- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- 新產(chǎn)品
- 聯(lián)系我們
別名: RG7204, RO5185426,PLX4032 中文名稱:維羅非尼
Vemurafenib (PLX4032, RG7204, RO5185426)是一種新型有效的B-RafV600E抑制劑,IC50為31 nM。Vemurafenib對B-RafV600E的選擇性比對野生型B-Raf的選擇性高10倍,在細胞實驗中,選擇性可高100倍以上。Vemurafenib (PLX4032, RG7204) 可誘導(dǎo)自噬。
Vemurafenib (PLX4032) Chemical Structure
CAS: 918504-65-1
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Vemurafenib (PLX4032, RG7204, RO5185426)是一種新型有效的B-RafV600E抑制劑,IC50為31 nM。Vemurafenib對B-RafV600E的選擇性比對野生型B-Raf的選擇性高10倍,在細胞實驗中,選擇性可高100倍以上。Vemurafenib (PLX4032, RG7204) 可誘導(dǎo)自噬。 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
特性 | PLX4032是新型有效的B-RAFV600E 腫瘤蛋白抑制劑。 | |||||||||||
靶點 |
|
體外研究(In Vitro) | ||||
體外研究活性 | PLX4032抑制B-RAFV600E, C-RAF, 和 野生型B-RAF, IC50分別為31 nM, 48 nM, 和100 nM。PLX4032 也抑制一些非-RAF激酶,包括ACK1, KHS1,和SRMS, IC50 為18 nM 到51 nM。[1] PLX4032作用于黑色素瘤細胞系,抑制效果依賴于B-RAF突變狀態(tài),因為PLX4032有效抑制含B-RAFV600突變的細胞, 包括V600E, V600D, V600K, 和V600R, 但是對野生型或其他突變沒有作用效果。PLX4032作用于MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和A2058細胞時,IC50為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療 ,因為PLX4032有效抑制B-RAFV600E。PLX4032作用于結(jié)腸癌細胞,抑制B-RAF V600E導(dǎo)致 EGFR激活的快速回應(yīng),可用于補償PLX4032抑制的細胞增殖。[3] | |||
---|---|---|---|---|
激酶實驗 | RAF激酶活性測定 | |||
通過測量生物素化的BAD蛋白磷酸化而測定野生型RAF和突變型的激酶活性。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 的混合物中室溫下進行反應(yīng)。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分鐘后,反應(yīng)終止。終止溶液也包含p-BAD (Ser112) 抗體,鏈霉親和素包被的供體小珠,蛋白A 受體小珠??贵w和小珠在終止溶液中黑暗環(huán)境下室溫預(yù)溫育30分鐘。 最終抗體被稀釋2000倍,每個小珠的終濃度為10 μg/mL。重復(fù)做三次單獨純化蛋白實驗,去不同兩批的平均值作為突變活性。 | ||||
細胞實驗 | 細胞系 | MALME-3M, Colo829, Colo38, A375, SK-MEL28, 和 A2058 細胞 | ||
濃度 | 0–10 μM , 溶于 DMSO | |||
孵育時間 | 5 天 | |||
方法 | 通過MTT 實驗測評細胞增殖。細胞按每孔1000到5000個接種在96孔板上,體積為180 μL。PLX4032按最終實驗濃度的10倍儲備在含1% DMSO的培養(yǎng)基中。細胞接種24小時后, 加入20 μL適當稀釋的PLX4032。接種6天后,進行增殖實驗。計算抑制百分數(shù),根據(jù)抑制百分數(shù)與濃度的對數(shù)的回歸分析測定IC50值。 |
|||
實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | PLX4032按6 mg/kg-20 mg/kg 劑量作用于B-RAFV600E-突變鼠移植瘤模型,抑制腫瘤生長。[1] PLX4032按12.5 mg/kg-100 mg/kg劑量作用于攜帶LOX, Colo829, 和A375移植瘤小鼠,抑制腫瘤生長,延長小鼠壽命。[2] | |
---|---|---|
動物實驗 | Animal Models | 攜帶LOX, Colo829, 和A375移植瘤細胞的無胸腺裸鼠 |
Dosages | 12.5 mg/kg–100 mg/kg | |
Administration | 口服飼喂,每天兩次 |
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 |
分子量 | 489.92 | 分子式 | C23H18ClF2N3O3S |
CAS號 | 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 | ||
儲存條件(自收到貨起) | 3年 -20°C(避光) 粉狀 1年 -80°C(避光) 溶于溶劑 |
||
體外溶解度 |
DMSO : 98 mg/mL ( (200.03 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段,您遇到的任何問題,均可以通過撥打我們的熱線電話400-668-6834,或者技術(shù)支持郵箱tech@selleck.cn,直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題,請給我們留言。
* 必填項
問題 1:
How about the half-life of Vemurafenib(S1267)?
回答:
It was reported that the half-life of the compound is 57 hours.
問題 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.