store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lifirafenib (Beigene-283) 是新型高效的Raf 激酶和EGFR 抑制剂,对重组BRafV600E 和EGFR 的IC50值分别为 23 和 29 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 396 | 现货 | ||
5 mg | ¥ 897 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 5,230 | 现货 | ||
100 mg | ¥ 7,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,350 | 现货 |
产品描述 | Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively. |
靶点活性 | B-Raf (V600E):23 nM, EGFR:29 nM, EGFR (L858R/T790M):495 nM (IC50) |
体外活性 | BGB-283 potently inhibits BRAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAFV600E and EGFR mutation/amplification.BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation,in BRAFV600E colorectal cancer cell lines. It demonstrates selective cytotoxicity to cell lines harboring BRAFV600E or EGFR mutations. In A431 cells, BGB-283 inhibits the EGF-induced EGFR autophosphorylation on Tyr1068 in a dose-dependent manner. In WiDr colorectal cancer cells, BGB-283 inhibits the feedback activation of EGFR signaling and achieves sustained inhibition of pERK[1] |
体内活性 | The treatment of BGB-283 leads to tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRAFV600E mutation in a dose-dependent manner. BGB-283 has high efficacy in BRAF(V600E) colorectal cancer xenograft models, including Colo205, HT29, and two primary tumor xenografts harboring BRAFV600E mutation. In addition, BGB-283 shows compelling efficacy in a WiDr xenograft model where EGFR reactivation is shown to be induced upon BRAF inhibition. BGB-283 induces tumor regression in HCC827 but not in A431 xenograft. BGB-283 inhibits phosphorylation of both EGFR and ERK1/2 and displays potent antitumor activity in WiDr tumor xenografts. BGB-283 does not induce EGFR feedback activation as reported for vemurafenib. BGB-283 potently inhibits DUSP6 expression, ERK and MEK phosphorylation in vivo when dosed repeatedly. There is no detectable difference on AKT phosphorylation[1]. |
别名 | BGB-283, Beigene-283 |
分子量 | 478.42 |
分子式 | C25H17F3N4O3 |
CAS No. | 1446090-79-4 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (209.02 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0902 mL | 10.4511 mL | 20.9021 mL | 52.2553 mL |
5 mM | 0.418 mL | 2.0902 mL | 4.1804 mL | 10.4511 mL | |
10 mM | 0.209 mL | 1.0451 mL | 2.0902 mL | 5.2255 mL | |
20 mM | 0.1045 mL | 0.5226 mL | 1.0451 mL | 2.6128 mL | |
50 mM | 0.0418 mL | 0.209 mL | 0.418 mL | 1.0451 mL | |
100 mM | 0.0209 mL | 0.1045 mL | 0.209 mL | 0.5226 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。
Lifirafenib 1446090-79-4 Angiogenesis JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors EGFR Raf Epidermal growth factor receptor ErbB-1 inhibit BGB-283 Raf kinases Beigene-283 Inhibitor HER1 BGB 283 BGB283 inhibitor