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激酶

Linifanib (ABT-869)

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
L126993-50mg 796967-16-3 询价
L126993-5mg 796967-16-3 询价
L126993-10mg 796967-16-3 询价
产品介绍

  • 分子式 C21H18FN5O
  • 分子量375.41

属性

溶解性 Soluble in water (<1 mg/ml) at 25 °C, DMSO (~20 mg/ml), DMF (~20 mg/ml), 1:5 DMSO:PBS (pH 7.2) (~0.2 mg/ml), ethanol (5 mg/ml) at 25 °C, and methanol.
存贮条件 储存温度-20°C

描述

应用 A VEGF (Flk/Flt) and PDGFR inhibitor.
产品介绍 Linifanib (ABT-869)是一种新型,有效,ATP竞争性VEGFR/PDGFR抑制剂,同时抑制KDR, CSF-1R, Flt-1/3和PDGFRβ,其IC50分别为4 nM, 3 nM, 3 nM/4 nM和66 nM ,对具有突变激酶依赖性的癌细胞(即FLT3)最有效。Phase 3。
备注 Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent canc
生化机理 ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (Flt/Flk) and PDGFR families (e.g., KDR, Flt1, Flt3, Flt4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM. ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50 > 1 μM). ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50 = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage. In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy in solid tumors including lung and hepatocellular carcinomas.
别名 N-[4-(3-氨基-1H-吲唑-4-基)苯基]-N'-(2-氟-5-甲基苯基)脲;ABT-869; AL-39324; ABT 869; ABT869; AL 39324; AL39324;1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea;N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea

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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