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RAF265

RAF265

产品编号 T6296   CAS 927880-90-8
别名: CHIR-265

RAF265 (CHIR-265) 是一种 RAF/VEGFR2抑制剂。

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RAF265 Chemical Structure
RAF265, CAS 927880-90-8
规格 价格/CNY 货期 数量
1 mg ¥ 433 现货
2 mg ¥ 623 现货
5 mg ¥ 937 现货
10 mg ¥ 1,490 现货
25 mg ¥ 2,830 现货
50 mg ¥ 4,180 现货
100 mg ¥ 5,990 现货
1 mL * 10 mM (in DMSO) ¥ 1,130 现货
产品目录号及名称: RAF265 (T6296)
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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 RAF265 (CHIR-265) (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.
靶点活性 B-Raf:3-60 nM, C-Raf:3-60 nM, VEGFR2:30 nM(EC50)
体外活性 RAF265 inhibits C-Raf, wild type B-Raf and mutant (V600E) B-Raf. RAF265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. Raf kinase inhibition by RAF265 in mutant B-Raf melanoma cell lines causes cell cycle arrest and induces apoptosis, mimicking the effect of Raf RNAi in these cells. RAF265 also potently inhibits the phosphorylation of VEGFR2 and proliferation of VEGF-stimulated hMVEC. [1] In HT29 and MDAMB231 cells, RAF265 shows inhibitory activity with IC20 of 1 to 3 μM and IC50 of 5 to 10 μM, respectively. While RAF265 leads to a significant decrease in clonogenic survival in all tested cell lines, which means that RAF265 induces a dominant effect on clonogenic survival. Addition of RAF265 to RAD001 in HCT116 cells could lead to moderately decreased AKT, S6 protein, and 4EBP1 phosphorylation. [2] Raf265 markedly reduces the protein level of Bcl-2 and great inhibitory in CM- and NCI-H727 cells, while having no effect on the TRAIL susceptibility of BON1 and GOT1 cells. [3] Protein kinase D3 (PRKD3) that when knocked down could enhance cell killing by RAF265 in A2058 melanoma cells, which prevent reactivation of MAPK signaling, induce PARP cleavage, increase caspase activity, interrupt cell-cycle progression, and inhibit colony formation. [4]
体内活性 RAF265 shows 71% to 72% TVI% (tumor volume inhibition percentage) in HCT116 xenografts at 12 mg/kg. While the combination of RAF265 and RAD001 shows enhanced antitumor activity with increased T10 (time to achieve a relative tumor volume of 10 times the initial tumor volume) and tumor growth delay. The combination of RAD001 and RAF265 also significantly enhances the activation of caspase-3 in HCT116 and MDAMB231 but not in A549 xenografts. [2] RAF265 inhibits FDG (2-deoxy-2-[18F]fluoro-d-glucose) accumulation and decreases the tumor volumes in A375M xenografts by orally dosed of 100 mg/kg. [5]
激酶实验 Assay Protocol: Raf and Mek are combined at 2 × final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2. 0.1 mM EDTA and 1 mM DTT) and dispensed 15 μL per well in polypropylene assay plates. Background levels are determined in wells containing Mek and DMSO without Raf. To the Raf/Mek containing wells is added 3 μL of 10 × of RAF265 diluted in 100% DMSO. The raf kinase activity reaction is started by the addition of 12 μL per well of 2.5 × 33P-ATP diluted in assay buffer. After 45-60 minutes, the reactions are stopped with the addition of 70 μL of stop reagent (30 mM EDTA). Filtration plates are pre-wetted for 5 min with 70% ethanol, and then rinsed by filtration with wash buffer. Samples (90 μL) from the reaction wells are then transferred to the filtration plates. The filtration plates are washed 6 × with wash buffer using Millipore filtration apparatus. The plates are dried and 100 μL per well of scintillation fluid is added. The CPM is then determined using a Wallac Microbeta 1450 reader.
细胞实验 The MTT assay and Bliss additivism model are used to assess the effect of RAF265 on cell viability. In each well of a 96-well plate, 1 × 104 cells are grown in 200 μL of medium. After 24 hours, RAF265 is added to achieve a final concentration of 0.1 to 10 μM. After 48 hours of treatment, 20 μL of 5 mg/mL MTT solution in PBS is added to each well. After 4 hours, supernatant is removed and formazan crystals are discarded in 200 μL of DMSO. Absorbance is then measured at 595 nm using an absorbance plate reader. Data are expressed as the percentage of viable cells.(Only for Reference)
别名 CHIR-265
分子量 518.41
分子式 C24H16F6N6O
CAS No. 927880-90-8

存储

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

溶解度

DMSO: 51.8 mg/mL (100 mM)

Ethanol: 10.4 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 1.929 mL 9.6449 mL 19.2898 mL 48.2244 mL
5 mM 0.3858 mL 1.929 mL 3.858 mL 9.6449 mL
10 mM 0.1929 mL 0.9645 mL 1.929 mL 4.8224 mL
20 mM 0.0964 mL 0.4822 mL 0.9645 mL 2.4112 mL
DMSO 50 mM 0.0386 mL 0.1929 mL 0.3858 mL 0.9645 mL
100 mM 0.0193 mL 0.0964 mL 0.1929 mL 0.4822 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. AACR Meeting Abstracts 2008;2008:4876. 2. Pérez-Rivera AA, et al. Mutat Res, 2009, 672(1), 27-39 3. Zitzmann K, et al. Endocr Relat Cancer, 2011, 18(2), 277-285. 4. Chen J, et al. Cancer Res, 2011, 71(12), 4280-4291. 5. Tseng JR, et al. Neoplasia, 2011, 13(3), 266-275.
Exarafenib Vemurafenib Effusanin A Lifirafenib I-37 free base( 2359690-13-2(free base)) Dabrafenib TAK-632 Belvarafenib

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 酪氨酸激酶分子库 抗肥胖化合物库 抗癌化合物库 血管生成库 抗心血管疾病化合物库 细胞重编程化合物库 细胞因子抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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

RAF265 927880-90-8 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors VEGFR Raf CHIR-265 inhibit Inhibitor RAF 265 Vascular endothelial growth factor receptor CHIR265 Raf kinases RAF-265 CHIR 265 inhibitor

 

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