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

Vemurafenib (PLX4032) Chemical Structure

CAS: 918504-65-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) 746.23 现货
10mg 567.23 现货
50mg 2213.19 现货
200mg 6308.84 现货
1g 10401.3 现货
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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
SRMS [1]
(Cell-free assay)
ACK1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
C-Raf [1]
(Cell-free assay)
MAP4K5 (KHS1) [1]
(Cell-free assay)
点击更多
18 nM 19 nM 31 nM 48 nM 51 nM
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。

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

体外溶解度
批次:

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
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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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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