafenib (PLX4032, RG7204, RO5185426)是一种新型有效的B-RafV600E抑制剂，IC50为31 nM。Vemurafenib对B-RafV600E的选择性比对野生型B-Raf的选择性高10倍，在细胞实验中，选择性可高100倍以上。Vemurafenib (PLX4032, RG7204) 可诱导自噬。
Vemurafenib (PLX4032) Chemical Structure
CAS: 918504-65-1
产品质控
批次：
纯度：
99.98%
99.98
Vemurafenib (PLX4032)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Calu-6 | Function Assay | 1 μM | 1 h | Activates MEK/ERK in cells with wild-type BRAF | 20179705 |
| C4 | Function Assay | 3 μM | 48 h | Increases collagen synthesis and decreases IL-8 expression | 25989506 |
| VMM12 | Function Assay | 3 μM | 48 h | Increases collagen synthesis and decreases IL-9 expression | 25989506 |
| SKMEL19 | Function Assay | 6 μM | 48 h | Triggers ER stress | 23362240 |
| ARO | Function Assay | 10 μM | 72 h | Induces the reexpression of the NIS pump | 18458053 |
| TPCI | Growth Inhibition Assay | 100 μM | 96 h | IC50=10.77 μM | 18458053 |
| ARO | Growth Inhibition Assay | 100 μM | 96 h | IC50=205 nM | 18458053 |
| NPA | Growth Inhibition Assay | 100 μM | 96 h | IC50=26 nM | 18458053 |
| A375 | Growth Inhibition Assay | 100 μM | 96 h | IC50=47 nM | 18458053 |
| UKF-NB-3 (ABCB1) | Function Assay | 1.25 µM | 2 h | Enhances accumulation of the fluorescent ABCB1 substrate rhodamine 123 | 24735766 |
| UKF-NB-3 | Function Assay | 1.25 µM | 2 h | Significantly affects on accumulation of the fluorescent ABCB1 substrate rhodamine 123 | 24735766 |
| Calu6 | Function assay | 3 uM | 2 hrs | Activation of CRAF in human Calu6 cells assessed as increase in MEK phosphorylation at 3 uM after 2 hrs by FRET assay | 28557458 |
| UACC-903 | Cytotoxicity assay | 25 uM | 48 hrs | Cytotoxicity against human UACC-903 cells assessed as cell viability at 25 uM after 48 hrs by MTT assay relative to control, IC50 = 3.6 μM. | 29133035 |
| A375 | Apoptosis Assay | 10 μM | Promotes apoptotic death | 18458053 | |
| HCT116 | Function assay | 0.34 to 20000 nM | Paradoxical activation of RAS/RAF/MEK signaling pathway in human HCT116 cells expressing wild type BRAF assessed as ERK phosphorylation at 0.34 to 20000 nM | 25965804 | |
| BHT101 (BRAF WT/V600E) | Growth Inhibition Assay | 96 h | EC50=97 nM | 19880792 | |
| BCPAP (BRAF WT/V600E) | Growth Inhibition Assay | 96 h | EC50=78 nM | 19880792 | |
| C643 (HRAS G13R)≥ 500 | Growth Inhibition Assay | 96 h | EC50 ≥ 500 nM | 19880792 | |
| HTH7 (NRAS Q61R) | Growth Inhibition Assay | 96 h | EC50≥ 1000 nM | 19880792 | |
| CAL62 (KRAS G12R) > 1000 > 1000 | Growth Inhibition Assay | 96 h | EC50> 1000 nM | 19880792 | |
| TPC-1 (RET/PTC1) | Growth Inhibition Assay | 96 h | EC50≥1000 nM | 19880792 | |
| PC | Growth Inhibition Assay | 96 h | EC50> 1000 nM | 19880792 | |
| SW1736 (BRAF WT/V600E) | Growth Inhibition Assay | 96 h | EC50=29 nM | 19880792 | |
| 8505C (BRAF V600E/V600E) | Growth Inhibition Assay | 96 h | EC50=57 nM | 19880792 | |
| A375 (BRAFV600E) | Function Assay | 8 h | Increases intracellular ROS and NO levels | 25363644 | |
| A375P | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A375P cells after 48 hrs by MTT assay, IC50 = 0.25 μM. | 24128410 | |
| A375 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A375 cells after 72 hrs by MTT assay, IC50 = 0.18 μM. | 24215818 | |
| SK-MEL-28 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant after 68 hrs by MTS assay, IC50 = 0.48 μM. | 24588073 | |
| insect cell | Function assay | 60 mins | Inhibition of full length human B-Raf V600E mutant expressed in baculovirus infected insect cells assessed as [gamma-33P]incorporation into MEK after 60 mins by scintillation counting, IC50 = 0.031 μM. | 24900315 | |
| MALME-3M | Function assay | 1 hr | Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME-3M cells after 1 hr by fluorescence analysis, IC50 = 0.061 μM. | 24900315 | |
| A375 | Function assay | 1 hr | Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A375 cells after 1 hr by fluorescence analysis, IC50 = 0.19 μM. | 24900315 | |
| COLO205 | Cytotoxicity assay | 4 days | Cytotoxicity against human COLO205 cells after 4 days by CellTiter-Glo assay, EC50 = 0.24 μM. | 24900315 | |
| WM266.4 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay, IC50 = 0.06 μM. | 25267006 | |
| A375 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A375 cells after 48 hrs by MTT assay, IC50 = 0.19 μM. | 25267006 | |
| WM1361 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human WM1361 cells after 48 hrs by MTT assay, IC50 = 1.87 μM. | 25267006 | |
| A375 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375 cells after 72 hrs by CCK8 assay, IC50 = 3.315 μM. | 25462267 | |
| A375 | Function assay | 72 hrs | Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay, IC50 = 0.15 μM. | 25965804 | |
| A375 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay, IC50 = 0.17 μM. | 25965804 | |
| A375 | Function assay | 15 mins | Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50 = 0.26 μM. | 25965804 | |
| A375 | Function assay | 15 mins | Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue, IC50 = 0.95 μM. | 25965804 | |
| NZM20 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human NZM20 cells expressing B-Raf V600E mutant isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay, IC50 = 0.024 μM. | 26005530 | |
| NZM07 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human NZM07 cells expressing B-Raf V600E mutant isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay, IC50 = 0.036 μM. | 26005530 | |
| A375 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay, IC50 = 0.079 μM. | 26005530 | |
| COLO205 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human COLO205 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay, IC50 = 0.309 μM. | 26005530 | |
| SK-MEL-28 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay, IC50 = 0.381 μM. | 26005530 | |
| HT-29 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human HT-29 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay, IC50 = 0.601 μM. | 26005530 | |
| SK-MEL-1 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human SK-MEL-1 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay, IC50 = 1.499 μM. | 26005530 | |
| NZM40 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human NZM40 cells expressing wild type B-Raf isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay, IC50 = 3.01 μM. | 26005530 | |
| NZM09 | Antiproliferative assay | 68 hrs | Antiproliferative activity against human NZM09 cells expressing wild type B-Raf isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay, IC50 = 8.33 μM. | 26005530 | |
| A375P | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375P cells expressing BRAF V600E mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.37 μM. | 26724730 | |
| A375 | Function assay | 1 hr | Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method, IC50 = 0.017 μM. | 27085672 | |
| MIAPaCa2 | Function assay | 1 hr | Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method, EC50 = 2.29 μM. | 27085672 | |
| COLO205 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.044 μM. | 27155899 | |
| HT-29 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.156 μM. | 27155899 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 14.58 μM. | 27155899 | |
| WM266.4 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay, GI50 = 0.21 μM. | 27238841 | |
| WM266.4 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human WM266.4 cells harboring BRAF V600E mutant assessed as cell growth inhibition after 24 hrs by MTT assay, IC50 = 0.07 μM. | 27634195 | |
| A375 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 24 hrs by MTT assay, IC50 = 0.21 μM. | 27634195 | |
| WM1361 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human WM1361 cells assessed as cell growth inhibition after 24 hrs by MTT assay, IC50 = 1.86 μM. | 27634195 | |
| SK-MEL-28 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as concentration required for total growth inhibition measured after 48 hrs resazurin assay, TGI = 2 μM. | 27774137 | |
| SK-MEL-28 | Growth inhibition assay | 1 hr | Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant preincubated for 1 hr followed by irradiation of 1.13 kW/m2 UV-light for 5 mins measured after 48 hrs resazurin assay | 27774137 | |
| A375 | Antiproliferative assay | 72 hrs | Antiproliferative activity human A375 cells after 72 hrs by cell titer-glo luminescence assay, IC50 = 0.7 μM. | 28242553 | |
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity human COLO205 cells after 72 hrs by cell titer-glo luminescence assay, IC50 = 5.16 μM. | 28242553 | |
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity human HepG2 cells after 72 hrs by cell titer-glo luminescence assay, IC50 = 5.48 μM. | 28242553 | |
| SK-MEL-2 | Antiproliferative assay | 72 hrs | Antiproliferative activity human SK-MEL-2 cells after 72 hrs by cell titer-glo luminescence assay, IC50 = 5.64 μM. | 28242553 | |
| K562 | Function assay | 1 hr | Stabilization of BRAF in human K562 cells after 1 hr by thermal shift assay, EC50 = 0.79433 μM. | 28280261 | |
| K562 | Function assay | 1 hr | Stabilization of FECH in human K562 cells after 1 hr by thermal shift assay, EC50 = 5.01187 μM. | 28280261 | |
| A375M | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375M cells harboring BRAF V600E mutant after 72 hrs by MTT assay, IC50 = 0.5 μM. | 28458134 | |
| 1205 Lu | Antiproliferative assay | 72 hrs | Antiproliferative activity against human 1205 Lu cells harboring BRAF V600E mutant after 72 hrs by MTT assay, IC50 = 2 μM. | 28458134 | |
| A375M | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A375M cells harboring BRAF V600E mutant after 48 hrs by MTT assay, IC50 = 2.05 μM. | 28458134 | |
| UACC-903 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 72 hrs by MTT assay, IC50 = 2.7 μM. | 28458134 | |
| 1205 Lu | Antiproliferative assay | 48 hrs | Antiproliferative activity against human 1205 Lu cells harboring BRAF V600E mutant after 48 hrs by MTT assay, IC50 = 7.6 μM. | 28458134 | |
| UACC-903 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 48 hrs by MTT assay, IC50 = 12.3 μM. | 28458134 | |
| CHL-1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay, IC50 = 12.7 μM. | 28458134 | |
| CHL-1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 48 hrs by MTT assay, IC50 = 20 μM. | 28458134 | |
| Sf9 | Function assay | 1 hr | Inhibition of human ZAK (5 to 309 residues) expressed in baculovirus infected Sf9 insect cells using ZAKtide as substrate after 1 hr by mass spectrometry, IC50 = 0.023 μM. | 28586211 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay, IC50 = 0.0314 μM. | 28586211 | |
| CHL-1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay, IC50 = 13.7 μM. | 29133035 | |
| A375 | Function assay | 96 hrs | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in cell proliferation incubated for 96 hrs by MTT assay, IC50 = 0.127 μM. | 29407977 | |
| WM266.4 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay, GI50 = 0.21 μM. | 29940463 | |
| A375 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A375 cells after 48 hrs by MTT assay, GI50 = 0.95 μM. | 29940463 | |
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, GI50 = 1.88 μM. | 29940463 | |
| WM1361 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human WM1361 cells after 48 hrs by MTT assay, GI50 = 20.8 μM. | 29940463 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, GI50 = 25.2 μM. | 29940463 | |
| A375P | Antiproliferative assay | Antiproliferative activity against human A375P cells, IC50 = 0.254 μM. | 22460030 | ||
| A375 | Antiproliferative assay | Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50 = 0.31 μM. | 22808911 | ||
| SK-MEL-28 | Cytotoxicity assay | Cytotoxicity against human SK-MEL-28 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M229 | Cytotoxicity assay | Cytotoxicity against human M229 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M263 | Cytotoxicity assay | Cytotoxicity against human M263 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M321 | Cytotoxicity assay | Cytotoxicity against human M321 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M238 | Cytotoxicity assay | Cytotoxicity against human M238 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M262 | Cytotoxicity assay | Cytotoxicity against human M262 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M249 | Cytotoxicity assay | Cytotoxicity against human M249 cells expressing B-raf V600E mutant, IC50 = 0.1 μM. | 24471466 | ||
| M14 | Cytotoxicity assay | Cytotoxicity against human M14 cells expressing NRAS G12C mutant, IC50 = 0.15 μM. | 24471466 | ||
| A375 | Function assay | Inhibition of B-raf V600E mutant in human A375 cells assessed as reduction in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method, IC50 = 0.0331 μM. | 25462267 | ||
| SK-MEL-2 | Function assay | Inhibition of wild type B-raf in human SK-MEL-2 cells assessed as reduction in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method | 25462267 | ||
| HCT116 | Function assay | Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA, IC50 = 16.6 μM. | 25965804 | ||
| BL21(DE3) | Function assay | Inhibition of N-terminal his-tagged BRAF V600E mutant (448 to 723 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells assessed as phosphorylation of biotinylated-MEK by AlphaScreen assay, IC50 = 0.031 μM. | 26852623 | ||
| HCT116 | Function assay | Stimulation of BRAF-CRAF dimerization in human HCT116 cells by luciferase complementation assay, EC50 = 0.601 μM. | 28557458 | ||
| A375 | Function assay | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay, IC50 = 0.032 μM. | 29461827 | ||
| SK-MEL-32 | Cytotoxicity assay | Cytotoxicity against human SK-MEL-32 cells, IC50 = 0.31 μM. | 29461827 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Vemurafenib (PLX4032, RG7204, RO5185426)是一种新型有效的B-RafV600E抑制剂，IC50为31 nM。Vemurafenib对B-RafV600E的选择性比对野生型B-Raf的选择性高10倍，在细胞实验中，选择性可高100倍以上。Vemurafenib (PLX4032, RG7204) 可诱导自噬。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | PLX4032是新型有效的B-RAFV600E 肿瘤蛋白抑制剂。 | |||||||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | PLX4032抑制B-RAFV600E, C-RAF, 和 野生型B-RAF, IC50分别为31 nM, 48 nM, 和100 nM。PLX4032 也抑制一些非-RAF激酶,包括ACK1, KHS1,和SRMS, IC50 为18 nM 到51 nM。[1] PLX4032作用于黑色素瘤细胞系，抑制效果依赖于B-RAF突变状态，因为PLX4032有效抑制含B-RAFV600突变的细胞, 包括V600E, V600D, V600K, 和V600R, 但是对野生型或其他突变没有作用效果。PLX4032作用于MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和A2058细胞时，IC50为20 nM 到 1 μM。0.1 μM 到30 μM PLX4032 也抑制MEK1/2 和ERK1/2磷酸化作用。[2] PLX4032高效作用于黑色素瘤的治疗 ，因为PLX4032有效抑制B-RAFV600E。PLX4032作用于结肠癌细胞，抑制B-RAF V600E导致 EGFR激活的快速回应，可用于补偿PLX4032抑制的细胞增殖。[3] | |||
|---|---|---|---|---|
| 激酶实验 | RAF激酶活性测定 | |||
| 通过测量生物素化的BAD蛋白磷酸化而测定野生型RAF和突变型的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% (v/v) Tween-20, 50 nM 生物素-BAD 蛋白，和 1 mM ATP 的混合物中室温下进行反应。加入5 μL 含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 0.3% (w/v) 牛血清蛋白 (BSA)的溶液，5分钟后，反应终止。终止溶液也包含p-BAD (Ser112) 抗体,链霉亲和素包被的供体小珠，蛋白A 受体小珠。抗体和小珠在终止溶液中黑暗环境下室温预温育30分钟。 最终抗体被稀释2000倍，每个小珠的终浓度为10 μg/mL。重复做三次单独纯化蛋白实验，去不同两批的平均值作为突变活性。 | ||||
| 细胞实验 | 细胞系 | MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和 A2058 细胞 | ||
| 浓度 | 0–10 μM , 溶于 DMSO | |||
| 孵育时间 | 5 天 | |||
| 方法 | 通过MTT 实验测评细胞增殖。细胞按每孔1000到5000个接种在96孔板上，体积为180 μL。PLX4032按最终实验浓度的10倍储备在含1% DMSO的培养基中。细胞接种24小时后, 加入20 μL适当稀释的PLX4032。接种6天后，进行增殖实验。计算抑制百分数，根据抑制百分数与浓度的对数的回归分析测定IC50值。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-ERK / p-CRAF p-MEK(S217/221) / pAKT(T308) / p-AKT(S473) / p-P70 S6K(T389) / p-S6(Ser235-236) / P-4EB-P1 Bax / Bcl2 / Bcl-xl / BIM / Mcl1 |
|
22448344 | |
| Growth inhibition assay | Cell viability |
|
29179510 | |
| Immunofluorescence | uPAR / α5-β1 p-Akt(Thr308) |
|
30611716 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | PLX4032按6 mg/kg-20 mg/kg 剂量作用于B-RAFV600E-突变鼠移植瘤模型，抑制肿瘤生长。[1] PLX4032按12.5 mg/kg-100 mg/kg剂量作用于携带LOX, Colo829, 和A375移植瘤小鼠，抑制肿瘤生长，延长小鼠寿命。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 携带LOX, Colo829, 和A375移植瘤细胞的无胸腺裸鼠 |
| Dosages | 12.5 mg/kg–100 mg/kg | |
| Administration | 口服饲喂，每天两次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05768178 | Recruiting | Solid Tumor|Haematological Malignancy|Melanoma|Thyroid Cancer Papillary|Ovarian Neoplasms|Colorectal Neoplasms|Laryngeal Neoplasms|Carcinoma Non-Small-Cell Lung|Glioma|Multiple Myeloma|Erdheim-Chester Disease|Thyroid Carcinoma Anaplastic |
Cancer Research UK|University of Manchester|University of Birmingham|Royal Marsden NHS Foundation Trust|Hoffmann-La Roche |
March 1 2023 | Phase 2|Phase 3 |
| NCT05068752 | Recruiting | Pancreas Cancer |
HonorHealth Research Institute|Bayer|Genentech Inc. |
October 28 2021 | Phase 2 |
| NCT03410875 | Active not recruiting | Hairy Cell Leukemia|Leukemia|Leukemia Hairy Cell |
Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Yale University |
February 9 2018 | Phase 2 |
| NCT03013491 | Completed | Solid Tumor|Lymphoma |
CytomX Therapeutics |
January 2017 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 489.92 | 分子式 | C23H18ClF2N3O3S |
| CAS号 | 918504-65-1 | SDF | Download Vemurafenib (PLX4032) SDF |
| Smiles | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)Cl)F | ||
| 储存条件(自收到货起) | 3年 -20°C(避光) 粉状 1年 -80°C(避光) 溶于溶剂 |
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体外溶解度 |
DMSO : 98 mg/mL ( (200.03 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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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:
How about the half-life of Vemurafenib(S1267)?
回答：
It was reported that the half-life of the compound is 57 hours.
问题 2:
The vemurafenib power, when prepared in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O solutions, form a pellet down the tube?
回答：
When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first. If it dissolves not readily, please sonicate and warm in the water bath at about 45 degree. Then add PEG and Tween. After they mixed homogeneously, then dilute with water.
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