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PLX-4720

PLX-4720

产品编号 T2473   CAS 918505-84-7
别名: PLX4720

PLX-4720 是一种有效且选择性的 B-Raf (V600E) 抑制剂,IC50为 13 nM,与 c-Raf-1(Y340D 和 Y341D 突变)同样有效。

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PLX-4720 Chemical Structure
PLX-4720, CAS 918505-84-7
规格 价格/CNY 货期 数量
10 mg ¥ 465 现货
50 mg ¥ 997 现货
1 mL * 10 mM (in DMSO) ¥ 371 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: PLX-4720 (T2473)
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选择批次  
纯度: 99.89%
纯度: 99.62%
纯度: 99.5%
纯度: 97.78%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).
靶点活性 B-Raf (V600E):13 nM (cell free), B-Raf:160 nM (cell free), C-Raf1 (340D/Y341D):6.7 nM (cell free)
体外活性 PLX4720 inhibits B-Raf(V600E) with an IC50 of 13 nM. Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-Raf(V600E)-bearing tumor cell lines but not in cells lacking oncogenic B-Raf [1]. PLX4720 treatment significantly increased BIM expression in the PTEN+ (>14-fold) compared with the PTEN- cell lines (four-fold). Dual treatment of PTEN- cells with PLX4720 and a PI3K inhibitor enhanced BIM expression at both the mRNA and protein level and increased the level of apoptosis through a mechanism involving AKT3 and the activation of FOXO3a [2].
体内活性 In B-Raf(V600E)-dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity [1]. In vivo, PLX4720 treatment of 8505c orthotopic thyroid tumors inhibited tumor aggressiveness and significantly upregulated the thyroid differentiation markers thyroid transcription factor 1 and paired box gene 8 [3]. Treatment of orthotopic thyroid tumors, initiated 1 week after tumor cell implantation with PLX4720 caused a significant tumor growth delay and decreased distant metastases, without evidence of toxicity [4].
激酶实验 In vitro Raf kinase activities: The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader [1].
细胞实验 Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37 °C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus [1].
动物实验 Female athymic mice (NCr nu/nu) were implanted s.c. on day 0 with 30–60 mg COLO205 tumor fragments. Treatments began on day 11, when the mean estimated tumor mass was 104 mg (range, 95–113 mg). All animals were dosed with vehicle (5% DMSO, 1% methylcellulose) or PLX4720 suspended in vehicle by gavage daily for 14 consecutive days. Tumor burden (mg) was estimated from caliper measurements [1].
别名 PLX4720
分子量 413.83
分子式 C17H14ClF2N3O3S
CAS No. 918505-84-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 77 mg/mL (186.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4165 mL 12.0823 mL 24.1645 mL 60.4113 mL
5 mM 0.4833 mL 2.4165 mL 4.8329 mL 12.0823 mL
10 mM 0.2416 mL 1.2082 mL 2.4165 mL 6.0411 mL
20 mM 0.1208 mL 0.6041 mL 1.2082 mL 3.0206 mL
50 mM 0.0483 mL 0.2416 mL 0.4833 mL 1.2082 mL
100 mM 0.0242 mL 0.1208 mL 0.2416 mL 0.6041 mL

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TargetMol Library Books参考文献

1. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. 2. Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71(7), 2750-2760. 3. Nucera C, et al. Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. Oncologist. 2011;16(3):296-309. 4. Nucera C, et al. B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107(23), 10649-10654.
K-Ras(G12C) inhibitor 9 Indirubin TBAP-001 K-Ras-IN-1 Raf inhibitor 1 BAY-293 Pelitinib AZ 628

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抑制剂库 激酶抑制剂库 抗癌活性化合物库 酪氨酸激酶分子库 免疫/炎症分子化合物库 临床前化合物库 已知活性化合物库 抗癌化合物库 抗前列腺癌化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PLX-4720 918505-84-7 MAPK Raf Inhibitor inhibit Raf kinases PLX 4720 PLX4720 inhibitor

 

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