Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZ 628 是一种泛Raf 激酶抑制剂,抑制B-Raf、B-RafV600E 和c-Raf-1,IC50分别为 105、34和 29 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 262 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 561 | 现货 | ||
10 mg | ¥ 898 | 现货 | ||
25 mg | ¥ 1,820 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,220 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 581 | 现货 |
产品描述 | AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. |
靶点活性 | B-Raf (V600E):34 nM, BRAF:105 nM, C-Raf1:29 nM |
体外活性 | AZ628 prevents activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 suppresses anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. The profile of AZ628 cross-reactivity suggests that similar to sorafenib, AZ628 may be antiangiogenic based on prevention of VEGFR2. [1] AZ628-resistant clones are approximately 100-fold more resistant to AZ628 than the parental cell line, exhibiting IC50 of approximately 10 μM, compared with 0.1 μM for the parental cell line. Effective suppression of p-ERK1/2 levels is observed in the M14 parental cell line following treatment with increasing concentrations of AZ628. AZ628-resistant clones express elevated CRAF. Elevated CRAF expression is a potential mechanism of acquired resistance to continuous AZ628 exposure, resulting in sustained activation of ERK1/2. p-ERK1/2 activity is not significantly inhibited by exposure to AZ628 in one of these three AZ628-insensitive cell lines (Wm1552C). Unlike in the AZ628-resistant M14 cells in which AZ628 fails to suppress the activation of ERK, AZ628 treatment efficiently attenuates ERK activation in the NRAS mutant melanoma cells.[2] |
细胞实验 | Approximately 0.5-2.5 × 105 M14 cells are seeded in 12 or 24 - well plates, respectively, in medium supplemented with 5% FBS. After overnight incubation, the cells are treated with various concentrations of AZ628. Fresh medium and drug is replaced every 2 days until the untreated control wells reached confluence. At this time-point, the media is removed and the cells are fixed in 4% formaldehyde in PBS for 20 minutes at room temperature. Cells are then washed twice with PBS and stained with a 1:5000 solution of the fluorescent nucleic acid stain Syto60. Quantitation of fluorescent signal intensity is carried out at 700 nm, using an Odyssey Infrared Imager. Each experiment is performed in quadruplicate and the results shown represent the average of the four values compared to untreated wells. Error bars represent standard deviation of the 4 values from the mean. High-throughput cell growth/viability assays are performed.(Only for Reference) |
分子量 | 451.52 |
分子式 | C27H25N5O2 |
CAS No. | 878739-06-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | 55.3685 mL |
5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | 11.0737 mL | |
10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL | 5.5369 mL | |
20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7684 mL | |
50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1074 mL | |
100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
AZ 628 878739-06-1 Apoptosis MAPK Raf inhibit Inhibitor AZ628 Raf kinases AZ-628 inhibitor