化合物Lifirafenib (BGB-283) T22272
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mg | 1446090-79-4 | ¥894.00 | 询底价 |
100 mg | 1446090-79-4 | 面议 | 询底价 |
5 mg | 1446090-79-4 | ¥538.00 | 询底价 |
25 mg | 1446090-79-4 | ¥1,780.00 | 询底价 |
1 mL | 1446090-79-4 | ¥793.00 | 询底价 |
50 mg | 1446090-79-4 | ¥3,130.00 | 询底价 |
1 mg | 1446090-79-4 | ¥237.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Lifirafenib
描述: 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。
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].
存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 100 mg/mL (209.02 mM)
关键字: Epidermal growth factor receptor | ErbB-1 | inhibit | EGFR | Raf | Raf kinases | Inhibitor | Lifirafenib | HER1 | BGB 283 | BGB283
相关产品: EGFR/CSC-IN-1 | EGFR-IN-9 | Mubritinib | Butein | PD158780 | Afatinib | lavendustin A | CL-387785 | Tuxobertinib | JCN037
相关库: Anti-Cancer Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途